KR20080041639A - 멜라노코르틴 수용체의 리간드 - Google Patents
멜라노코르틴 수용체의 리간드 Download PDFInfo
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Abstract
본 발명은 하나 이상의 멜라노코르틴 수용체에 대해 리간드로서 작용하는 식: (R2R3)-B1-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-A11-A12-A13-B2-B3-R1에 따른 화합물, 약제학적으로 허용가능한 그의 염, 포유류를 치료하기 위한 상기 화합물의 이용 방법, 및 상기 화합물을 포함하는 포유류 치료에 이용가능한 약학 조성물에 관한 것이다.
Description
본 발명은 한가지 이상의 멜라노코르틴 수용체(MC-R)에 대한 리간드인 펩티드, 약제학적으로 허용가능한 그의 염, 포유류를 치료하기 위한 상기 펩티드의 이용 방법, 및 상기 펩티드를 포함하는 유용한 약학 조성물에 관한 것이다.
멜라노코르틴은 프로-호르몬 프로-오피오멜라노코르틴(POMC; 131개의 아미노산으로 이루어짐)의 번역 후 과정에 의해 형성되는 조절 펩티드 계열이다. POMC는 3종의 호르몬, 즉 멜라노코르틴, 부신 피질 자극 호르몬 및 여러가지 엔도르핀(예, 리포트로핀)으로 진행된다(Cone, et al., Recent Prog. Horm. Res., 51:287-317, (1996); Cone et al., Ann. N.Y. Acad. Sci., 31:342-363, (1993)).
멜라노코르틴은 뇌, 부신, 피부, 고환, 비장, 신장, 난소, 폐, 갑상선, 간, 대장, 소장 및 췌장 등의 매우 다양한 정상적인 인간 조직에서 발견되었다(Tatro, J. B. et al., Endocrinol. 121:1900-1907 (1987); Mountjoy, K. G. et al., Science 257:1248-1251 (1992); Chhajlani, V. et al., FEBS Lett. 309:417-420 (1992); Gantz, I. et al. J. Biol. Chem. 268:8246-8250 (1993) and Gantz, I. et al., J. Biol. Chem. 268:15174-15179 (1993)).
멜라노코르틴 펩티드는 행동 및 기억의 조절, 신경성(neurotrophic) 특성 및 해열 특성에 대한 작용 뿐만 아니라 면역계의 조절에 작용하는 등의 매우 다양한 생리학적인 활성을 보이는 것으로 입증되었다. 잘 알려져 있는 멜라노코르틴의 부신 피질 기능(부신 피질 자극 호르몬, ACTH) 및 멜라노사이트(멜라노사이트 자극 호르몬, MSH)에 대한 작용 이외에도, 또한 심혈관계, 무통증, 체온 조절 및 프로락틴, 황체형성 호르몬 및 생물성 아민(biogenic amine)을 포함한 그외 신경호르몬 물질의 분비를 조절하는 것으로 입증되었다(De Wied, D. et al., Methods Achiev. Exp. Pathol. 15:167-199 (1991); De Wied, D. et al., Physiol. Rev. 62:977-1059 (1982); Guber, K.A. et al., Am. J. Physiol. 257:R681-R694 (1989); Walker J.M. et al., Science 210:1247-1249 (1980); Murphy, M. T. et al., Science 221:192-193 (1983); Ellerkmann, E. et al., Endocrinol. 130:133-138 (1992) and Versteeg, D. H. G. et al., Life Sci. 38:835-840 (1986)).
또한, 눈물샘, 악하선, 췌장, 지방, 방광, 십이지장, 비장, 뇌 및 생식선 조직과 같은 다수의 여러 조직들 뿐만 아니라 악성 흑색종 종양에 분포되어 있는 것으로 확인되었다. 지금까지 5개의 멜라노코르틴 수용체(MC-R)가 확인되었다. 확인된 수용체는, 멜라노사이트에 특이적인 수용체(MC1-R), 부신피질에 특이적인 ACTH 수용체(MC2-R), 멜라코르틴-3 수용체(MC3-R), 멜라코르틴-4 수용체(MC4-R) 및 멜라코르틴-5 수용체(MC5-R)이다. 멜라노코르틴 수용체들 모두 펩티드 호르몬 계열의 멜라노사이트 자극 호르몬(MSH)에 반응한다(Cone, R. D. et al., Ann. N.Y. Acad. Sci., 680:342-363 (1993); Cone, R. D. et al., Recent Prog. Horm. Res., 51:287-318 (1996)).
당업계에서 멜라노사이트 자극 호르몬 수용체(MSH-R), 멜라노트로핀 수용체 또는 멜라노코르틴-1 수용체라고 알려져 있는 MC1-R은, G-단백질이 커플링된 수용체 패밀리에 속하는 315개의 아미노산으로 이루어진 트랜스멤브레인 단백질이다. MC1-R은 MSH와 ACTH 둘다에 대한 수용체이다. MC1-R의 활성은 아데닐레이트 사이클라제를 활성화시키는 G-단백질에 의해 매개된다. MC1-R 수용체는 멜라노사이트와 부신피질 조직 뿐만 아니라, 부신, 백혈구, 폐, 림프절, 난소, 고환, 뇌하수체, 태반, 비장 및 자궁에서 발견된다. 부신 피질 자극 호르몬 수용체(ACTH-R)라고도 불리우는 MC2-R은 멜라노사이트와 부신 피질 조직에서 발견되는 297개의 아미노산으로 이루어진 트랜스멤브레인 단백질이다. MC2-R은 ACTH의 피질 자극 작용을 매개한다. 인간의 MC3-R은 뇌 조직에서 발견되는 360개의 아미노산으로 이루어진 단백질이며, 마우스 및 랫의 MC3-R은 323개의 아미노산으로 이루어진 단백질이다. MC4-R은 뇌, 태반 조직과 내장 조직에서도 발현되는, 332개의 아미노산으로 이루어진 트랜스멤브레인 단백질이다. MC5-R은 부신, 위, 폐 및 비장에서 발현되며 뇌에서도 매우 약하게 발현되는, 325개의 아미노산으로 이루어진 트랜스멤브레인 단백질이다. 또한, MC5-R은 부신 피질의 3개의 층에서도 발현되며, 알도스테론을 생산하는 사구층(zona glomerulosa) 세포에서 주로 발현된다.
그러나, 공지된 5종의 멜라노코르틴 수용체는 그 기능면에서 상이하다. 예를 들어, MC1-R은 강력한 MC1-R 작용제인 α-MSH에 반응하여 색소 형성을 조절하는 G-단백질이 커플링된 수용체이다. MC1-R의 작용성 현상(Agonism)은 유멜라닌을 초래하여 피부암 발병 위험성을 증가시키는, 멜라노사이트의 자극을 발생시킨다. 또 한, MC1-R의 작용성 현상은 신경학적 효과가 있을 수 있다. MC2-R의 활성 자극은 부신 조직의 암화를 유발할 수 있다. 최근, 주요한 MC4-R이 멜라노코르틴 작용제 및 길항제 각각에 대하여 보고된 식욕 부진 및 식욕 촉진 효과의 주된 매개체인 것으로, 약학적으로 확정되었다. MC3-R과 MC5-R에 대한 작용성 효과는 아직 확인되지 않았다.
비만과 악액질과 같은 체중 장애를 치료하기 위한 새로운 치료제 고안에 있어 타겟으로서 멜라노코르틴(MC-R) 수용체가 큰 주목을 받고 있다. 유전적 및 약학적 증거는, 주요한 MC4-R을 주된 타겟으로 지적하고 있다(Giraudo, S. Q. et al., Brain Res., 809:302-306 (1998); Farooqi, I. S. et al., NE J Med., 348:1085-1095 (2003); MacNeil, D. J. et al., Eu. J. Pharm., 44:141-157 (2002); MacNeil, D. J. et al., Eu. J. Pharm., 450:93-109 (2002); Kask, A. et al., NeuroReport, 10:707-711 (1999)). 현재 수용체 선택적인 작용제 및 길항제로 진행된 연구 결과는, 멜라노코르틴 수용체 활성화, 특히 MC4-R의 치료학적 가능성을 입증한다.
작용제, 길항제 또는 하나 이상의 멜라노코르틴 수용체를 활성화시키는 그외 리간드 화합물은, 일반적인 염증(U.S. Patent No. 6,613,874; Catania, A. et al., Pharm. Rev., 56:1-29 (2004)), 염증성 장 질환(U.S. Patent No. 6,713,487; Catania, A. et al., Pharm. Rev., 56:1-29 (2004)), 뇌 염증(Catania, A. et al., Pharm. Rev., 56:1-29 (2004)), 패혈증(U.S. Patent No. 6,613,874; U.S. Patent No. 6,713,487; Catania, A. et al., Pharm. Rev., 56:1-29 (2004)) 및 패혈성 쇼 크(U.S. Patent No. 6,613,874; Catania, A. et al., Pharm. Rev., 56:1-29 (2004))와 같은 급성 및 만성적인 염증 질환; 류마티스 관절염(U.S. Patent No. 6,713,487; Catania, A. et al., Pharm. Rev., 56:1-29 (2004)), 통풍성 관절염(Catania, A. et al., Pharm. Rev., 56:1-29 (2004), Getting, S. J. et al., Curr. Opin. Investig. Drugs, 2:1064-1069 (2001)) 및 다발성 경화증(U.S. Patent No. 6,713,487)과 같은 자가면역과 관련된 질병; 비만(U.S. Patent No. 6,613,874; U.S. Patent No. 6,600,015; Fehm, H. L. et al., J. Clin. Endo. & Metab., 86:1144-1148 (2001); Hansen, M. J. et al., Brain Res., 1039:137-145 (2005); Ye, Z. et al., Peptides, 26:2017-2025 (2005); Farooqi, I. S. et al., NE J Med., 348:1085-1095 (2003); MacNeil, D. J. et al., Eu. J. Pharm., 44:141-157 (2002); MacNeil, D. J. et al., Eu. J. Pharm., 450:93-109 (2002); Kask, A. et al., NeuroReport, 10:707-711 (1999); Schwartz, M. W., J. Clin. Invest., 108:963-964 (2001), Gura, T., Science, 287:1738-1740 (2000), Raffin-Sanson, M. L., Eu. J. Endo., 144:207-208 (2001), Hamilton, B. S. et al., Obesity Res. 10:182-187 (2002)), 섭식 장애(U.S. Patent No. 6,720,324; Fehm, H. L. et al., J. Clin. Endo. & Metab., 86:1144-1148 (2001); Pontillo, J. et al., Bioorganic & Med. Chem. Ltrs., 15:2541-2546 (2005)) 및 프레더-윌리 증후군(GE, Y. et al., Brain Research, 957:42-45 (2002))과 같은 체중 증가를 수반하는 대사성 질환 및 의학적 상태; 식욕 부진(U.S. Patent No. 6,613,874; Wisse, B. R. et al., Endo., 142:3292-3301 (2001)), 다식증(U.S. Patent No. 6,720,324), AIDS성 소모 증(Marsilje, T. H. et al., Bioorg. Med. Chem. Lett., 14:3721-3725 (2004); Markison, S. et al., Endocrinology, 146:2766-2773 (2005)), 악액질(U.S. Patent No. 6,613,874; Lechan, R. M. et al., Endo., 142:3288-3291 (2001); Pontillo, J. et al., Bioorganic & Med. Chem. Ltrs., 15:2541-2546 (2005)), 암 악액질(U.S. Patent No. 6,639,123) 및 허약 노인에서의 쇠약증(U.S. Patent No. 6,639,123)과 같은 체중 감소를 수반하는 대사성 질환 및 의학적 상태; 당뇨병(U.S. Patent No. 6,713,487)과, 망막증(U.S. Patent No. 6,525,019)과 같은 당뇨병 관련 증상 및 당뇨병 합병증; 피부 암(Sturm, R.A., Melanoma Res., 12:405-416 (2002); Bastiens, M. T. et al., Am. J. Hum. Genet., 68:884-894 (2001)) 및 전립선 암(Luscombe, C. J. et al., British J. Cancer, 85:1504-1509 (2001))과 같은 신생물 증식(U.S. Patent No. 6,713,487); 자궁 내막증(U.S. Patent No. 6,713,487), 자궁 출혈증(U.S. Patent No. 6,613,874), 성기능 장애(U.S. Patent No. 6,720,324; Van der Ploeg, L. H. T. et al., PNAS, 99:11381-11386 (2002), Molinoff, P. B. et al., Ann. N.Y. Acad. Sci., 994:96-102 (2003), Hopps, C. V. et al., BJU International, 92:534-538 (2003)), 발기부전((U.S. Patent No. 6,613,874; Diamond, L. E. et al., Urology, 65:755-759 (2005), Wessells, H. et al., Int. J. Impotence Res., 12:S74-S79 (2000), Andersson, K-E. et al., Int. J. Impotence Res., 14:S82-S92 (2002), Bertolini, A. et. al., Sexual Behavior: Pharmacology and Biochemistry, Raven Press, NY, p 247-257 (1975); Wessells, H. et al., Neuroscience, 118:755-762 (2003), Wessells, H. et al., Urology, 56:641-646 (2000), Shadiack, A. M. et al., Society for Neuroscience Abstract, (2003); Wessells, H. et al., J. Urology, 160:389-393 (1998), Rosen, R. C. et al., Int. J. Impotence Res., 16:135-142 (2004), Wessells, H. et al., Peptides, 26:1972-1977 (2005)) 및 여성의 성적 반응 감소(U.S. Patent No. 6,713,487; Fourcroy, J. L., Drugs, 63:1445-1457 (2003))와 같은 생식기 또는 성과 관련된 의학 상태; 장기 이식 거부 반응(U.S. Patent No. 6,713,487; Catania, A. et al., Pharm. Rev., 56:1-29 (2004)), 허혈증 및 재관류 손상(Mioni, C. et al., Eu. J. Pharm., 477:227-234 (2003); Catania, A. et al., Pharm. Rev., 56:1-29 (2004)), 척수 손상의 치료 및 상처 치유를 가속화하기 위한 치료(Sharma H. S. et al., Acta. Nerochir. Suppl., 86:399-405 (2003); Sharma H.S., Ann . N.Y. Acad. Sci . 1053: 407-421 (2005); U.S. Patent No. 6,525,019) 뿐만 아니라 화학요법, 방사선요법, 일시 고정화, 영구 고정화(Harris, R. B. et al., Physiol. Behav., 73:599-608 (2001)) 또는 투석에 의해 유발되는 체중 감소와 같이, 유기체의 치료 또는 상해가 원인인 질환 또는 상태; 출혈성 쇼크(Catania, A. et al., Pharm. Rev., 56:1-29 (2004)), 심장 쇼크(U.S. Patent No. 6,613,874), 저혈량성 쇼크(U.S. Patent No. 6,613,874), 심혈관 장애(U.S. Patent No. 6,613,874) 및 심장 악액질(Markison, S. et al., Endocrinology, 146:2766-2773 (2005))과 같이, 심혈관성 질환 또는 상태; 급성 호흡 곤란 증후군(U.S. Patent No. 6,350,430; Catania, A. et al., Pharm. Rev., 56:1-29 (2004)), 만성 폐색성 폐 질환(U.S. Patent No. 6,713,487), 천식(U.S. Patent No. 6,713,487) 및 폐 섬유증과 같은 폐 질환 또는 상태; 면역 관용을 강화하기 위해(Luger, T. A. et al., Pathobiology, 67:318-321 (1999)), 그리고 특정 알러지(U.S. Patent No. 6,713,487) 또는 장기 이식 거부 반응(U.S. Patent No. 6,713,487; Catania, A. et al., Pharm. Rev., 56:1-29 (2004))과 관련된 바와 같이 면역계에 대한 공격과 싸우기 위하여; 건선(U.S. Patent No. 6,713,487), 피부 색소 형성 감소증(U.S. Patent No. 6,713,487; Ye, Z. et al., Peptides, 26:2017-2025 (2005)), 여드름(Hatta, N. et al., J. Invest. Dermatol., 116:564-570 (2001); Bohm, M. et al., J. Invest. Dermatol., 118:533-539 (2002)), 켈로이드 형성(U.S. Patent No. 6,525,019) 및 피부 암(Sturm, R.A., Melanoma Res., 12:405-416 (2002); Bastiens, M. T. et al., Am. J. Hum. Genet., 68:884-894 (2001))과 같은, 피부 질환 및 상태 치료; 불안(U.S. Patent No. 6,720,324; Pontillo, J. et al., Bioorganic & Med. Chem. Ltrs., 15:2541-2546 (2005)), 우울증(Chaki, S. et al., Peptides, 26:1952-1964 (2005), Bednarek, M. A. et al., Expert Opinion Ther. Patents, 14:327-336 (2004); U.S. Patent No. 6,720,324), 기억력 및 기억 장애(U.S. Patent No. 6,613,874; Voisey, J. et al., Curr. Drug Targets, 4:586-597 (2003)), 통증 인지 조절(U.S. Patent No. 6,613,874; Bertolini, A. et al., J. Endocrinol. Invest., 4:241-251 (1981); Vrinten, D. et al., J. Neuroscience, 20:8131-8137 (2000)) 및 신경성 통증 치료(Pontillo, J. et al., Bioorganic & Med. Chem. Ltrs., 15:2541-2546 (2005))와 같은 행동 체계, 중추 신경계 또는 신경성 상태 및 장애; 알코올 섭취, 알코올 남용 및/또는 알코올 중독과 관련된 상태 및 질환(WO 05/060985; Navarro, M. et al., Alcohol Clin. Exp. Res., 29:949-957 (2005)); 및 신장 악액질(Markison, S. et al., Endocrinology, 146:2766-2773 (2005)) 또는 나트륨뇨(U.S. Patent No. 6,613,874)의 치료와 같은 신장 상태 또는 질환 등의, 매우 다양한 징후를 치료가 필요한 개체나 발병 위험이 있는 개체에서 치료하는데 유용할 것이다.
하나 이상의 멜라노코르틴 수용체를 활성화시키는 작용제, 길항제 또는 기타 리간드 화합물은, 티록신 분비(U.S. Patent No. 6,613,874), 알도스테론 합성 및 분비(U.S. Patent No. 6,613,874), 체온(U.S. Patent No. 6,613,874), 혈압(U.S. Patent No. 6,613,874), 심장 박동수(U.S. Patent No. 6,613,874), 혈관 긴장도(U.S. Patent No. 6,613,874), 뇌 혈류(U.S. Patent No. 6,613,874), 혈당 농도(U.S. Patent No. 6,613,874), 골 대사, 골 형성 또는 발생(Dumont, L. M. et al., Peptides, 26:1929-1935 (2005)), 난소 무게(U.S. Patent No. 6,613,874), 태반 발생(U.S. Patent No. 6,613,874), 프로락틴 및 FSH 분비(U.S. Patent No. 6,613,874), 자궁에서의 태아 성장(U.S. Patent No. 6,613,874), 출산(U.S. Patent No. 6,613,874), 정자 형성(U.S. Patent No. 6,613,874), 피지 및 페로몬 분비(U.S. Patent No. 6,613,874), 신경보호(U.S. Patent No. 6,639,123) 및 신경 성장(U.S. Patent No. 6,613,874) 뿐만 아니라 동기 부여(U.S. Patent No. 6,613,874), 학습(U.S. Patent No. 6,613,874) 및 그외 행태(U.S. Patent No. 6,613,874) 등의, 다양한 정상화 또는 항상성 작용을, 필요한 개체에서 조절하는데 유용할 것이다.
따라서, 본 발명의 목적은 선천적인 멜라노코르틴 수용체 리간드 보다 멜라노코르틴 수용체에 대해 안정성 및 선택성이 높은, 멜라노코르틴 수용체 리간드를 제공하는 것이다.
발명의 개요
일 측면에서, 본 발명은 식 (I)의 화합물 또는 약제학적으로 허용가능한 그의 염에 관한 것이다:
식 (I)
(R2R3)-B1-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-A11-A12-A13-B2-B3-R1
상기 식 (I)에서,
B1은 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 또는 15개의 아미노산을 포함하며 5개 이상의 아미노산은 독립적으로 L-Arg, D-Arg, L-hArg 및 D-hArg으로 이루어진 군으로부터 선택되는 펩티드 모이어티이거나, 또는 B1은 선택적으로 삭제되며;
A1은 Acc, HN-(CH2)m-C(O), L-아미노산 또는 D-아미노산이거나, 삭제되며;
A2는 Cys, D-Cys, hCys, D-hCys, Pen, D-Pen, Asp, 또는 Glu이며;
A3는 Gly, Glu, Ala, β-Ala, Gaba, Aib 또는 D-아미노산이거나, 삭제되며;
A4는 His, 2-Pal, 3-Pal, 4-Pal, Taz, 2-Thi, 3-Thi, 또는 (X1,X2,X3,X4,X5)Phe이며;
A5는 D-Phe, D-1-Nal, D-2-Nal, D-Trp, D-Bal, D-(X1,X2,X3,X4,X5)Phe, D-(Et)Tyr, D-Dip, D-Bip 또는 D-Bpa이며;
A6은 Arg, hArg, Dab, Dap, Lys, Orn 또는 HN-CH((CH2)n-N(R4R5))-C(O)이며;
A7은 Trp, 1-Nal, 2-Nal, Bal, Bip, Dip, Bpa, D-Trp, D-1-Nal, D-2-Nal, D-Bal, D-Dip 또는 D-Bip이며;
A8은 Gly, D-Ala, Acc, Ala, β-Ala, Gaba, Apn, Ahx, Aha, HN-(CH2)s-C(O)이거나, 삭제되며;
A9는 Cys, D-Cys, hCys, D-hCys, Pen, D-Pen, Dab, Dap, Orn 또는 Lys이며;
A10은 Acc, HN-(CH2)t-C(O), Pro, hPro, 3-Hyp, 4-Hyp, Thr, L- 또는 D-아미노산이거나, 삭제되며;
A11은 Pro, hPro, 3-Hyp 또는 4-Hyp이거나, 삭제되며;
A12는 Lys, Dab, Dap, Arg 또는 hArg이거나, 삭제되며;
A13은 Asp 또는 Glu이거나, 삭제되며;
B2는 1, 2, 3, 4 또는 5개의 아미노산을 포함하는 펩티드 모이어티이거나, 삭제되며,
B3은 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 또는 15개의 아미노산을 포함하며 5개 이상의 아미노산은 독립적으로 L-Arg, D-Arg, L-hArg 및 D-hArg로 이루어진 군으로부터 선택되는 펩티드 모이어티이거나, 삭제되며;
R1은 -OH 또는 -NH2이며;
R2 및 R3은 각각 각 경우에 독립적으로, H, (C1-C30)알킬, (C1-C30)헤테로알킬, (C1-C30)아실, (C2-C30)알케닐, (C2-C30)알키닐, 아릴(C1-C30)알킬, 아릴(C1-C30)아실, 치환된 (C1-C30)알킬, 치환된 (C1-C30)헤테로알킬, 치환된 (C1-C30)아실, 치환된 (C2-C30)알케닐, 치환된 (C2-C30)알키닐, 치환된 아릴(C1-C30)알킬 및 치환된 아릴(C1-C30)아실로 이루어진 군으로부터 선택되며;
R4 및 R5는 각각 각 경우에 독립적으로, H, (C1-C40)알킬, (C1-C40)헤테로알킬, (C1-C40)아실, (C2-C40)알케닐, (C2-C40)알키닐, 아릴(C1-C40)알킬, 아릴(C1-C40)아실, 치환된 (C1-C40)알킬, 치환된 (C1-C40)헤테로알킬, 치환된 (C1-C40)아실, 치환된 (C2-C40)알케닐, 치환된 (C2-C40)알키닐, 치환된 아릴(C1-C40)알킬, 치환된 아릴(C1-C40)아실, (C1-C40)알킬설포닐 또는 -C(NH)-NH2이며;
n은 각 경우에 독립적으로, 1, 2, 3, 4 또는 5이며;
m은 각 경우에 독립적으로, 1, 2, 3, 4, 5, 6 또는 7이며;
s는 각 경우에 독립적으로, 1, 2, 3, 4, 5, 6 또는 7이며;
t는 각 경우에 독립적으로, 1, 2, 3, 4, 5, 6 또는 7이며;
X1, X2, X3, X4 및 X5는 각각 각 경우에 독립적으로 H, F, Cl, Br, I, (C1 -10)알킬, 치환된 (C1 -10)알킬, (C2 -10)알케닐, 치환된 (C2 -10)알케닐, (C2 -10)알키닐, 치환된 (C2 -10)알키닐, 아릴, 치환된 아릴, OH, NH2, NO2 또는 CN이며;
단, 하기를 만족한다:
(I). R4가 (C1-C40)아실, 아릴(C1-C40)아실, 치환된 (C1-C40)아실, 치환된 아릴(C1-C40)아실, (C1-C40)알킬설포닐 또는 -C(NH)-NH2이면, R5는 H, (C1-C40)알킬, (C1-C40)헤테로알킬, (C2-C40)알케닐, (C2-C40)알키닐, 아릴(C1-C40)알킬, 치환된 (C1-C40)알킬, 치환된 (C1-C40)헤테로알킬, 치환된 (C2-C40)알케닐, 치환된 (C2-C40)알키닐, 또는 치환된 아릴(C1-C40)알킬이고;
(II). R2가 (C1-C30)아실, 아릴(C1-C30)아실, 치환된 (C1-C30)아실, 또는 치환된 아릴(C1-C30)아실이면, R3은 H, (C1-C30)알킬, (C1-C30)헤테로알킬, (C2-C30)알케닐, (C2-C30)알키닐, 아릴(C1-C30)알킬, 치환된 (C1-C30)알킬, 치환된 (C1-C30)헤테로알킬, 치환된 (C2-C30)알케닐, 치환된 (C2-C30)알키닐, 또는 치환된 아릴(C1-C30)알킬이고;
(III) B1 및 B2 둘다 아미노산 서열: Arg-(Lys)2-(Arg)2-Gln-(Arg)3, Tyr-Ala-Arg-Lys-Ala-(Arg)2-Gln-Ala-(Arg)2, Tyr-Ala-Arg-(Ala)2-(Arg)2-(Ala)2-(Arg)2, Tyr-Ala-(Arg)9, Tyr-(Ala)3-(Arg)7, Tyr-Ala-Arg-Ala-Pro-(Arg)2-Ala-(Arg)3 및 Tyr-Ala-Arg-Ala-Pro-(Arg)2-Pro-(Arg)2 중 하나 이상을 포함하지 않으며;
(IV) B1 및 B2 중 어느 하나 또는 둘다는 상기 화합물에 존재하여야 하며;
(V) A2가 Cys, D-Cys, hCys, D-hCys, Pen 또는 D-Pen이면, A9는 Cys, D-Cys, hCys, D-hCys, Pen 또는 D-Pen이고;
(VI) A2가 Asp 또는 Glu이면, A9는 Dab, Dap, Orn 또는 Lys이다.
본 발명의 제2 측면에서, 상기 화합물의 바람직한 그룹은 하기한 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
B1은 Arg-Lys-Gln-Lys-(Arg)5, Arg-(Lys)2-Arg-Gln-(Arg)4, Arg-(Lys)2-(Arg)3-Gln-(Arg)2, Arg-(Lys)2-(Arg)4-Gln-Arg, Arg-(Lys)2-(Arg)5-Gln, Arg-(Lys)2-Gln-(Arg)5, Arg-Gln-(Lys)2-(Arg)5, Arg-Gln-(Arg)7, Arg-Gln-(Arg)8, (Arg)2-Gln-(Arg)6, (Arg)2-Gln-(Arg)7, (Arg)3-Gln-(Arg)5, (Arg)3-Gln-(Arg)6, (Arg)4-Gln-(Arg)4, (Arg)4-Gln-(Arg)5, (Arg)5, (Arg)5-Gln-(Arg)3, (Arg)5-Gln-(Arg)4, (Arg)6, (Arg)6-Gln-(Arg)3, (Arg)7, (Arg)7-Gln-(Arg)2, (Arg)8, (Arg)8-Gln-Arg, (Arg)9, (Arg)9-Gln, (D-Arg)5, (D-Arg)6, (D-Arg)7, (D-Arg)8, (D-Arg)9, Gln-Arg-(Lys)2-(Arg)5, Gln-(Arg)8, Gln-(Arg)9, Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3, Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc이거나, 삭제되며;
B2는 β-Ala, β-Ala-Gly, β-Ala-Tyr, β-Ala-Tyr-Gly, (β-Ala)2, (β-Ala)2-Gly, (β-Ala)2-Tyr, (β-Ala)2-Tyr-Gly, Doc, Doc-Gly, Doc-Tyr, Doc-Tyr-Gly, (Doc)2, (Doc)2-Gly, (Doc)2-Tyr, (Doc)2-Tyr-Gly이거나, 삭제되며;
B3은 Arg-Lys-Gln-Lys-(Arg)5, Arg-Lys-(Arg)3-Gln-(Arg)3, Arg-(Lys)2-Arg-Gln-(Arg)4, Arg-(Lys)2-Gln-(Arg)5, Arg-(Lys)2-(Arg)2-Gln-(Arg)3, Arg-(Lys)2-(Arg)3-Gln-(Arg)2, Arg-(Lys)2-(Arg)4-Gln-Arg, Arg-(Lys)2-(Arg)5-Gln, Arg-Gln-(Lys)2-(Arg)5, Arg-Gln-(Arg)7, Arg-Gln-(Arg)8, (Arg)2-Lys-(Arg)2-Gln-(Arg)3, (Arg)2-Gln-(Arg)6, (Arg)2-Gln-(Arg)7, (Arg)3-Gln-(Arg)5, (Arg)3-Gln-(Arg)6, (Arg)4-Gln-(Arg)4, (Arg)4-Gln-(Arg)5, (Arg)5, (Arg)5-Gln-(Arg)3, (Arg)5-Gln-(Arg)4, (Arg)6, (Arg)6-Gln-(Arg)3, (Arg)7, (Arg)7-Gln-(Arg)2, (Arg)8, (Arg)8-Gln-Arg, (Arg)9, (Arg)9-Gln, (D-Arg)5, (D-Arg)6, (D-Arg)7, (D-Arg)8, (D-Arg)9, Gln-Arg-(Lys)2-(Arg)5, Gln-(Arg)8, Gln-(Arg)9이거나 또는 삭제된다.
본 발명의 제3 측면에서, 제2 측면에 따른 화합물의 바람직한 그룹은 하기한 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
A1은 A6c, Gaba, Nle, Met, Phe, D-Phe, D-2-Nal, hPhe, Chg, D-Chg, Cha, hCha, hPro, hLeu, Nip, β-hMet, Oic이거나, 삭제되며;
A3은 Gly, Glu, Ala, β-Ala, Gaba, Aib, D-Ala, D-Abu, D-Val, D-Leu, D-Ile, D-Met, D-Nle, D-Cha, D-Phe, D-Tyr, D-Trp, D-Tle이거나, 삭제되며;
A4는 His이며;
A5는 D-Phe, D-1-Nal, D-2-Nal, D-Trp, D-Bal, D-(X1,X2,X3,X4,X5)Phe 또는 D-(Et)Tyr이며;
A6은 Arg 또는 hArg이며;
A7은 Trp, 1-Nal, 2-Nal, Bal, Bip 또는 D-Trp이며;
A8은 Gly, A5c, A6c, Ala, β-Ala, Gaba, Apn, Ahx, Aha이거나, 삭제되며;
A9는 Cys, D-Cys, hCys, D-hCys, Pen, D-Pen 또는 Lys이며;
A10은 Pro, Thr이거나, 삭제되며;
A11은 Pro이거나, 삭제되며;
A12는 Lys 또는 Arg이거나, 삭제되며;
A13은 Asp이거나 또는 삭제된다.
본 발명의 제4 측면에서, 제3 측면에 따른 화합물의 바람직한 그룹은 하기한 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
R2 및 R3은 각각 독립적으로 H 또는 아실이다.
본 발명의 제5 측면에서, 제5 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Aib-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2.
본 발명의 제6 측면에서, 제5 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Aib-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2 ;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2.
본 발명의 제7 측면에서, 제4 측면에 따른 화합물의 바람직한 그룹은 하기한 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
B1은 Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3; Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc이거나, 삭제되며;
B2는 β-Ala; β-Ala-Gly; β-Ala-Tyr-Gly; (β-Ala)2; (β-Ala)2-Gly; (β-Ala)2-Tyr-Gly; Doc; Doc-Gly; Doc-Tyr-Gly; (Doc)2; (Doc)2-Gly; (Doc)2-Tyr-Gly이거나, 삭제되며; 및
B3은 Arg-Lys-Gln-Lys-(Arg)5; Arg-Lys-(Arg)3-Gln-(Arg)3; Arg-(Lys)2-Gln-(Arg)5; Arg-(Lys)2-Arg-Gln-(Arg)4; Arg-(Lys)2-(Arg)2-Gln-(Arg)3; Arg-(Lys)2-(Arg)3-Gln-(Arg)2; Arg-(Lys)2-(Arg)4-Gln-Arg; Arg-(Lys)2-(Arg)5-Gln; (Arg)2-Lys-(Arg)2-Gln-(Arg)3; Arg-Gln-(Lys)2-(Arg)5; (Arg)5-Gln-(Arg)3; (Arg)5-Gln-(Arg)4; (Arg)6-Gln-(Arg)3이거나 또는 삭제된다.
본 발명의 제8 측면에서, 제7 측면에 따른 화합물의 바람직한 그룹은 하기한 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
B2는 β-Ala; β-Ala-Gly; β-Ala-Tyr-Gly; Doc-Tyr-Gly; (Doc)2-Tyr-Gly이거나 또는 삭제된다.
본 발명의 제9 측면에서, 제7 측면에 따른 화합물의 바람직한 그룹은 하기한 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
B3는 Arg-Lys-(Arg)3-Gln-(Arg)3; Arg-(Lys)2-Gln-(Arg)5; Arg-(Lys)2-Arg-Gln-(Arg)4; Arg-(Lys)2-(Arg)2-Gln-(Arg)3; Arg-(Lys)2-(Arg)3-Gln-(Arg)2; Arg-(Lys)2-(Arg)4-Gln-Arg; Arg-(Lys)2-(Arg)5-Gln; (Arg)2-Lys-(Arg)2-Gln-(Arg)3; Arg-Gln-(Lys)2-(Arg)5; (Arg)5-Gln-(Arg)3; (Arg)5-Gln-(Arg)4; (Arg)6-Gln-(Arg)3이거나 또는 삭제된다.
본 발명의 제10 측면에서, 제7 측면에 따른 상기 화합물의 바람직한 그룹은 하기한 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
A1 = Nle 또는 삭제되며;
A2 = Cys이며;
A3 = Glu 또는 D-Ala이며;
A4 = His이며;
A5 = D-Phe 또는 D-2-Nal이며;
A6 = Arg이며;
A7 = Trp, 1-Nal, 2-Nal 또는 Bal이며;
A8 = Gly 또는 Ala이며;
A9 = Cys이며;
A10 = Pro이거나, 삭제되며;
A12 = Lys, Arg 또는 삭제됨.
본 발명의 제11 측면에서, 제10 측면에 따른 화합물의 바람직한 그룹은 하기한 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
A3 = Glu;
A5 = D-2-Nal.
본 발명의 제12 측면에서, 제10 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Aib-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2; 또는
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2.
본 발명의 제13 측면에서, 제11 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Aib-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp--β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2; 또는
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2.
본 발명의 제14 측면에서, 제13 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2; 또는
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2.
본 발명의 제15 측면에서, 제14 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2.
본 발명의 제16 측면에서, 제14 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2.
본 발명의 제17 측면에서, 제14 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2.
본 발명의 제18 측면에서, 제14 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2.
본 발명의 제19 측면에서, 제17 측면에 따른 화합물의 바람직한 그룹은 하기 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
A1 = Nle, Phe, D-Phe, hPhe, Chg, D-Chg, hChg, Cha 또는 hCha이고;
A2 = Cys 또는 Asp이고;
A3 = D-Ala, D-Leu, D-Cha 또는 삭제되고;
A5 = D-Phe 또는 D-(Et)-Tyr이고;
A7 = Trp, Bal 또는 D-Trp이고;
A8 = Ala, β-Ala, Gaba, Apn, Ahx 또는 삭제되고;
A9 = Cys, D-Cys, Pen 또는 Lys이고;
A10 = Thr 또는 삭제되고;
A11 = 삭제되고;
A12 = 삭제되고;
A13 = 삭제되고;
단, A3 또는 A8 중 어느 하나는 삭제되나 둘다 삭제되진 않는다.
본 발명의 제20 측면에서, 제19 측면에 따른 화합물의 바람직한 그룹은 하기 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
A1 = Nle;
A2 = Cys이며;
A3 = D-Ala이며;
A5 = D-Phe;
A7 = Trp;
A8 = 삭제되며;
A9 = Cys.
본 발명의 제21 측면에서, 제19 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2; 또는
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2.
본 발명의 제22 측면에서, 제21 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2; 또는
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2.
본 발명의 제23 측면에서, 제17 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2.
본 발명의 제24 측면에서, 제17 측면에 따른 화합물의 바람직한 그룹은 하기 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
A1 = Nle;
A2 = Asp;
A3 = 삭제;
A5 = D-Phe 또는 D-2-Nal이며;
A6 = Arg이며;
A7 = Trp;
A8 = 삭제;
A9 = Lys이며;
A10 = 삭제;
A11 = 삭제;
A12 = 삭제;
A13 = 삭제.
본 발명의 제25 측면에서, 제24 측면에 따른 화합물의 바람직한 그룹은 하기 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
B1 = Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3; Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc 또는 삭제되며;
B3 = Arg-(Lys)2-(Arg)2-Gln-(Arg)3; (Arg)5-Gln-(Arg)3; (Arg)5-Gln-(Arg)4; 또는 삭제된다.
본 발명의 제26 측면에서, 제25 측면에 따른 화합물의 바람직한 그룹은 하기 기를 갖는 화합물 또는 약제학적으로 허용가능한 그의 염이다:
A5 = D-2-Nal.
본 발명의 제27 측면에서, 제24 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2; 또는
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2.
본 발명의 제28 측면에서, 제26 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
H-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2; 또는
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2.
본 발명의 제29 측면은 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염에 관한 것이다:
식 (II):
Ac-c(Cys-Glu-His-A1-Arg-A2-A3-Cys)-(Pro)2-Lys-Asp-NH2
상기에서,
A1은 D-이성체의 X-Phe 또는 2-Nal이고 상기 X는 할로겐이고;
A2는 Bal, 1-Nal, 2-Nal, 또는 Trp이고; 및
A3은 Aib, Ala, β-Ala 또는 Gly이다.
본 발명의 제30 측면에서, 제29 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-4-Br-Phe-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-NH2 ;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-β-Ala-Cys)-(Pro)2-Lys-Asp-NH2; 또는
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Aib-Cys)-(Pro)2-Lys-Asp-NH2.
본 발명의 제31 측면에서, 제30 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-NH2.
본 발명의 제32 측면에서, 제30 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-NH2.
본 발명의 제33 측면에서, 제30 측면에 따른 화합물의 바람직한 그룹은 하기 화합물 또는 약제학적으로 허용가능한 그의 염이다:
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-NH2.
더욱 바람직한 식 (I) 또는 식 (II)의 화합물은 본 발명의 실시예에서 구체적으로 기재된 각각의 화합물 또는 약제학적으로 허용가능한 그의 염이다.
다른 측면에 있어서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염, 및 약제학적으로 허용가능한 담체 또는 희석제를 포함하는 약학 조성물을 제공한다.
다른 측면에 있어서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 상기 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 약학 조성물을 제공한다.
다른 측면에 있어서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 상기 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-1 수용체, 인간 멜라노코르틴-3 수용체 및 인간 멜라노코르틴-5 수용체에 비하여 15배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진, 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 약학 조성물을 제공한다.
또다른 측면으로, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 상기 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비해 17배 이상 또는 90배 이상 높고 인간 멜라노코르틴-5 수용체에 비해 200배 이상 또는 3000배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진, 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 약학 조성물을 제공한다.
다른 측면으로, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 일반 염증, 염증성 장 질환, 뇌 염증, 패혈증 및 패혈증 쇼크와 같은 급성 또는 만성 염증 질환 또는 의학적 상태를 치료하는데 유용한 약학 조성물을 제공한다.
다른 측면으로, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 류마티스 관절염, 통풍성 관절염 및 다발성 경화증과 같은 자가면역성 질환 또는 의학적 상태를 치료하는데 유용한 약학 조성물을 제공한다.
다른 측면으로, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 비만, 섭식 장애 및 프레더 윌리 증후군과 같은 체중 증가를 수반하는 대사 질환 또는 의학적 상태를 치료하는데 유용한 약학 조성물을 제공한다. 또 다른 측면에서, 상기 치료되는 질환 또는 의학적 상태는 비만이다. 또다른 측면으로, 상기 치료되는 질환 또는 의학적 상태는 섭식 장애이다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 음식물 섭취 감소, 체중 감소 또는 이의 조합에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 체중 감소없이 음식물 섭취를 감소시키는데 유용한 약학 조성물을 제공한다. 또다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 체중을 증가시키면서 음식물 섭취를 감소시키는데 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 식욕 부진, 다식증, AIDS성 소모증, 악액질, 암 악액질 및 허약 노인의 쇠약증과 같은 체중 감소를 수반하는 대사 질환 또는 의학적 상태 치료에 유용한 약학 조성물을 제공한다. 다른 측면으로, 상기 치료되는 질환 또는 상태는 식욕 부진이다. 다른 측면으로, 상기 치료되는 질환 또는 상태는 AIDS성 소모증 또는 허약 노인의 쇠약증이다. 다른 측면으로, 상기 치료되는 질환은 악액질 또는 암 악액질이다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 음식물 섭취 증가, 체중 증가 또는 이의 조합에 유용한 약학 조성물을 제공한다. 바람직한 예로, 본 발명은 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 상기 화합물이 하기 화합물 또는 약제학적으로 허용가능한 그의 염인, 약학 조성물을 제공한다: Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2; Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2; Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2; 또는 Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 피부 암 및 암 악액질과 같은 신생물 질환 또는 의학적 상태 치료에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 자궁내막증, 자궁 출혈, 성 기능 장애, 발기 부전 및 여성의 성 반응 감소와 같은 생식기 또는 성 관련 의학적 상태 치료에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 장기 이식 거부 반응, 허혈증 및 재관류 손상, 상처 및 척수 손상, 및 화학요법, 방사선요법, 일시 고정화, 영구 고정화 및 투석으로 이루어진 군으로부터 선택되는 의학 시술로 인한 체중 감소와 같은 유기체의 치료 또는 상해가 원인인 질환 또는 의학적 상태 치료에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 출혈성 쇼크, 심장 쇼크, 저혈량성 쇼크, 심혈관 장애 및 심장 악액질과 같은 심혈관 질환 또는 의학적 상태 치료에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 급성 호흡 곤란 증후군, 폐 섬유증, 만성 폐색성 폐 질환 및 천식과 같은 폐 질환 또는 의학적 상태 치료에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 면역 관용 강화 및 알러지 치료에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 건선, 피부 색소 형성 감소증, 여드름 및 켈로이드 형성과 같은 피부 질환 또는 의학적 상태 치료에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 불안, 우울증, 기억 장애 및 신경성 통증과 같은 행동 체계, 중추 신경계 또는 신경 질환 또는 의학적 상태 치료에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 신장 악액질 및 나트륨뇨증과 같은 신장 질환 또는 의학적 상태 치료에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 난소 무게, 태반 발생, 프로락틴 분비, FSH 분비, 자궁내 태아 성장, 출산, 정자 형성, 티록신 분비, 알도스테론 합성과 분비, 체온, 혈압, 심장 박동수, 혈관 긴장도, 뇌혈류, 혈당 수치, 피지 분비, 페로몬 분비, 동기 부여, 학습 및 행동, 통증 인지, 신경 보호 및 신경 성장 조절에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 골 대사, 골 형성 및 골 발생 조절에 유용한 약학 조성물을 제공한다.
다른 측면에서, 본 발명은, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 유효량으로, 약제학적으로 허용가능한 담체 또는 희석제와 함께 포함하며, 알코올 섭취 저해, 알코올 섭취 감소, 알코올 중독 치료 또는 알코올 남용 치료에 유용한 약학 조성물을 제공한다. 다른 측면에서, 알코올 섭취 저해, 알코올 섭취 감소, 알코올 중독 치료 또는 알코올 남용 치료에 유용한 조성물의 화합물은, 선택적인 멜라노코르틴-4 수용체 작용제이다. 또다른 측면으로, 알코올 섭취 저해에 유용한 조성물의 화합물은, 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-1 수용체, 인간 멜라노코르틴-3 수용체 및 인간 멜라노코르틴-5 수용체에 비하여 15배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진, 선택적인 멜라노코르틴-4 수용체 작용제 또는 약학적으로 허용가능한 그의 염이다. 또다른 측면에서, 알코올 섭취 저해에 유용한 조성물의 화합물은, 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비해 17배 이상 또는 90배 이상 높거나, 또는 인간 멜라노코르틴-5 수용체에 비해 200배 이상 또는 3000배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진, 선택적인 멜라노코르틴-4 수용체 작용제 또는 약제학적으로 허용가능한 그의 염이다.
다른 측면에서, 본 발명은, 치료가 필요한 개체에서 알코올 섭취 저해, 알코올 섭취 감소, 알코올 중독 치료 또는 알코올 남용 치료에 유용한 약제 제조에 있어, 치료학적 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염의 용도를 제공한다.
또다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 필요한 개체에 투여하는 단계를 포함하는, 상기 개체에서 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어내는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 필요한 개체에 투여하는 단계를 포함하며, 상기 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인, 상기 개체에서 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어내는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 필요한 개체에 투여하는 단계를 포함하며, 상기 화합물은 EC50에 의해 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-1 수용체, 인간 멜라노코르틴-3 수용체 및 인간 멜라노코르틴-5 수용체에 비하여 15배 이상 높은 것으로 특정화된 기능적 활성을 가진 선택적인 멜라노코르틴-4 수용체 작용제인, 상기 개체에서 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어내는 방법을 제공한다.
또다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 필요한 개체에 투여하는 단계를 포함하며, 상기 화합물은 EC50에 의해 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비해 17배 이상 또는 90배 이상 높고 인간 멜라노코르틴-5 수용체에 비해 200배 이상 또는 3000배 이상 높은 것으로 특정화된 기능적 활성을 가진 선택적인 멜라노코르틴-4 수용체 작용제인, 상기 개체에서 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어내는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 일반 염증, 염증성 장 질환, 뇌 염증, 패혈증 및 패혈증 쇼크와 같은 급성 또는 만성 염증 질환 또는 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 류마티스 관절염, 통풍성 관절염 및 다발성 경화증과 같은 자가면역성 질환 또는 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 비만, 섭식 장애 및 프레더 윌리 증후군과 같은 체중 증가를 수반하는 대사 질환 또는 의학적 상태를 치료하는 방법을 제공한다. 상기 방법의 다른 측면에서, 치료되는 질환 또는 상태는 비만이다. 상기 방법의 또다른 측면에서, 치료되는 질환 또는 상태는 섭식 장애이다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 음식물 섭취를 감소시키는 방법, 체중을 감소시키는 방법, 또는 음식물 섭취와 체중을 감소시키는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 체중 감소없이 음식물 섭취를 감소시키는 방법을 제공한다. 또다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 체중을 증가시키면서 음식물 섭취를 감소시키는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 음식물 섭취를 증가시키는 방법, 체중을 증가시키는 방법, 또는 음식물 섭취와 체중을 증가시키는 방법을 제공한다. 상기 방법의 바람직한 예에서, 음식물 섭취 증가, 체중 증가 또는 이의 조합에 이용가능한 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염은, Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2; Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2; Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2; Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는 약제학적으로 허용가능한 그의 염이다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 식욕 부진, 다식증, AIDS성 소모증, 악액질, 암 악액질 및 허약 노인의 쇠약증과 같은 체중 감소를 수반하는 대사 질환 또는 의학적 상태를 치료하는 방법을 제공한다. 다른 측면으로, 상기 방법은 식욕 부진 치료에 사용된다. 다른 측면으로, 상기 방법은 다식증 치료에 사용된다. 다른 측면으로, 상기 방법은 AIDS성 소모증 또는 허약 노인의 쇠약증 치료에 사용된다. 다른 측면으로, 상기 방법은 악액질 또는 암 악액질 치료에 사용된다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 피부 암 및 암 악액질과 같은 신생물 질환 또는 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 자궁내막증, 자궁 출혈, 성 기능 장애, 발기 부전 및 여성의 성 반응 감소와 같은 생식기 또는 성 관련 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 장기 이식 거부 반응, 허혈증 및 재관류 손상, 상처 및 척수 손상, 및 화학요법, 방사선요법, 일시 고정화, 영구 고정화 및 투석으로 이루어진 군으로부터 선택되는 의학 시술로 인한 체중 감소와 같은 유기체의 치료 또는 상해가 원인인 질환 또는 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 출혈성 쇼크, 심장 쇼크, 저혈량성 쇼크, 심혈관 장애 및 심장 악액질과 같은 심혈관 질환 또는 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 급성 호흡 곤란 증후군, 폐 섬유증, 만성 폐색성 폐 질환 및 천식과 같은 폐 질환 또는 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 면역 관용을 강화하는 방법 또는 알러지를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 건선, 피부 색소 형성 감소증, 여드름 및 켈로이드 형성과 같은 피부 질환 또는 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 불안, 우울증, 기억 장애 및 신경성 통증과 같은 행동 체계, 중추 신경계 또는 신경 질환 또는 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 신장 악액질 및 나트륨뇨증과 같은 신장 질환 또는 의학적 상태를 치료하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 난소 무게, 태반 발생, 프로락틴 분비, FSH 분비, 자궁내 태아 성장, 출산, 정자 형성, 티록신 분비, 알도스테론 합성과 분비, 체온, 혈압, 심장 박동수, 혈관 긴장도, 뇌혈류, 혈당 수치, 피지 분비, 페로몬 분비, 동기 부여, 학습 및 행동, 통증 인지, 신경 보호 및 신경 성장과 같은 정상화 및 항상성 활성을 조절하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 골 대사, 골 형성 및 골 발생과 같은 정상 또는 항상성 활성을 조절하는 방법을 제공한다.
다른 측면에서, 본 발명은, 유효량의, 식 (I) 또는 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염을 투여하는 단계에 의해 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 이끌어냄으로써, 알코올 섭취를 저해하는 방법, 알코올 섭취를 감소시키는 방법, 알코올 중독을 치료하는 방법 또는 알코올 남용을 치료하는 방법을 제공한다. 상기 방법의 다른 측면에서, 상기 화합물은 선택적 멜라노코르틴-4 수용체 작용제이다. 상기 방법의 또다른 측면에서, 알코올 섭취 저해에 사용가능한 조성물의 화합물은, 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-1 수용체, 인간 멜라노코르틴-3 수용체 및 인간 멜라노코르틴-5 수용체에 비하여 15배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진, 선택적인 멜라노코르틴-4 수용체 작용제 또는 약학적으로 허용가능한 그의 염이다. 상기 방법의 또다른 측면에서, 알코올 섭취 저해에 유용한 조성물의 화합물은, 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비해 17배 이상 또는 90배 이상 높거나, 또는 인간 멜라노코르틴-5 수용체에 비해 200배 이상 또는 3000배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진, 선택적인 멜라노코르틴-4 수용체 작용제 또는 약제학적으로 허용가능한 그의 염이다.
다른 측면으로, 본 발명은, 일반 염증, 염증성 장 질환, 뇌 염증, 패혈증 및 패혈증 쇼크와 같은 급성 또는 만성 염증 질환; 류마티스 관절염, 통풍성 관절염 및 다발성 경화증과 같은 자가면역성 질환; 비만, 섭식 장애 및 프레더 윌리 증후군과 같은 체중 증가를 수반하는 대사 질환 또는 의학적 장애; 식욕 부진, 다식증, AIDS성 소모증, 악액질, 암 악액질 및 허약 노인의 쇠약증과 같은 체중 감소를 수반하는 대사 질환 또는 의학적 장애; 당뇨병, 당뇨병 관련 증상 및 망막증과 같은 당뇨병 합병증; 피부암 및 전립선 암과 같은 신생물 증식; 자궁내막증, 자궁 출혈, 성 기능 장애, 발기 부전 및 여성의 성 반응 감소와 같은 생식기 또는 성 관련 의학적 상태; 장기 이식 거부 반응, 허혈증 및 재관류 손상, 상처 및 척수 손상과 같은 유기체의 치료 또는 상해가 원인인 질환 또는 상태 뿐만 아니라, 화학요법, 방사선요법, 일시 고정화, 영구 고정화 또는 투석으로 야기된 체중 감소; 출혈성 쇼크, 심장 쇼크, 저혈량성 쇼크, 심혈관 장애 및 심장 악액질과 같은 심혈관 질환 또는 상태; 급성 호흡 곤란 증후군, 폐 섬유증, 만성 폐색성 폐 질환 및 천식과 같은 폐 질환 또는 상태; 특정 알러지나 장기 이식 거부 반응과 관련된 면역 관용 강화 및 면역계 공격에 대항하기 위해; 건선, 피부 색소 형성 감소증, 여드름 및 켈로이드 형성과 같은 피부 질환 또는 상태; 불안, 우울증, 기억 장애 및 신경성 통증과 같은 행동 체계, 중추 신경계 또는 신경 장애; 및 신장 악액질 및 나트륨뇨증과 같은 신장 상태 또는 질환으로 이루어진 군으로부터 선택되는 질환 및/또는 의학적 상태 치료에 이용가능한 약제 제조에 있어서의, 식 (I) 또는 식 (II)의 화합물에 따른, 치료학적 유효량의, 멜라노코르틴-4 수용체 작용제 또는 길항제 화합물, 또는 약제학적으로 허용가능한 그의 염의, 용도를 제공한다.
다른 측면에서, 본 발명은 난소 무게, 태반 발생, 프로락틴 분비, FSH 분비, 자궁내 태아 성장, 출산, 정자 형성, 티록신 분비, 알도스테론 합성과 분비, 체온, 혈압, 심장 박동수, 혈관 긴장도, 뇌혈류, 혈당 수치, 피지 분비, 페로몬 분비, 동기 부여, 학습 및 행동, 통증 인지, 신경 보호, 신경 성장, 골 대사, 골 형성 및 골 발생과 같은 정상화 및 항상성 활성 조절에 유용한 약제 제조에 있어서의, 식 (I) 또는 식 (II)의 화합물에 따른, 치료학적 유효량의, 멜라노코르틴-4 수용체 작용제 또는 길항제 화합물, 또는 약제학적으로 허용가능한 그의 염의, 용도를 제공한다.
멜라노코르틴 수용체를 이용하는 정상적인 생리과정과 병적생리과정 둘다를 대처하는 치료적 개입 역시 본 발명에 포함되는 것으로 인정될 것이다.
본 발명의 추가적인 목적, 이점 및 특징들은 첨부된 도면과 함께 하기 상세한 설명 및 첨부된 청구항으로부터 명확해질 것이다.
식 (I) 또는 (II)의 화합물은 하나 이상의 멜라노코르틴 수용체(MC1-R, MC2-R, MC3-R, MC4-R 및 MC5-R)에 대한 리간드이므로, 이를 선택하여 하기 개시된 시험관내 분석을 통해 리간드로서 작용하는 이들의 능력에 대해 테스트하였다.
발명의 상세한 설명
펩티드를 특정하기 위해 사용된 명칭은 전형적으로 당업계에서 사용되는 것으로, N-말단의 아미노기는 좌측이며, C-말단의 카르복시기는 우측이다. 아미노산이 이성질체인 경우, 명확하게 나타나있지 않다면 표시된 아미노산은 L 형이다. 명확하지 않다면, 본원에 사용된 모든 기술 용어 및 과학 용어는 본 발명이 속하는 기술 분야의 당업자가 통상적으로 이해하는 바와 동일한 의미를 가진다. 또한, 본 명세서에 언급된 모든 공개 문헌, 특허 출원, 특허 및 그외 참조문헌들은 원용에 의해 본 명세서에 포함된다.
명칭 및 약어
기호 의미
Abu α-아미노부티르산
Ac 아실기
Acc 1-아미노-1-사이클로(C3-C9)알킬 카르복시산
A3c 1-아미노-1-사이클로프로판카르복시산
A4c 1-아미노-1-사이클로부탄카르복시산
A5c 1-아미노-1-사이클로펜탄카르복시산
A6c 1-아미노-1-사이클로헥산카르복시산
Aha 7-아미노펩탄산
Ahx 6-아미노헥산산
Aib α-아미노이소부티르산
Ala 또는 A 아민
β-Ala β-아민
Apn 5-아미노펜탄산 (HN-(CH2)4-C(O)
Arg 또는 R 아르기닌
hArg 호모아르기닌
Asn 또는 N 아스파라긴
Asp 또는 D 아스파르트산
Bal 3-벤조티에닐알라닌
Bip 하기 구조로 표시되는 4,4'-바이페닐알라닌
Bpa 4-벤조일페닐알라닌
4-Br-Phe 4-브로모-페닐알라닌
Cha β-사이클로헥실알라닌
hCha 호모-사이클로헥실알라닌
Chg 사이클로헥실글리신
Cys 또는 C 시스테인
hCys 호모시스테인
Dab 2,4-디아미노부티르산
Dap 2,3-디아미노프로피온산
Dip β,β-디페닐알라닌
Doc 하기 구조로 표시되는 8-아미노-3,6-디옥사옥타노산
2-Fua β-(2-푸릴)-알라닌
Gaba 4-아미노부티르산
Gln 또는 Q 글루타민
Glu 또는 E 글루탐산
Gly 또는 G 글리신
His 또는 H 히스티딘
3-Hyp 트랜스-3-하이드록시-L-프롤린, 즉 (2S, 3S)-3-하이드록시피롤리딘-2-카르복시산
4-Hyp 4-하이드록시프롤린, 즉 (2S, 4R)-4-하이드록시피롤리딘-2-카르복시산
Ile 또는 I 이소루신
Leu 또는 L 루신
hLeu 호모루신
Lys 또는 K 라이신
Met 또는 M 메티오닌
β-hMet β-호모메티오닌
1-Nal β-(1-나프틸)알라닌
2-Nal β-(2-나프틸)알라닌
Nip 니펙코트산
Nle 노르루신
Oic 옥타하이드로인돌-2-카르복시산
Orn 오르니틴
2-Pal β-(2-피리디일)알라닌)
3-Pal β-(3-피리디일)알라닌)
4-Pal β-(4-피리디일)알라닌)
Pen 페니실아민
Phe 또는 F 페닐알라닌
hPhe 호모페닐알라닌
Pro 또는 P 프롤린
hPro 호모프롤린
Ser 또는 S 세린
Tle tert-루신
Taz β-(4-티아졸릴)알라닌
2-Thi β-(2-티아졸릴)알라닌
3-Thi β-(3-티아졸릴)알라닌
Thr 또는 T 트레오닌
Trp 또는 W 트립토판
Tyr 또는 Y 타이로신
D-(Et)Tyr 하기 구조로 표시되는 화합물
Val 또는 V 발린
본원에 사용된 그외 특정 약어는 다음과 같이 정의된다:
Boc: tert-부틸옥시카르보닐
Bzl: 벤질
DCM: 디클로로메탄
DIC: N, N-디이소프로필카르보디이미드
DIEA: 디이소프로필에틸아민
Dmab: 4-{N-(1-(4,4-디메틸-2,6-디옥소사이클로헥실리덴)-3-메틸부틸)-아미노}벤질
DMAP: 4-(디메틸아미노)피리딘
DMF: 디메틸포름아미드
DNP: 2,4-디니트로페닐
Fm: 플루오레닐메틸
Fmoc: 플루오레닐메틸옥시카르보닐
For: 포르밀
HBTU: 2-(1H-벤조트리아졸-1-일)-1,1,3,3-테트라메틸우로늄 헥사플루오로포스페이트
cHex: 사이클로헥실
HOAT: O-(7-아자벤조트리아졸-1-일)-1,1,3,3-테트라메틸우로늄 헥사플루오로포스페이트
HOBt: 1-하이드록시-벤조트리아졸
MBHA: 4-메틸벤즈하이드릴아민
Mmt: 4-메톡시트리틸
NMP: N-메틸피롤리돈
O-tBu: 옥시-tert-부틸
Pbf: 2,2,4,6,7-펜타메틸디하이드로벤조퓨란-5-설포닐
PyBroP: 브로모-트리스-피롤리디노-포스포늄 헥사플루오로포스페이트
tBu: tert-부틸
TIS: 트리이소프로필실란
TOS: 토실
Trt: 트리틸
TFA: 트리플루오로 아세트산
TFFH: 테트라메틸플루오로포름아미디늄 헥사플루오로포스페이트
Z: 벤질옥시카르보닐
언급되어 있지 않는 한, 본원에서 N-말단 아미노산을 제외하고는 아미노산의 모든 약어(예, Ala)는 구조 -NH-C(R)(R')-CO-를 유지하며, 여기에서 R 및 R'은 각각 독립적으로 수소 또는 아미노산의 측쇄(예, Ala의 경우, R = CH3 및 R' = H)이거나, R 및 R'은 연결되어 고리 시스템을 형성할 수 있다.
N-말단 아미노산은, 하기 구조를 유지한다:
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH2에서, "NH2"는 펩티드의 C-말단이 아미드화되었음을 나타낸다. Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys), 또는 대안적으로 Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-OH는, C-말단이 유리산임을 나타낸다.
"-c(Cys-Cys)-" 또는 "-사이클로(Cys-Cys)-"는 하기 구조를 나타낸다:
"-c(Cys-Pen)-" 또는 "-사이클로(Cys-Pen)-"은 하기 구조를 나타낸다:
"-c(Asp-Lys)-" 또는 "-사이클로(Asp-Lys)-"은 하기 구조를 나타낸다:
"아실"은 R"이 H, 알킬, 치환된 알킬, 헤테로알킬, 치환된 헤테로알킬, 알케닐, 치환된 알케닐, 아릴, 알킬아릴 또는 치환된 알킬아릴인, R"-C(O)-이다.
"알킬"은 복수의 탄소 원자가 존재하다면 단일 결합으로 연결되어 있는, 하나 이상의 탄소 원자를 포함하고 있는 탄화수소기이다. 알킬 탄화수소기는 직쇄일 수 있거나, 또는 하나 이상의 분지나 사이클기를 포함할 수도 있다.
"하이드록시알킬"은 탄화수소기에서 하나 이상의 수소 원자가 하이드록시메틸, 하이드록시에틸, 하이드록시프로필, 하이드록시부틸, 하이드록시펜틸, 하이드록시헥실 등과 같은 하나 이상의 하이드록시 라디칼로 치환된 알킬기이다.
"치환된 알킬"은 탄화수소기에서 하나 이상의 수소 원자가, 할로겐(즉, F, l, Br 및 I), -OH, -CN, -SH, NH2, -NHCH3, -NO2, 및 각 경우에 독립적으로 할로겐, -CF3, -OCH3, -OCF3 및 -(CH2)0-20-COOH로 이루어진 군으로부터 하나 이상의 치환기로 선택적으로 치환될 수 있는 -C1 -20 알킬로 이루어진 군으로부터 선택된 하나 이상의 치환기로 치환된, 알킬이다. 여러가지 예에서, 1, 2, 3 또는 4개의 치환기가 존재된다. -(CH2)0-20-COOH이 존재하면, 알킬 산이 생성된다. -(CH2)0-20-COOH를 포함하는 알킬 산 또는 -(CH2)0-20-COOH로 이루어진 알킬 산의 예로는, 2-노르보난 아세트산, tert-부티르산 및 3-사이클로펜틸 프로피오온산 등이 있으나, 이로 한정되지 않는다.
용어 "할로"는 F, Cl, Br 및 I를 나타낸다.
"헤테로알킬"은 탄화수소기에서 하나 이상의 탄소 원자가 아미노, 아미도, -O-, -S- 또는 카르보닐 중 하나 이상으로 치환된 알킬이다. 여러가지 예에서, 1 또는 2개의 헤테로원자가 존재된다.
"치환된 헤테로알킬"은 탄화수소기에서 하나 이상의 수소 원자가 할로겐(즉, F, l, Br 및 I), -OH, -CN, -SH, NH2, -NHCH3, -NO2, 및 각 경우에 독립적으로 할로겐, -CF3, -OCH3, -OCF3 및 -(CH2)0-20-COOH로 이루어진 군으로부터 하나 이상의 치환기로 선택적으로 치환될 수 있는 -C1 -20 알킬로 이루어진 군으로부터 선택된 하나 이상의 치환기로 치환된, 헤테로알킬이다. 여러가지 예에서, 1, 2, 3 또는 4개의 치환기가 존재된다.
"알케닐"은 하나 이상의 탄소-탄소 이중 결합이 존재하는 2개 이상의 탄소로 구성된 탄화수소기이다. 알케닐 탄화수소기는 직쇄이거나, 또는 하나 이상의 분지 또는 사이클기를 포함할 수도 있다.
"치환된 알케닐"은 하나 이상의 수소가 할로겐(즉, F, l, Br 및 I), -OH, -CN, -SH, NH2, -NHCH3, -NO2, 및 각 경우에 독립적으로 할로겐, -CF3, -OCH3, -OCF3 및 -(CH2)0-20-COOH로 이루어진 군으로부터 하나 이상의 치환기로 선택적으로 치환될 수 있는 -C1 -20 알킬로 이루어진 군으로부터 선택된 하나 이상의 치환기로 치환된, 알케닐이다. 여러가지 예에서, 1, 2, 3 또는 4개의 치환기가 존재된다.
"아릴"은 접합된 pi-전자계를 가진 1개 이상의 고리가 있으며, 최대 3개의 접합되거나 융합된 고리 시스템을 포함하는 선택적으로 치환된 방향족 기이다. 아릴은 카르보사이클 아릴, 헤테로사이클 아릴 및 바이아릴기를 포함한다. 바람직하기로는, 아릴은 5 또는 6원환이다. 헤테로사이클 아릴에 바람직한 원자는, 하나 이상의 황, 산소 및/또는 질소이다. 아릴의 예로는, 페닐, 1-나프틸, 2-나프틸, 인돌, 퀴놀린, 2-이미다졸 및 9-안트라센 등이 있으나, 이로 한정되지 않는다. 아릴 치환기는 -C1 -20 알킬, -C1 -20 알콕시, 할로겐(즉, F, Cl, Br 및 I), -OH, -CN, -SH, -NH2, -NO2, 및 할로겐, -CF3, -OCF3 또는 -(CH2)0-20-COOH로 치환된 -C1 -20 알킬로 이루어진 군으로부터 선택된다. 여러가지 예에서, 아릴은 0, 1, 2, 3 또는 4개의 치환기를 포함한다.
"알킬아릴"은 "아릴"이 연결된 "알킬"이다.
용어 "(C1-C12)탄화수소 모이어티"는 알킬, 알케닐 및 알키닐을 포함하며, 알케닐 및 알키닐의 경우에는 C2-C12이다.
본원에서, 용어 "정상화(normalizing) 기능"은 정상적인 신체 기능 또는 유기체의 항상성에 관여하는 것으로 볼 수 있는 유형의 기능을 의미한다. 이러한 기능으로는 티록신 분비, 알도스테론 합성과 분비, 체온, 혈압, 심장 박동율, 혈관 긴장도, 뇌 혈류, 혈당 수치 등에 작용하는 활성 및 기능이 있으나, 이로 한정되지 않는다.
본원에서, 특정 멜라노코르틴 수용체에 대해 선택적으로 것으로 간주되는 화합물은 임의의 다른 멜라노코르틴 수용체와 비교하여, 특정 멜라노코르틴 수용체에 대한 선택성이, 약 2배 이상, 약 5배 이상, 약 10배 이상, 약 15배 이상, 약 17배 이상, 약 90배 이상, 약 200배 이상, 약 3000배 이상, 약 10,000배 이상 또는 그 이상인 것으로 EC50에 의해 특정화된 기능적 활성을 가진 화합물이다. 예컨대, 본 발명의 선택적인 멜라노코르틴-4 수용체 작용제는, 인간 멜라노코르틴-1 수용체, 인간 멜라노코르틴-3 수용체 및 인간 멜라노코르틴-5 수용체에 비하여 인간 멜라노코르틴-4 수용체에 대해 약 15배 이상 선택적인 것으로, EC50에 의해 특정화된 기능적 활성을 가진다. 또한, 예로, 본 발명의 선택적인 멜라노코르틴-4 수용체 작용제는 인간 멜라노코르틴-3 수용체에 비하여 인간 멜라노코르틴-4 수용체에 대해 약 17배 이상 선택적인 것으로, EC50에 의해 특정화된 기능적 활성을 가진다.
합성
본 발명의 펩티드는 표준적인 고상 펩티드 합성에 의해 제조할 수 있다. 예로, Stewart, J.M., et al., Solid Phase Synthesis(Pierce Chemical Co., 2d ed. 1984)을 참조한다. 상기 일반식의 치환기 R2 및 R3을 당업계에 공지된 표준 방법에 의해 N-말단 아미노산의 유리 아민에 부착할 수 있다. 예로, 알킬기, 예, (C1-C30)알킬을 환원성 알킬화를 이용하여 부착할 수 있다. 하이드록시알킬기, 예컨대 (C1-C30)하이드록시알킬 또한 환원성 알킬화로 부착할 수 있으며, 유리 하이드록시기는 t-부틸 에스테르로 보호된다. 아실기, 예컨대 COE1을 유기 산, 예컨대 완료된 수지를 각각 3몰 당량의 유리 산 및 디이소프로필카르보디이미드와 메틸렌 클로라이드중에서 한시간 동안 혼합하여, E1COOH을 N-말단 아미노산의 유리 아민에 커플링함으로써 부착할 수 있다. 유리 산에 유리 하이드록시기, 예컨대 p-하이드록시페닐프로피온산을 포함하고 있다면, 커플링은 부가적인 3몰 당량의 HOBt를 사용하여 수행하여야 한다.
R1이 -NH2이면, 링크 아미드 MBHA 수지가 커플링된 Fmoc-아미노산으로 펩티드의 합성을 개시한다. R1이 -OH이면, 펩티드 합성은 Wang 수지가 커플링된 Fmoc-아미노산으로 펩티드의 합성을 개시한다.
본 발명의 A6c 및/또는 Aib가 포함된 펩티드의 합성시에는, 커플링 시간은 이들 잔기와 이들 잔기 바로 다음에 잔기에 대해서는 2시간이다.
도 1. 선택 화합물을 8 μmole/Kg으로 투여한 후 4시간 동안 랫에서의 음식물 누적 섭취량.
도 2A. 화합물 B 및 화합물 E를 다양한 농도를 투여한 후 랫에서의 비히클 섭취량 대비 음식물의 섭취량의 누적 평균 변화.
도 2B. 화합물 B 및 화합물 E를 다양한 농도를 투여한 후 랫에서의 비히클 섭취량 대비 체중의 누적 평균 변화.
도 3A. 화합물 B를 다양한 농도를 투여한 후 랫에서의 비히클 섭취량 대비 음식물의 섭취량의 누적 평균 변화.
도 3B. 화합물 B를 다양한 농도를 투여한 후 랫에서의 비히클 섭취량 대비 체중의 누적 평균 변화.
도 4A. 화합물 F를 다양한 농도를 투여한 후 랫에서의 비히클 섭취량 대비 음식물의 섭취량의 누적 평균 변화.
도 4B. 화합물 F를 다양한 농도를 투여한 후 랫에서의 비히클 섭취량 대비 체중의 누적 평균 변화.
하기 실시예들은 본 발명의 펩티드를 제조하는 당업자들에게 잘 알려져 있는 합성 방법을 개시한다. 다른 방법들 역시 당업자들에게 공지되어 있다. 실시예들은 예시하기 위한 것일 뿐 어떠한 방식으로도 본 발명의 범위를 한정하는 것으로 의미되지 않는다.
실시예
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Ac
-c(
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표제 펩티드는 Applied Biosystems®(Foster City, CA) 모델 433A 펩티드 합성기로 합성하였다. 0.66 mmol/g의 치환을 갖는 4-(2',4'-디메톡시페닐-Fmoc-아미노메틸)-페녹시아세트아미도-노르루실-MBHA 수지(Rink Amide MBHA® resin, Novabiochem®, San Diego, CA)를 사용하였다. 하기 Fmoc 아미노산(AnaSpec®, San Jose, CA)을 합성에 사용하였다: Fmoc-Arg(Pbf)-OH, Fmoc-Cys(Trt)-OH, Fmoc-D-2-Nal-OH, Fmoc-Bal-OH, Fmoc-Pro-OH, Fmoc-Lys(Boc)-OH, Fmoc-Ala-OH, Fmoc-Glu(O-tBu)-OH, Fmoc-His(Trt)-OH, 및 Fmoc-Asp(O-tBu)-OH. Fmoc-Bal-OH는 Peptech®(Burlington, MA)로부터 구입하였다. 합성은 1.00 mmol 스케일로 수행하였다. N-메틸피롤리돈(NMP) 중의 20% 피페리딘으로 30분간 처리하여, Fmoc 기를 제거하였다. 각 커플링 단계에서, Fmoc 아미노산(1 mmol)을 먼저 DMF 중의 HBTU(0.9 mmol) 및 HOBT(0.9 mmol)로 활성화시킨 다음, 수지를 첨가하였다. ABI 433A 펩티드 합성기를 하기 반응 사이클을 수행하도록 프로그램을 설정하였다: (1) NMP로 세척, (2) 30분간 NMP 중의 20% 피페리딘을 사용하여 Fmoc 보호기 제거, (3) NMP로 세정, (4) 1시간 동안 미리 활성화시킨 Fmoc 아미노산과 커플링. 합성기에서 마지막 사이클을 수행하는 동안, Fmoc는 탈차단되었고, 펩티드는 아세트 안하이드라이드 및 디이소프로필에틸아민으로 캡핑되었다.
세척 및 건조한 다음, TFA(38 mL), H2O(3.4 mL) 및 트리이소프로필실 란(TIS)(3.2 mL) 혼합물을 3시간 동안 이용하여 수지에서 펩티드를 잘랐다. 수지는 여과 제거하고, 여과물을 에테르 70 mL에 부었다. 형성된 침전물은 여과 제거하고, 에테르로 완전히 세척하였다. 상기 펠렛 조산물을 아세토니트릴 30 mL에 용해하고 5% 아세트산 300 mL로 희석하여, 펩티드를 환화하였다. MeOH 중의 2N KI를 용액 색이 변화지 않을 때까지 점적하였다. 반응 혼합물은 열수조에서 열처리하고 2시간 동안 교반하였다. 여기에 10% NaSSO3 수용액을 첨가하여 반응을 중지시켰다.
조산물은 Luna® 컬럼(2.1 x 25 cm C18(2); Phenomenex®, Torrance, CA.)이 장착된 역상 조제용 HPLC 시스템으로 정제하였다. 선형 농도 구배 95% A 및 5% B -> 55% A 및 45% B로 90분간 컬럼에서 용출시켰으며, 상기에서 A는 수중의 0.1% TFA이고, B는 아세토니트릴 중의 0.1% TFA이다. 분석용 HPLC로 분획을 체크하였다. 순수한 산물이 함유된 분획을 모아 동결건조로 건조하였다. 화합물의 순도는 99%였다. 수율은 17%였다. 전자-분무 이온화 질량 측정기(ESI-MS)를 이용한 분석시, 분자량은 1594.4이었다(분자량 계산치인 1594.9와 일치됨).
실시예
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Ac
-c(
Cys
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His
-D-2-
Nal
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Nal
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Pro
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Gln
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NH
2
표제 펩티드는 Applied Biosystems®(Foster City, CA) 모델 433A 펩티드 합성기로 합성하였다. 0.66 mmol/g의 치환을 갖는 4-(2',4'-디메톡시페닐-Fmoc-아미노메틸)-페녹시아세트아미도-노르루실-MBHA 수지(Rink Amide MBHA® resin, Novabiochem®, San Diego, CA)를 사용하였다. 하기 Fmoc 아미노산(AnaSpec®, San Jose, CA)을 합성에 사용하였다: Fmoc-Arg(Pbf)-OH, Fmoc-β-Ala-OH, Fmoc-Cys(Trt)-OH, Fmoc-Pro-OH, Fmoc-Lys(Boc)-OH, Fmoc-Ala-OH, Fmoc-Glu(O-tBu)-OH, Fmoc-His(Trt)-OH, Fmoc-Tyr(O-tBu)-OH, Fmoc-Gly-OH, Fmoc-Gln(Trt)-OH, 및 Fmoc-Asp(O-tBu)-OH. Fmoc-D-2-Nal-OH는 Peptech®(Burlington, MA)에서 구입하였다. Fmoc-2-Nal-OH는 Peptides International(St. Louis, MO)에서 구입하였다. 합성은 0.3 mmol 스케일로 수행하였다. N-메틸피롤리돈(NMP) 중의 20% 피페리딘으로 30분간 처리하여, Fmoc 기를 제거하였다. 각 커플링 단계에서, Fmoc 아미노산(1 mmol)을 먼저 DMF 중의 HBTU(0.9 mmol) 및 HOBT(0.9 mmol)로 활성화시킨 다음, 수지를 첨가하였다. ABI 433A 펩티드 합성기를 하기 반응 사이클을 수행하도록 프로그램을 설정하였다: (1) NMP로 세척, (2) 30분간 NMP 중의 20% 피페리딘을 사용하여 Fmoc 보호기 제거, (3) NMP로 세정, (4) 각 커플링 단계마다 1시간씩 미리 활성화시킨 Fmoc 아미노산과 2중 커플링. 합성기에서 마지막 사이클을 수행하는 동안, Fmoc는 탈차단되었고, 펩티드는 아세트 안하이드라이드 및 디이소프로필에틸아민으로 캡핑되었다.
세척 및 건조한 다음, TFA(17.5 mL), H2O(0.6 mL), DL-디티오트레이톨(36 mg) 및 트리이소프로필실란(TIS)(1.0 mL) 혼합물을 6시간 동안 이용하여 수지에서 펩티드를 잘랐다. 수지는 여과 제거하고, 여과물을 에테르 70 mL에 부었다. 형성된 침전물은 여과 제거하고, 에테르로 완전히 세척하였다. 상기 펠렛 조산물을 아 세토니트릴 30 mL에 용해하고 5% 아세트산 150 mL로 희석하여, 펩티드를 환화하였다. MeOH 중의 2N KI를 용액 색이 변화지 않을 때까지 점적하였다. 반응 혼합물은 열수조에서 열처리하고 2시간 동안 교반하였다. 여기에 10% NaSSO3 수용액을 첨가하여 반응을 중지시켰다.
조산물은 Luna® 컬럼(2.1 x 25 cm C18(2); Phenomenex®, Torrance, CA.)을 이용한 역상 조제용 HPLC 시스템으로 정제하였다. 선형 농도 구배 95% A 및 5% B -> 55% A 및 25% B로 80분간 컬럼에서 용출시켰으며, 상기에서 A는 수중의 0.1% TFA이고, B는 아세토니트릴 중의 0.1% TFA이다. 분석용 HPLC로 분획을 체크하였다. 순수한 산물이 함유된 분획을 모아 동결건조로 건조하였다. 화합물의 순도는 99%였다. 수율은 4.2%였다. 전자-분무 이온화 질량 측정기(ESI-MS)를 이용한 분석시, 분자량은 3201.0이었다(분자량 계산치인 3201.7과 일치됨).
전술한 적합한 방법에 따라 하기 예들을 제조할 수 있다.
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2- Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Aib-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly- Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala- (Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr- Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-(Arg)3- Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3- NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3- NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4- NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln- (Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4- NH2;
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr- Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-β-Ala-Cys)-Pro-Pro-Lys-Asp-NH2; 또는
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Aib-Cys)-Pro-Pro-Lys-Asp-NH2.
표 1A 및 1B에 나타낸 화합물과 같은 본 발명의 다른 펩티드들은, 일반적으로 상기에서 개시된 방법 및/또는 전술한 실시예에서 구체적으로 기재된 방법과 유사한 합성 공정을 이용하여 당업자가 제조할 수 있다.
표 1A
화합물 | 분자량 계산치 | 분자량 실험치 | 순도 |
Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2 | 2574.05 | 2573.7 | 99 |
Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2 | 2719.2 | 2718.4 | 99 |
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2645.12 | 2646.8 | 99 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2687.16 | 2688.4 | 93.8 |
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Doc-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2864.36 | 2864.4 | 96.5 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Pro-Pro-Lys-Asp-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3053.58 | 3053.6 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-Pro-Pro-Lys-Asp-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3105.61 | 3105.6 | 99.9 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2758.24 | 2758.3 | 99.9 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3198.73 | 3198.8 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3250.77 | 3250.8 | 97.3 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3190.72 | 3190.7 | 99.2 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3264.79 | 3264.8 | 95.3 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Doc-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2906.4 | 2906.43 | 97.1 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3201.74 | 3201.2 | 99.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3043.57 | 3043.2 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3100.62 | 3099.8 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3263.79 | 3263.6 | 97.4 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Gln-Arg-Arg-Arg-Arg-NH2 | 3190.72 | 3190.0 | 99.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Gln-Arg-Arg-Arg-Arg-Arg-NH2 | 3190.72 | 3190.0 | 99.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-Arg-Arg-Arg-Arg-Arg-NH2 | 3190.72 | 3190.0 | 95.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Arg-Arg-Gln-Arg-NH2 | 3190.72 | 3190.1 | 99.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Aib-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3235.82 | 3235.3 | 99.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3065.55 | 3065.2 | 95.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3037.54 | 3036.8 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3193.73 | 3193.4 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3065.55 | 3065.6 | 97.4 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3037.54 | 3037.1 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3193.73 | 3193.7 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3227.77 | 3227.4 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3071.58 | 3071.1 | 99.1 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3199.76 | 3199.1 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Arg-Gln-Arg-Arg-NH2 | 3190.72 | 3190.5 | 97.5 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-Lys-Lys-Arg-Arg-Arg-Arg-Arg-NH2 | 3190.72 | 3190.2 | 99.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Arg-Arg-Arg-Gln-NH2 | 3190.72 | 3190.2 | 99.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3201.74 | 3201.6 | 99.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3207.77 | 3207.5 | 99.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3009.53 | 3009.6 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3009.53 | 3009.5 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3009.53 | 3009.3 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3229.75 | 3229.3 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3066.58 | 3066.5 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3066.58 | 3066.6 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2906.44 | 2905.6 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Gln-Arg-Arg-Arg-Arg-NH2 | 2687.21 | 2686.8 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2761.28 | 2761.6 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2580.06 | 2579.7 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2523.01 | 2522.5 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2743.23 | 2742.7 | 99.0 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-Arg-NH2 | 2736.25 | 2735.6 | 99.9 |
Ac-c(Cys-Glu-His-D-4-Br-Phe-Arg-Trp-Gly-Cys)-Pro-Pro-Lys-Asp-NH2 | 1592.61 | 1590.8 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 1577.81 | 1577.3 | 99.1 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 1588.83 | 1588.0 | 98.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 1588.83 | 1589.3 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 1594.86 | 1594.1 | 99.9 |
표 1B
화합물 | 분자량 계산치 | 분자량 실험치 | 순도 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-β-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 1588.83 | 1588.6 | 95.6 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Aib-Cys)-Pro-Pro-Lys-Asp-NH2 | 1602.86 | 1602.3 | 94.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3229.75 | 3229.7 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3229.75 | 3230.6 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3066.58 | 3067.0 | 95.4 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3066.58 | 3067.0 | 95.43 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3009.53 | 3009.7 | 99.2 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3229.75 | 3229.7 | 99.45 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3015.55 | 3015.6 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3235.78 | 3235.9 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3235.78 | 3235.9 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3072.61 | 3072.8 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3015.55 | 3015.43 | 99.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3072.61 | 3072.5 | 99.90 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2715.22 | 22715.0 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2715.22 | 2714.7 | 98.8 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2552.05 | 2552.2 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2552.05 | 2552.0 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2494.99 | 2494.9 | 99.9 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2494.99 | 2494.7 | 99.9 |
실시예
3:
시험관내
연구
본 발명의 화합물은, 하기 과정에 따라 하나 이상의 멜라토코르틴 수용체의 리간드로서의 활성을 테스트할 수 있으며, 테스트하였다. 당업자라면 본원에 기재된 방법과 유사한 공정을 이용하여 멜라노코르틴 수용체 분자에 대한 본 발명의 화합물의 결합 활성을 분석할 수 있음을 알 것이다.
방사능 표지된 리간드(Radioligand)의 결합 분석
시험관내 수용체 결합 분석에 사용되는 세포 막은, hMC-R 수용체 서브타입 1, 3, 4 또는 5를 안정적으로 발현하는 CHO-K1 형질전환주로부터 수득하였다. 원하는 hMC-R 수용체를 발현하는 CHO-K1 세포를, pH 7.4의 빙냉한 50 mM Tris-HCl 중에서 초음파처리한 다음(Branson® 7로 설정, 약 30초), 약 4 ℃에서 39,000 g로 10분간 원심분리하였다. 펠렛은 동일한 완충액에 재현탁하고, 약 4 ℃에서 50,000 g로 10분간 원심분리하였다. 세포 막 성분이 함유된 세정한 펠렛은 약 - 80 ℃에 보관하였다.
[125I](Tyr2)-(Nle4-D-Phe7)α-MSH ([125I]-NDP-α-MSH, Amersham Biosciences®) 결합에 대한 경쟁적 저해는, 폴리프로필렌 96 웰 플레이트에서 수행하였다. 전술한 바와 같이 준비한 세포 막(1-10 ㎍ 단백질/웰)은 테스트 화합물의 농도를 증가시키면서 0.2% 소 혈청 알부민(BSA), 5 mM MgCl2, 1 mM CaCl2 및 0.1 mg/mL 박시트라신이 함유된 pH 7.4의 50 mM Tris-HCl 중에서 0.1-0.3 nM [125I]-NDP-α-MSH와 함께 90-12분간 약 37 ℃에서 인큐베이션하였다. Packard Filtermate® 수거기를 이용하여, 0.1 % (w/v) 폴리에틸렌이민(PEI)으로 미리 침지시킨 GF/C 유리 섬유 필터 플레이트(Unifilter®; Packard)를 통한 여과로, 유리 [125I]-NDP-α-MSH로부터, 결합된 [125I]-NDP-α-MSH 리간드를 분리시켰다. 필터를 약 0-4 ℃에서, pH 7.4의 50 mM Tris-HCl을 이용하여 3번 세정한 다음, Packard Topcount® 신틸레이션 카운터를 이용하여 방사능을 분석하였다. 결합 데이타는 컴퓨터를 이용한 비선형 회귀 분석으로 분석하였다(XL fit; IDBS).
선택한 바람직한 구현예를 상기 분석으로 테스트하였고, 결합 상수(nM의 Ki)는 표 2A 및 2B에 나타내었다.
표 2A
화합물 | Ki hMC1-R | Ki hMC3-R | Ki hMC4-R | Ki hMC5-R |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 49.9 | 9.00 | 0.569 | 218 |
Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2 | 11.9 | 38.1 | 5.70 | 11.8 |
Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2 | 3.46 | 16.6 | 6.65 | 4.88 |
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.614 | 5.09 | 2.31 | 3.23 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.56 | 14.1 | 5.17 | 7.12 |
H-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Doc-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.10 | 1.58 | 6.00 | 0.629 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Pro-Pro-Lys-Asp-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.0868 | 0.751 | 0.0944 | 0.147 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-Pro-Pro-Lys-Asp-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.66 | 4.80 | 0.250 | 9.62 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.0452 | 0.298 | 0.169 | 0.386 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.0808 | 0.396 | 0.0747 | 0.311 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 4.41 | 4.23 | 0.455 | 12.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.25 | 0.661 | 0.292 | 5.94 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.89 | 0.546 | 0.166 | 6.06 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 87.8 | 9.08 | 1.20 | 359 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 124 | 17.8 | 1.11 | 348 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 163 | 23.0 | 0.586 | 844 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Doc-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.144 | 0.352 | 0.0845 | 0.415 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.74 | 0.590 | 0.170 | 4.38 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3.86 | 4.97 | 0.192 | 38.3 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 12.8 | 15.9 | 0.950 | 165 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3.07 | 4.05 | 0.498 | 31.1 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-bAla-Tyr-Gly-Arg-Lys-Lys-Arg-Gln-Arg-Arg-Arg-Arg-NH2 | 0.792 | 0.570 | 0.162 | 4.18 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Gln-Arg-Arg-Arg-Arg-Arg-NH2 | 0.726 | 0.474 | 0.209 | 5.12 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-Arg-Arg-Arg-Arg-Arg-NH2 | 0.857 | 0.580 | 0.209 | 4.42 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Arg-Arg-Gln-Arg-NH2 | 0.813 | 0.675 | 0.269 | 4.20 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Aib-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 7.84 | 10.2 | 0.783 | 91.8 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.93 | 9.07 | 0.293 | 59.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.42 | 6.56 | 0.238 | 41.7 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 6.66 | 19.3 | 0.819 | 88.8 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.63 | 2.09 | 0.0737 | 11.6 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.48 | 1.21 | 0.209 | 9.17 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3.65 | 2.26 | 0.261 | 12.1 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 7.32 | 11.0 | 0.659 | 78.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 4.11 | 7.26 | 0.302 | 48.3 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 6.77 | 14.3 | 0.781 | 84.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Arg-Gln-Arg-Arg-NH2 | 3.04 | 3.22 | 0.230 | 3.85 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-Lys-Lys-Arg-Arg-Arg-Arg-Arg-NH2 | 3.24 | 2.66 | 0.208 | 5.96 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Arg-Arg-Arg-Gln-NH2 | 1.58 | 1.43 | 0.275 | 2.97 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 4.59 | 6.28 | 0.588 | 22.6 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 6.46 | 5.22 | 0.380 | 15.3 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 4.62 | 5.68 | 0.505 | 45.3 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.12 | 3.99 | 0.352 | 27.5 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3.41 | 0.975 | 0.549 | 11.3 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 4.18 | 1.12 | 0.223 | 15.3 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.71 | 0.732 | 0.202 | 5.53 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 5.66 | 1.40 | 0.446 | 6.23 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.211 | 0.665 | 0.635 | 118 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Gln-Arg-Arg-Arg-Arg-NH2 | 0.351 | 0.891 | 0.503 | 102 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.209 | 0.699 | 0.596 | 137 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.439 | 1.52 | 0.476 | 115 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.821 | 2.50 | 0.700 | 148 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.406 | 1.11 | 0.602 | 131 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-Arg-NH2 | 1.27 | 4.63 | 1.51 | 220 |
표 2B
화합물 | Ki hMC1-R | Ki hMC3-R | Ki hMC4-R | Ki hMC5-R |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-β-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 2058 | 113 | 10.7 | 239 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Aib-Cys)-Pro-Pro-Lys-Asp-NH2 | 1818 | 306 | 5.87 | 979 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.75 | 1.74 | 0.15 | 16.8 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.50 | 1.61 | 0.301 | 10.4 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.81 | 2.08 | 0.305 | 19.3 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.69 | 2.59 | 0.243 | 19.2 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.25 | 0.62 | 0.303 | 2.77 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.49 | 0.604 | 0.865 | 3.13 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3.28 | 1.95 | 0.575 | 15.5 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.24 | 1.57 | 0.437 | 16.4 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.14 | 1.12 | 0.624 | 11.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.50 | 1.59 | 0.573 | 15.7 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3.00 | 1.70 | 0.442 | 15.5 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 4.29 | 2.15 | 0.425 | 15.5 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.410 | 0.837 | 0.246 | 56.3 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.572 | 1.07 | 0.210 | 63.6 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.475 | 0.800 | 0.196 | 53.8 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.779 | 1.21 | 0.293 | 56.0 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.212 | 1.23 | 0.484 | 58.5 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.778 | 1.22 | 0.468 | 47.0 |
사이클릭
AMP
생분석
세포내 사이클릭 AMP(cAMP) 농도를 전자화학발광(ECL) 분석(Meso Scale Discovery®, Gaithersburg, MD; 이하 MSD라 함)으로 측정하였다. hMC 수용체 서브타입을 안정적으로 발현하는 CHO-K1 세포를 RMPI 1640® 분석 완충액(RMPI 1640 완충액은 0.5 mM 이소부틸메틸크산틴(IBMX) 및 0.2% 단백질 칵테일(MSD blocker A)을 포함함)에 현탁하였다. hMC 수용체 서브타입 1, 3, 4 또는 5를 안정적으로 발현하는 CHO-K1 형질전환주를, 통합형 탄소 전극이 장착되어 있으며 항-cAMP 항체로 코팅된 384웰 멀티-어레이®에 약 7,000 세포/웰의 밀도로 넣었다. 테스트 화합물을 농도를 증가시키면서 첨가하고, 세포를 약 40분간 약 37 ℃에서 배양하였다. 배양한 후, 0.2% 단백질 칵테일 및 2.5 nM TAGTM 루테늄-표지된 cAMP (MSD)이 함유된 라이시스 완충액(MgCl2 및 Triton X-100®이 첨가된 HEPES-완충화된 염수 용액, pH 7.3)을 첨가하여, 세포를 실온에서 약 90분간 배양하였다. 이차 배양한 후, 리딩 완충액(ECL 공-시약 및 X-100가 함유된 Tris-완충화된 용액, pH 7.8)을 첨가하고, Sector Imager 6000 reader®(MSD)를 이용한 ECL 검출에 의해 즉시 세포 라이세이트(cell lysate)에서의 cAMP 농도를 측정하였다. 데이타는 컴퓨터를 이용한 비선 형 회귀 분석(XL fit; IDBS)으로 분석하였고, EC50 수치 또는 Kb 값 중 어느 하나로 기록하였다.
EC50은 최대 반응 반응의 50%, 예컨대 전술한 분석으로 이용하여 결정된 cAMP의 최대 농도의 50%를 수득하는데 필요한 작용제 화합물의 농도이다. Kb 값은 길항제의 효능을 나타내며, Schild 분석에 의해 결정하였다. 간략하게는, 길항제의 농도를 증가시키면서 작용제의 농도-반응 곡선을 구하였다. Kb 값은 작용제에 대한 농도-반응 곡선에서 2배수 변화(shift)를 만드는 길항제의 농도이다. 이는 Schild 플롯에서 y-축에서 0에 라인을 외삽하여 계산한다.
선택한 화합물을 상기 분석으로 테스트하고, 선택 화합물에 대한 cAMP 생분석 데이타는 표 3A, 3B, 3C 및 3D에 나타내었다.
표 3A
화합물 | EC50 hMC1-R | Kb hMC3-R | Kb hMC4-R | EC50 hMC5-R |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 66.1 | 33.4 | 0.687 | 6.84 |
Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2 | ND | 4500 | 105 | ND |
Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2 | ND | 395 | 16.8 | ND |
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | ND | 207 | 18.5 | ND |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | ND | 220 | 4.07 | ND |
H-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Doc-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | ND | 261 | 3.11 | ND |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Pro-Pro-Lys-Asp-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | ND | 14.1 | 22.8 | ND |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-Pro-Pro-Lys-Asp-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | ND | 233 | 26.0 | ND |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.39 | 16.2 | 7.94 | 0.839 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3.65 | 19.4 | 3.73 | 1.61 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | ND | 17.7 | 1.49 | ND |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 6.3 | 70.0 | 1.66 | 38.2 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 12.1 | 30.3 | 1.81 | 70.0 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 33.6 | 140 | 12.2 | 66.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 269 | 105 | 5.92 | 104 |
Ac-c Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | 690 | 70.7 | 4.56 | 177 |
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-Doc-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 3.23 | 8.97 | 4.61 | 2.86 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 52.0 | 170 | 6.14 | 328 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 146 | 104 | 32.0 | 1400 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 114 | 44.6 | 28.4 | 879 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Aib-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 67.1 | 439 | 46.5 | 582 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 144 | 116 | 8.93 | 819 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 36.0 | 46.5 | 11.4 | 56.1 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 93.0 | 71 | 15.9 | >10000 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 39.7 | 30.9 | 6.66 | 501 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 35.2 | 22.9 | 12.6 | 199 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 29.1 | 13.6 | 13.4 | 204 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 86.1 | 41.7 | 19.4 | 2360 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Arg-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 38.3 | 20.2 | 21.2 | >10000 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 68.6 | 153 | 33.2 | >10000 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 70.4 | 286 | 18.6 | >10000 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 33.1 | 65.1 | 15.3 | 1720 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 88.2 | 10.6 | 17.4 | 514 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 58.7 | 39.3 | 10.3 | 460 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 45.4 | 12.7 | 12.7 | 162 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 309 | 22.8 | 17.1 | 570 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 7.86 | 10.5 | 0.843 | 4900 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 29.7 | 25.6 | 7.37 | 82.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Gln-Arg-Arg-Arg-Arg-NH2 | 15.2 | 14.6 | 4.52 | 36.8 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Gln-Arg-Arg-Arg-Arg-Arg-NH2 | 6.7 | 9.38 | 11.7 | 46.2 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-Arg-Arg-Arg-Arg-Arg-NH2 | 7.9 | 41.7 | 10.9 | 62.4 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Arg-Arg-Gln-Arg-NH2 | 16.9 | 36.0 | 7.12 | 58.9 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Arg-Gln-Arg-Arg-NH2 | 16.4 | 20.8 | 7.31 | 44.2 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-Lys-Lys-Arg-Arg-Arg-Arg-Arg-NH2 | 12.0 | 13.7 | 9.38 | 54.2 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Arg-Arg-Arg-Gln-NH2 | 7.5 | 12.2 | 7.61 | 51.7 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 43.3 | 215 | 5.87 | 1286 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 37.9 | 112 | 41.1 | 1798 |
ND = 검출 안됨
표 3B
화합물 | EC50 hMC1 -R | EC50 hMC3 -R | EC50 hMC4 -R | EC50 hMC5 -R |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 4.70 | 4.56 | 0.634 | 147 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Gln-Arg-Arg-Arg-Arg-NH2 | 5.90 | 7.73 | 1.02 | 2890 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 0.481 | 7.32 | 0.964 | 2010 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Arg-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 7.15 | 9.37 | 1.25 | 1570 |
표 3C
화합물 | EC 50 hMC1 -R | Kb hMC3 -R | Kb hMC4 -R | EC 50 hMC5 -R |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-β-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 | ND | ND | ND | ND |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Aib-Cys)-Pro-Pro-Lys-Asp-NH2 | 770 | 221 | 4.52 | 869 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 29 | 22.6 | 16.7 | 173 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 102 | 26.3 | 14.6 | 261 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 26.6 | 101 | 9.34 | 351 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 45.5 | 181 | 6.35 | 149 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 23.7 | 9.22 | 5.87 | 39.7 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 34.7 | 15.0 | 8.68 | 28.2 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 19.1 | 106 | 4.59 | 100 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 19.8 | 37.8 | 8.43 | 158 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 11.2 | 52.1 | 9.45 | 95.7 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 33.8 | 93.6 | 4.42 | 89.5 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 232 | 68.8 | 10.0 | 250 |
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 32.2 | 98.3 | 5.23 | 194 |
ND = 검출 안됨
표 3D
화합물 | EC50 hMC1 -R | EC50 hMC3 -R | EC50 hMC4 -R | EC50 hMC5 -R |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 5.66 | 4.70 | 0.422 | 1551 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 7.57 | 4.18 | 0.600 | 1792 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.36 | 2.74 | 0.260 | 500 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.81 | 3.29 | 0.298 | 566 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 1.86 | 1.39 | 0.367 | 165 |
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2 | 2.06 | 1.61 | 0.394 | 199 |
실시예
4:
시험관내
분석
본 발명의 멜라노코르틴 수용체에 대한 리간드는, 하기 과정에 따라 음식물 섭취 및/또는 체중에 대한 효과를 테스트할 수 있어, 테스트하였다. 당업자라면 본원에 기재된 방법과 유사한 공정을 이용하여 음식물 섭취 및/또는 체중에 대한 본 발명의 화합물의 효과를 분석할 수 있음을 알 것이다.
생체내 분석에서 조사한 화합물은 다음과 같다(표 4).
표 4
리간드 코드 | 구조 |
화합물 A | Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 |
화합물 B | Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 |
화합물 C | Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 |
화합물 D | Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2 |
화합물 E | Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 |
화합물 F | Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2 |
단기 급식 실험(단식)
Sprague Dawley 수컷 랫(250g)을 각각의 케이지에서 넣어, 12:12 시간의 주:야 조건하에 유지시켰다. 랫은 실험을 개시하기 전에 18시간동안 절식시켰으며 물을 자유롭게 식이가능하게 하였다. 0 시간에, 랫에 선택 화합물을 선정한 투여량으로, 예컨대 500 또는 100 nmole/kg 또는 비히클을 피하 주사하고, 음식물을 제공하였다. 개별 음식물 섭취량은 주사 후 약 1, 2, 3, 4, 5 및 6시간동안 측정하였다.
단기 급식 실험(단식 안함)
Sprague Dawley 수컷 랫(250g)을 각각의 케이지에서 넣어, 12:12 시간의 주:야 조건하에 유지시켰다. 실험하는 동안 음식물과 물을 자유롭게 식이가능하게 하였다. 0 시간에, 랫에 화합물을 투여량 8 μmole/kg으로 또는 비히클을 피하 주사하였다. 개별 음식물 섭취량은 주사 후 약 0.5, 1, 1.5, 2, 3 및 4시간 동안 측정하였다. 본 발명의 선택 화합물에 대한 데이타는 도 1에 나타낸다.
장기 급식 실험
Sprague Dawley 수컷 랫(250g)을 각각의 케이지에서 넣어, 12:12 시간의 주:야 조건하에 유지시고, 음식물과 물을 자유롭게 식이가능하게 하였다. 랫에 다양한 용량의 화합물 또는 비히클을 7일간 하루에 3번씩(대략 8시, 12시 및 16시에) 피하 주사하였다. 각각의 체중 및 음식물 섭취량을 매일 측정하였다. 본 발명의 선택 화합물에 대한 데이타는 도 2A, 2B, 3A, 3B, 4A 및 4B에 개시되어 있다.
투약
본 발명의 펩티드는 약제학적으로 하용가능한 염 형태로 제공될 수 있다. 그러한 염의 예로는, 유기산(예, 아세트산, 락트산, 말레산, 시트르산, 말산, 아스코르브산, 숙신산, 벤조산, 메탄설폰산, 톨루엔설폰산 또는 파모산), 무기산(예, 염산, 황산, 또는 인산) 및 폴리머산(예, 탄닌산, 카르복시메틸 셀룰로스, 폴리락트산, 또는 폴리락트산-글리콜산의 공중합체)과 형성된 염이 있으나, 이로 한정되는 것은 아니다. 본 발명의 펩티드 염을 제조하는 전형적인 방법은 당업계에 잘 알려져 있으며, 표준적인 염 교체 방법에 의해 달성될 수 있다. 따라서, 본 발명의 펩티드의 TFA 염(제조용 HPLC 및 TFA가 함유된 완충액에 의한 용출로, 펩티드 정제하여 수득되는 TFA 염)은, 0.25 N 아세트산 수용액 소량에 펩티드를 용해시킴으로써, 아세테이트 염과 같은 다른 염으로 변환시킬 수 있다. 수득되는 용액은 세미-제조용 HPLC 컬럼(Zorbax®, 300 SB, C-8)에 적용한다. 컬럼은, (1) 0.1 N 암모늄 아세테이트 수용액으로 0.5시간; (2) 0.25 N 아세트산 수용액으로 0.5시간; 및 (3) 유속 4 ml/min로 선형 농도 구배(용액 B를 30분간 20%에서 100%로 농도 구배(용액 A는 0.25 N 아세트산 수용액이고, 용액 B는 아세토니트릴/물, 80:20 중의 0.25 N 아세트산 수용액임)로 용출시킨다.
당업자들에게 잘 알려져 있는 바와 같이, 멜라노코르틴 수용체(MC-R) 작용제 활성을 가질 펩티드의 공지된 용도 및 잠재적인 용도는 다양하고 다채로워, 작용제 작용을 도출하기 위한 목적으로 본 발명의 화합물을 투여하면 멜라노코르틴 그 자체와 동일한 효과 및 용도를 가질 수 있다.
따라서, 본 발명은 활성 성분으로서 식(I)의 화합물 1종 이상을 약제학적으로 허용가능한 담체와 조합하여 포함하는, 약학 조성물을 포함한다.
본 발명의 조성물에서 활성 성분의 투여량은 다양할 수 있지만, 활성 성분의 양은 적합한 투약 형태를 수득할 수 있어야 한다. 선택되는 투여량은 원하는 치료 효과, 투여 경로 및 치료 기간에 따라 결정된다. 대게, 본 발명의 활성에 있어 유효량은 1x10-7 내지 200 mg/kg/day, 바람직하기로는 1x10-4 내지 100 mg/kg/day이며, 이는 단일 투약으로서 투여하거나 또는 다중 투약으로 분할하여 투여할 수 있다.
본 발명의 화합물은 경구, 비경구(예, 근육내, 복막내, 정맥내 또는 피하내 주입 또는 이식), 비내, 질, 직장, 설하 또는 국소 투여 경로에 의해 투여될 수 있으며, 각 투여 경로에 적합한 투약 형태를 제공하기 위해 약제학적으로 허용가능한 담체와 함께 제형화될 수 있다.
경구 투여를 위한 고형의 투약 형태로는, 캡슐제, 정제, 환제(pills), 산제 및 과립제를 포함한다. 상기 고형의 투약 형태에서, 활성 화합물은 하나 이상의 약제학적으로 허용가능한 불활성 담체, 예컨대 자당, 유당 또는 전분과 혼합된다. 상기 투약 형태는 또한 통상 실시되는 바와 같이, 상기한 불활성 희석제 이외의 부가적인 물질, 예컨대 마그네슘 스테아레이트와 같은 윤활제를 포함할 수 있다. 캡슐제, 정제 및 환제의 경우, 투약 형태는 또한 완충제를 포함할 수도 있다. 정제와 환제는 부가적으로 장내 코팅형태(entteric coating)로 제조될 수 있다.
경구 투여를 위한 액상 투약 형태는, 약학적으로 허용가능한 유제, 액제, 현 탁제, 시럽제, 물과 같이 당해분야에서 일반적으로 사용되는 불활성의 희석제를 함유하는 엘릭실제를 포함한다. 이러한 불활성의 희석제 이외에, 조성물은 또한 습윤제, 유화제, 현탁제, 감미제, 향미제 및 향료와 같은 보강제(adjuvant)를 더 포함할 수 있다.
본 발명의 비경구 투여용 조제물은, 멸균 수용액 또는 비수성 용액, 현탁제 또는 유화제를 포함한다. 비수성 용액 또는 비히클의 예로는, 프로필렌 글리콜, 폴리에틸렌 글리콜, 올리브 오일 및 옥수수 오일과 같은 식물성 오일, 젤라틴 및 에틸 올레이트와 같은 주사가능한 유기 에스테르를 포함한다. 이러한 투약 형태는 또한 보존제, 습윤제, 유화제 및 분산제와 같은 보강제를 포함할 수 있다. 이는, 예컨대 박테리아 체류 필터를 통한 여과, 조성물내 멸균제 첨가, 조성물에 방사선 조사 또는 조성물의 열처리에 의해 멸균시킬 수도 있다. 또한, 이는 사용하기 바로 전에 멸균수 또는 주입가능한 기타 멸균 매질에 용해될 수 있는 고형의 멸균 조성물의 형태로 제조될 수 있다.
직장 또는 질 투여용 조성물은 바람직하기로는 활성 성분과 더불어 코코아 버터나 좌제 왁스와 같은 부형제를 포함할 수도 있는 좌제이다.
비내 또는 설하 투여용 조성물은 또는 당해분야에 잘 알려진 표준적인 부형제가 부가된 형태로 제조된다.
또한, 본 발명의 화합물은 하기 특허 및 특허 출원에 개시된 바와 같이 서방형 방출 조성물 형태로 투여될 수 있다. 미국 특허 제 5,672,659호에는, 생활성제와 폴리에스테르로 구성된 서방형 방출 조성물이 개시되어 있다. 미국 특허 제 5,595,760호에는 생활성제로 구성된 젤 형태의 서방형 방출 조성물이 개시되어 있다. 미국 특허 제 5,821,221호에는 생활성제 및 키토산으로 구성된 폴리머성 서방형 방출 조성물이 개시되어 있다. 미국 특허 제 5,916,883호에는 생활성제 및 사이클로덱스트린으로 구성된 서방형 방출 조성물이 개시되어 있다. 이러한 특허 및 출원의 내용은 원용에 의해 본 명세서에 포함된다.
SEQUENCE LISTING
<110> BIOMEASURE, INCORPORATED
<120> LIGANDS OF MELANOCORTIN RECEPTORS
<130> 156P/PCT2
<140> PCT/US2006/26554
<141> 2006-07-10
<150> US 60/697594
<151> 2005-07-08
<160> 211
<170> PatentIn version 3.3
<210> 1
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (12)..(12)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (13)..(18)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (15)..(15)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 1
Tyr Gly Arg Lys Lys Arg Arg Gln Arg Arg Arg Xaa Asp His Xaa Arg
1 5 10 15
Trp Lys
<210> 2
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (12)..(12)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (14)..(19)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (16)..(16)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 2
Tyr Gly Arg Lys Lys Arg Arg Gln Arg Arg Arg Xaa Xaa Asp His Xaa
1 5 10 15
Arg Trp Lys
<210> 3
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle or Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 3
Xaa Asp His Xaa Arg Trp Lys Xaa Tyr Gly Arg Lys Lys Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 4
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 4
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Tyr Gly Arg Lys Lys Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 5
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 5
Xaa Asp His Xaa Arg Trp Lys Pro Pro Lys Asp Tyr Gly Arg Lys Lys
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 6
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 6
Cys Glu His Xaa Arg Trp Gly Cys Pro Pro Lys Asp Tyr Gly Arg Lys
1 5 10 15
Lys Arg Arg Gln Arg Arg Arg
20
<210> 7
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 7
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Tyr Gly Arg Lys Lys Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 8
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (12)..(12)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 8
Xaa Asp His Xaa Arg Trp Lys Pro Pro Lys Asp Xaa Tyr Gly Arg Lys
1 5 10 15
Lys Arg Arg Gln Arg Arg Arg
20
<210> 9
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 9
Cys Glu His Xaa Arg Trp Gly Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Arg Gln Arg Arg Arg
20
<210> 10
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala or 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 10
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Arg Gln Arg Arg Arg
20
<210> 11
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 11
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Tyr Gly Arg Lys Lys Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 12
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal), beta-(1-naphthyl)Ala (1-Nal)
or 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 12
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Arg Gln Arg Arg Arg
20
<210> 13
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 13
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 14
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 14
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Gly Arg Arg
1 5 10 15
Arg Arg Arg Gln Arg Arg Arg
20
<210> 15
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 15
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Gln Arg Arg Arg
20
<210> 16
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 16
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Gln Arg Arg Arg Arg
20
<210> 17
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 17
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Gln Arg Arg Arg Arg Arg
20
<210> 18
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 18
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Gln Lys Arg Arg Arg Arg Arg
20
<210> 19
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 19
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Arg Arg Arg Gln Arg
20
<210> 20
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (15)..(15)
<223> Xaa = alpha-aminoisobutyric acid (Aib)
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 20
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Tyr Xaa Arg
1 5 10 15
Lys Lys Arg Arg Gln Arg Arg Arg
20
<210> 21
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Arg or Lys
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 21
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 22
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal) or beta-(2-naphthyl)Ala
(2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 22
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Arg Gln Arg Arg Arg
20
<210> 23
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Arg or Lys
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 23
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 24
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Arg or Lys
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 24
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Arg Gln Arg Arg Arg
20
<210> 25
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 25
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Arg Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 26
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 26
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Arg Arg Gln Arg Arg
20
<210> 27
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 27
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Gln Lys Lys Arg Arg Arg Arg Arg
20
<210> 28
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 28
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Arg Arg Arg Arg Gln
20
<210> 29
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal) or beta-(2-naphthyl)Ala
(2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 29
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Arg Lys
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 30
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 30
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Lys Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 31
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 31
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Lys Arg Arg Gln Arg Arg Arg
20
<210> 32
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 32
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Gly Arg Arg
1 5 10 15
Lys Arg Arg Gln Arg Arg Arg
20
<210> 33
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal) or beta-(1-naphthyl)Ala
(1-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 33
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Gly Arg Lys
1 5 10 15
Arg Arg Arg Gln Arg Arg Arg
20
<210> 34
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 34
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Arg Lys
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 35
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 35
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Lys Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 36
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 36
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Lys Arg Arg Gln Arg Arg Arg
20
<210> 37
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 37
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Arg Arg Arg Gln Arg Arg Arg
20
<210> 38
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 38
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Gly Arg Arg
1 5 10 15
Lys Arg Arg Gln Arg Arg Arg
20
<210> 39
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 39
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Arg Lys
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 40
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 40
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Lys Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 41
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal) or 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 41
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Lys Arg Arg Gln Arg Arg Arg
20
<210> 42
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal) or 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 42
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Arg Arg Arg Gln Arg Arg Arg
20
<210> 43
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal) or 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 43
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Gly Arg Arg
1 5 10 15
Lys Arg Arg Gln Arg Arg Arg
20
<210> 44
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal) or 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 44
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Gly Arg Lys
1 5 10 15
Arg Arg Arg Gln Arg Arg Arg
20
<210> 45
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 45
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Arg Lys
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 46
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 46
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Arg Lys Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 47
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 47
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Gln Arg Arg Arg Arg
20
<210> 48
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 48
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Gln Arg Arg Arg Arg Arg
20
<210> 49
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 49
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Gln Lys Arg Arg Arg Arg Arg
20
<210> 50
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 50
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Gln Lys Lys Arg Arg Arg Arg Arg
20
<210> 51
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 51
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Arg Arg Gln Arg Arg
20
<210> 52
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 52
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Arg Arg Arg Gln Arg
20
<210> 53
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 53
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Lys Asp Xaa Tyr Gly Arg
1 5 10 15
Lys Lys Arg Arg Arg Arg Arg Gln
20
<210> 54
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 54
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 55
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 55
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Gln Arg Arg Arg
20
<210> 56
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 56
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg Arg
20
<210> 57
<211> 25
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (25)..(25)
<223> AMIDATION
<400> 57
Cys Glu His Xaa Arg Trp Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Gln Arg Arg Arg Arg
20 25
<210> 58
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 58
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 59
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 59
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg Arg
20
<210> 60
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 60
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Arg Gln Arg Arg Arg
20
<210> 61
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 61
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Gln Arg Arg Arg
20
<210> 62
<211> 25
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (25)..(25)
<223> AMIDATION
<400> 62
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Gln Arg Arg Arg Arg
20 25
<210> 63
<211> 25
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(1-naphthyl)Ala (1-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (25)..(25)
<223> AMIDATION
<400> 63
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Arg Gln Arg Arg Arg
20 25
<210> 64
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 64
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 65
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 65
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Arg Gln Arg Arg Arg
20
<210> 66
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 66
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg Arg
20
<210> 67
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 67
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Gln Arg Arg Arg
20
<210> 68
<211> 25
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (25)..(25)
<223> AMIDATION
<400> 68
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Arg Gln Arg Arg Arg
20 25
<210> 69
<211> 25
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (25)..(25)
<223> AMIDATION
<400> 69
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Gln Arg Arg Arg Arg
20 25
<210> 70
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 70
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 71
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 71
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg Arg
20
<210> 72
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 72
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Arg Arg Arg
1 5 10 15
Arg Arg Arg Gln Arg Arg Arg
20
<210> 73
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 73
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp Xaa Gly Arg Arg
1 5 10 15
Arg Arg Arg Gln Arg Arg Arg
20
<210> 74
<211> 24
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (24)..(24)
<223> AMIDATION
<400> 74
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Gln Arg Arg Arg
20
<210> 75
<211> 25
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (25)..(25)
<223> AMIDATION
<400> 75
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Gln Arg Arg Arg Arg
20 25
<210> 76
<211> 25
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 3-benzothienylAla (Bal)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Lys or Arg
<220>
<221> MISC_FEATURE
<222> (13)..(13)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (25)..(25)
<223> AMIDATION
<400> 76
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Xaa Asp Xaa Tyr Gly Arg
1 5 10 15
Arg Arg Arg Arg Arg Gln Arg Arg Arg
20 25
<210> 77
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 77
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Tyr Gly Arg Lys Lys Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 78
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 78
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Tyr Gly Arg Lys Lys Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 79
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 79
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 80
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 80
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 81
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 81
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Gly Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 82
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 82
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Gly Arg Arg Lys Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 83
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 83
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Gly Arg Lys Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 84
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 84
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Arg Arg Lys Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 85
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 85
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Arg Lys Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 86
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 86
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Tyr Gly Arg Lys Lys Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 87
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 87
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Tyr Gly Arg Lys Lys Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 88
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 88
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 89
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 89
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 90
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 90
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Xaa Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 91
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 91
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 92
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 92
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 93
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 93
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Xaa Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 94
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 94
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg Arg
20
<210> 95
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 95
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 96
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 96
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Xaa Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 97
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 97
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg Arg
20
<210> 98
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 98
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 99
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 99
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Xaa Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 100
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 100
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 101
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 101
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 102
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 102
Xaa Asp His Xaa Arg Trp Ala Lys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 103
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 103
Xaa Asp His Xaa Arg Trp Ala Lys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 104
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 104
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 105
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 105
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 106
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 106
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 107
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 107
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Gly Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 108
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 108
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Xaa Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 109
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 109
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 110
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 110
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg Arg
<210> 111
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 111
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg Arg
20
<210> 112
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 112
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 113
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 113
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg Arg
<210> 114
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 114
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg Arg
20
<210> 115
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(7)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 115
Xaa Asp His Xaa Arg Trp Lys Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 116
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 116
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 117
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 117
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 118
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 6-aminohexanoic acid (Ahx)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 118
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 119
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 6-aminohexanoic acid (Ahx)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 119
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 120
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 120
Xaa Cys His Xaa Arg Trp Xaa Xaa Thr Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 121
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 121
Xaa Cys His Xaa Arg Trp Xaa Xaa Thr Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 122
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 122
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 123
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 123
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 124
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = beta-cyclohexylAla (Cha) or Nle, both modified with acyl (Ac)
(Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 124
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 125
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = beta-cyclohexylAla (Cha) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 125
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 126
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle or cyclohexylGly (Chg), both modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 126
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 127
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = cyclohexylGly (Chg) or homo-cyclohexylAla (hCha), both
modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 127
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 128
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-cyclohexylAla (hCha) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 128
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 129
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-cyclohexylAla (hCha) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 129
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 130
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-cyclohexylAla (hCha) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 130
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 131
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-cyclohexylAla (hCha) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 131
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 132
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-cyclohexylAla (hCha) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 132
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 133
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-cyclohexylAla (hCha) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 133
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 134
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-cyclohexylAla (hCha) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 134
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 135
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-cyclohexylAla (hCha) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 135
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 136
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-cyclohexylGly (D-Chg) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 136
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 137
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-cyclohexylGly (D-Chg) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 137
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 138
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-phenylAla (hPhe) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 138
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 139
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = homo-phenylAla (hPhe) modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 139
Xaa Asp His Xaa Arg Trp Xaa Lys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 140
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = D-Trp
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn) or 6-aminohexanoic acid (Ahx)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 140
Xaa Cys His Xaa Arg Xaa Xaa Cys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 141
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = D-Trp
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn) or 6-aminohexanoic acid (Ahx)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 141
Xaa Cys His Xaa Arg Xaa Xaa Cys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 142
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = D-Trp
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 142
Xaa Cys His Xaa Arg Xaa Xaa Cys Xaa Tyr Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 143
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = D-Trp
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 143
Xaa Cys His Xaa Arg Xaa Xaa Cys Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 144
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = penicillamine (Pen)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 144
Xaa Cys Xaa His Xaa Arg Trp Xaa Xaa Xaa Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 145
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = penicillamine (Pen)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 145
Xaa Cys Xaa His Xaa Arg Trp Xaa Xaa Xaa Xaa Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 146
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = penicillamine (Pen)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 146
Xaa Cys Xaa His Xaa Arg Trp Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 147
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = penicillamine (Pen)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 147
Xaa Cys Xaa His Xaa Arg Trp Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 148
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = penicillamine (Pen)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 148
Xaa Cys Xaa His Xaa Arg Trp Xaa Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 149
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = penicillamine (Pen)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 149
Xaa Cys Xaa His Xaa Arg Trp Xaa Xaa Xaa Xaa Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 150
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 150
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Xaa Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 151
<211> 18
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (18)..(18)
<223> AMIDATION
<400> 151
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg
<210> 152
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 152
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln Arg
1 5 10 15
Arg Arg Arg
<210> 153
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 153
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 154
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Gly or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 154
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Xaa Xaa Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 155
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 155
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Xaa Gly Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 156
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = Tyr or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 156
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Xaa Xaa Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 157
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 157
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 158
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 158
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 159
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 159
Xaa Cys His Xaa Xaa Trp Xaa Xaa Thr Xaa Xaa Tyr Gly Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 160
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 160
Xaa Cys His Xaa Xaa Trp Xaa Xaa Thr Xaa Xaa Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 161
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 161
Xaa Cys His Xaa Xaa Trp Xaa Xaa Thr Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 162
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 162
Xaa Cys His Xaa Xaa Trp Xaa Xaa Thr Xaa Xaa Tyr Gly Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 163
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 163
Xaa Cys His Xaa Xaa Trp Xaa Xaa Thr Xaa Xaa Tyr Gly Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg Arg
20
<210> 164
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 164
Xaa Cys His Xaa Xaa Trp Xaa Xaa Thr Xaa Xaa Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg Arg
20
<210> 165
<211> 23
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (23)..(23)
<223> AMIDATION
<400> 165
Xaa Cys His Xaa Xaa Trp Xaa Xaa Thr Xaa Xaa Tyr Gly Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg Arg
20
<210> 166
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 166
Xaa Cys His Xaa Xaa Trp Xaa Xaa Thr Xaa Xaa Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg Arg
20
<210> 167
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 4,4'-biphenylAla (Bip)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 167
Xaa Cys His Xaa Xaa Xaa Xaa Xaa Thr Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 168
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 4,4'-biphenylAla (Bip)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 168
Xaa Cys His Xaa Xaa Xaa Xaa Xaa Thr Xaa Xaa Tyr Gly Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 169
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 4,4'-biphenylAla (Bip)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 169
Xaa Cys His Xaa Xaa Xaa Xaa Xaa Thr Xaa Xaa Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 170
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = 4,4'-biphenylAla (Bip)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 170
Xaa Cys His Xaa Xaa Xaa Xaa Xaa Thr Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 171
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 4,4'-biphenylAla (Bip)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 171
Xaa Cys His Xaa Xaa Xaa Xaa Xaa Thr Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 172
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 4,4'-biphenylAla (Bip)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 172
Xaa Cys His Xaa Xaa Xaa Xaa Xaa Thr Xaa Xaa Tyr Gly Arg Arg Arg
1 5 10 15
Arg Arg Gln Arg Arg Arg
20
<210> 173
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = homo-Arg (hArg)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = 4,4'-biphenylAla (Bip)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (11)..(11)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 173
Xaa Cys His Xaa Xaa Xaa Xaa Xaa Thr Xaa Xaa Arg Arg Arg Arg Arg
1 5 10 15
Gln Arg Arg Arg
20
<210> 174
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(9)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 174
Xaa Cys Xaa His Xaa Arg Trp Gly Cys Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 175
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(9)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Ala
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 175
Xaa Cys Xaa His Xaa Arg Trp Gly Cys Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 176
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 176
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 177
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 177
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 178
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 178
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 179
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 179
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 180
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 180
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 181
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 181
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 182
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 182
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 183
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 5-aminopentanoic acid (Apn)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 183
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 184
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Leu
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 184
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 185
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Leu
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 185
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 186
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Leu
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 186
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 187
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Leu
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 187
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 188
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Leu
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 188
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 189
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Leu
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 189
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 190
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Leu
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 190
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 191
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-Leu
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 191
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 192
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-beta-cyclohexylAla (D-Cha)
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 192
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 193
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-beta-cyclohexylAla (D-Cha)
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 193
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 194
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-beta-cyclohexylAla (D-Cha)
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 194
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 195
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = beta-cyclohexylAla (D-Cha)
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 195
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 196
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-beta-cyclohexylAla (D-Cha)
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 196
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 197
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-beta-cyclohexylAla (D-Cha)
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 197
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 198
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-beta-cyclohexylAla (D-Cha)
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 198
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 199
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle modified with acyl (Ac)
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (3)..(3)
<223> Xaa = D-beta-cyclohexylAla (D-Cha)
<220>
<221> MISC_FEATURE
<222> (5)..(5)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 199
Xaa Cys Xaa His Xaa Arg Trp Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 200
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 200
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 201
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 201
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 202
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 202
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 203
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 203
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 204
<211> 21
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (21)..(21)
<223> AMIDATION
<400> 204
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg
20
<210> 205
<211> 19
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (19)..(19)
<223> AMIDATION
<400> 205
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg
<210> 206
<211> 22
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (22)..(22)
<223> AMIDATION
<400> 206
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Tyr Gly Arg Arg Arg Arg
1 5 10 15
Arg Gln Arg Arg Arg Arg
20
<210> 207
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = Nle
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-Phe
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = 4-aminobutyric acid (Gaba)
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc)
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = 8-amino-3,6-dioxaoctanoic acid (Doc) or absent
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 207
Xaa Cys His Xaa Arg Trp Xaa Cys Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 208
<211> 20
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> MISC_FEATURE
<222> (1)..(1)
<223> Xaa = D-Phe
<220>
<221> DOMAIN
<222> (2)..(8)
<223> cyclic
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-(Et)Tyr
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (8)..(8)
<223> Xaa = D-Cys
<220>
<221> MISC_FEATURE
<222> (9)..(9)
<223> Xaa = beta-Ala
<220>
<221> MISC_FEATURE
<222> (10)..(10)
<223> Xaa = beta-Ala
<220>
<221> MOD_RES
<222> (20)..(20)
<223> AMIDATION
<400> 208
Xaa Cys His Xaa Arg Trp Xaa Xaa Xaa Xaa Arg Arg Arg Arg Arg Gln
1 5 10 15
Arg Arg Arg Arg
20
<210> 209
<211> 12
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-4-bromo-phenylAla (D-4-Br-Phe)
<220>
<221> MOD_RES
<222> (12)..(12)
<223> AMIDATION
<400> 209
Cys Glu His Xaa Arg Trp Gly Cys Pro Pro Lys Asp
1 5 10
<210> 210
<211> 12
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = Trp, beta-(2-naphthyl)Ala (2-Nal), beta-(1-naphthyl)Ala
(1-Nal) or 3-benzothienylAla (Bal)
<220>
<221> MOD_RES
<222> (12)..(12)
<223> AMIDATION
<400> 210
Cys Glu His Xaa Arg Xaa Ala Cys Pro Pro Lys Asp
1 5 10
<210> 211
<211> 12
<212> PRT
<213> Artificial Sequence
<220>
<223> Ligand of melanocortin receptor
<220>
<221> DOMAIN
<222> (1)..(8)
<223> cyclic
<220>
<221> MOD_RES
<222> (1)..(1)
<223> modified with acyl (Ac)
<220>
<221> MISC_FEATURE
<222> (4)..(4)
<223> Xaa = D-beta-(2-naphthyl)Ala (D-2-Nal)
<220>
<221> MISC_FEATURE
<222> (6)..(6)
<223> Xaa = beta-(2-naphthyl)Ala (2-Nal)
<220>
<221> MISC_FEATURE
<222> (7)..(7)
<223> Xaa = beta-Ala or alpha-aminoisobutyric acid (Aib)
<220>
<221> MOD_RES
<222> (12)..(12)
<223> AMIDATION
<400> 211
Cys Glu His Xaa Arg Xaa Xaa Cys Pro Pro Lys Asp
1 5 10
Claims (133)
- 식 (I)의 화합물 또는 약제학적으로 허용가능한 그의 염:식 (I)(R2R3)-B1-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-A11-A12-A13-B2-B3-R1상기 식 (I)에서,B1은 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 또는 15개의 아미노산을 포함하며 5개 이상의 아미노산은 독립적으로 L-Arg, D-Arg, L-hArg 및 D-hArg으로 이루어진 군으로부터 선택되는 펩티드 모이어티이거나, 또는 B1은 선택적으로 삭제되며;A1은 Acc, HN-(CH2)m-C(O), L-아미노산 또는 D-아미노산이거나, 삭제되며;A2는 Cys, D-Cys, hCys, D-hCys, Pen, D-Pen, Asp 또는 Glu이며;A3는 Gly, Glu, Ala, β-Ala, Gaba, Aib 또는 D-아미노산이거나, 삭제되며;A4는 His, 2-Pal, 3-Pal, 4-Pal, Taz, 2-Thi, 3-Thi, 또는 (X1,X2,X3,X4,X5)Phe이며;A5는 D-Phe, D-1-Nal, D-2-Nal, D-Trp, D-Bal, D-(X1,X2,X3,X4,X5)Phe, D-(Et)Tyr, D-Dip, D-Bip 또는 D-Bpa이며;A6은 Arg, hArg, Dab, Dap, Lys, Orn 또는 HN-CH((CH2)n-N(R4R5))-C(O)이며;A7은 Trp, 1-Nal, 2-Nal, Bal, Bip, Dip, Bpa, D-Trp, D-1-Nal, D-2-Nal, D-Bal, D-Dip 또는 D-Bip이며;A8은 Gly, D-Ala, Acc, Ala, β-Ala, Gaba, Apn, Ahx, Aha, HN-(CH2)s-C(O)이거나, 삭제되며;A9는 Cys, D-Cys, hCys, D-hCys, Pen, D-Pen, Dab, Dap, Orn 또는 Lys이며;A10은 Acc, HN-(CH2)t-C(O), Pro, hPro, 3-Hyp, 4-Hyp, Thr, L- 또는 D-아미노산이거나, 삭제되며;A11은 Pro, hPro, 3-Hyp 또는 4-Hyp이거나, 삭제되며;A12는 Lys, Dab, Dap, Arg 또는 hArg이거나, 삭제되며;A13은 Asp 또는 Glu이거나, 삭제되며;B2는 1, 2, 3, 4 또는 5개의 아미노산을 포함하는 펩티드 모이어티이거나, 삭제되며,B3은 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 또는 15개의 아미노산을 포함하며 5개 이상의 아미노산은 독립적으로 L-Arg, D-Arg, L-hArg 및 D-hArg로 이루어진 군 으로부터 선택되는 펩티드 모이어티이거나, 삭제되며;R1은 -OH 또는 -NH2이며;R2 및 R3는 각각 각 경우에 독립적으로, H, (C1-C30)알킬, (C1-C30)헤테로알킬, (C1-C30)아실, (C2-C30)알케닐, (C2-C30)알키닐, 아릴(C1-C30)알킬, 아릴(C1-C30)아실, 치환된 (C1-C30)알킬, 치환된 (C1-C30)헤테로알킬, 치환된 (C1-C30)아실, 치환된 (C2-C30)알케닐, 치환된 (C2-C30)알키닐, 치환된 아릴(C1-C30)알킬 및 치환된 아릴(C1-C30)아실로 이루어진 군으로부터 선택되며;R4 및 R5는 각각 각 경우에 독립적으로, H, (C1-C40)알킬, (C1-C40)헤테로알킬, (C1-C40)아실, (C2-C40)알케닐, (C2-C40)알키닐, 아릴(C1-C40)알킬, 아릴(C1-C40)아실, 치환된 (C1-C40)알킬, 치환된 (C1-C40)헤테로알킬, 치환된 (C1-C40)아실, 치환된 (C2-C40)알케닐, 치환된 (C2-C40)알키닐, 치환된 아릴(C1-C40)알킬, 치환된 아릴(C1-C40)아실, (C1-C40)알킬설포닐 또는 -C(NH)-NH2이며;n은 각 경우에 독립적으로, 1, 2, 3, 4 또는 5이며;m은 각 경우에 독립적으로, 1, 2, 3, 4, 5, 6 또는 7이며;s는 각 경우에 독립적으로, 1, 2, 3, 4, 5, 6 또는 7이며;t는 각 경우에 독립적으로, 1, 2, 3, 4, 5, 6 또는 7이며;X1, X2, X3, X4 및 X5는 각각 각 경우에 독립적으로 H, F, Cl, Br, I, (C1 -10)알킬, 치환된 (C1 -10)알킬, (C2 -10)알케닐, 치환된 (C2 -10)알케닐, (C2 -10)알키닐, 치환된 (C2 -10)알키닐, 아릴, 치환된 아릴, OH, NH2, NO2 또는 CN이며;단, 하기를 만족한다:(I). R4가 (C1-C40)아실, 아릴(C1-C40)아실, 치환된 (C1-C40)아실, 치환된 아릴(C1-C40)아실, (C1-C40)알킬설포닐 또는 -C(NH)-NH2이면, R5는 H, (C1-C40)알킬, (C1-C40)헤테로알킬, (C2-C40)알케닐, (C2-C40)알키닐, 아릴(C1-C40)알킬, 치환된 (C1-C40)알킬, 치환된 (C1-C40)헤테로알킬, 치환된 (C2-C40)알케닐, 치환된 (C2-C40)알키닐, 또는 치환된 아릴(C1-C40)알킬이고;(II). R2가 (C1-C30)아실, 아릴(C1-C30)아실, 치환된 (C1-C30)아실, 또는 치환된 아릴(C1-C30)아실이면, R3은 H, (C1-C30)알킬, (C1-C30)헤테로알킬, (C2-C30)알케닐, (C2-C30)알키닐, 아릴(C1-C30)알킬, 치환된 (C1-C30)알킬, 치환된 (C1-C30)헤테로알킬, 치환된 (C2-C30)알케닐, 치환된 (C2-C30)알키닐, 또는 치환된 아릴(C1-C30)알킬이고;(III) B1 및 B2 둘다 아미노산 서열: Arg-(Lys)2-(Arg)2-Gln-(Arg)3, Tyr-Ala- Arg-Lys-Ala-(Arg)2-Gln-Ala-(Arg)2, Tyr-Ala-Arg-(Ala)2-(Arg)2-(Ala)2-(Arg)2, Tyr-Ala-(Arg)9, Tyr-(Ala)3-(Arg)7, Tyr-Ala-Arg-Ala-Pro-(Arg)2-Ala-(Arg)3 및 Tyr-Ala-Arg-Ala-Pro-(Arg)2-Pro-(Arg)2 중 하나 이상을 포함하지 않으며;(IV) B1 및 B2 중 어느 하나 또는 둘다는 상기 화합물에 존재하여야 하며;(V) A2가 Cys, D-Cys, hCys, D-hCys, Pen 또는 D-Pen이면, A9는 Cys, D-Cys, hCys, D-hCys, Pen 또는 D-Pen이고;(VI) A2가 Asp 또는 Glu이면, A9는 Dab, Dap, Orn 또는 Lys이다.
- 제 1항에 있어서,B1은 Arg-Lys-Gln-Lys-(Arg)5, Arg-(Lys)2-Arg-Gln-(Arg)4, Arg-(Lys)2-(Arg)3-Gln-(Arg)2, Arg-(Lys)2-(Arg)4-Gln-Arg, Arg-(Lys)2-(Arg)5-Gln, Arg-(Lys)2-Gln-(Arg)5, Arg-Gln-(Lys)2-(Arg)5, Arg-Gln-(Arg)7, Arg-Gln-(Arg)8, (Arg)2-Gln-(Arg)6, (Arg)2-Gln-(Arg)7, (Arg)3-Gln-(Arg)5, (Arg)3-Gln-(Arg)6, (Arg)4-Gln-(Arg)4, (Arg)4-Gln-(Arg)5, (Arg)5, (Arg)5-Gln-(Arg)3, (Arg)5-Gln-(Arg)4, (Arg)6, (Arg)6-Gln-(Arg)3, (Arg)7, (Arg)7-Gln-(Arg)2, (Arg)8, (Arg)8-Gln-Arg, (Arg)9, (Arg)9-Gln, (D-Arg)5, (D-Arg)6, (D-Arg)7, (D-Arg)8, (D-Arg)9, Gln-Arg-(Lys)2- (Arg)5, Gln-(Arg)8, Gln-(Arg)9, Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3, 또는 Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc이거나, 삭제되며;B2는 β-Ala, β-Ala-Gly, β-Ala-Tyr, β-Ala-Tyr-Gly, (β-Ala)2, (β-Ala)2-Gly, (β-Ala)2-Tyr, (β-Ala)2-Tyr-Gly, Doc, Doc-Gly, Doc-Tyr, Doc-Tyr-Gly, (Doc)2, (Doc)2-Gly 또는 (Doc)2-Tyr, Doc)2-Tyr-Gly이거나, 삭제되며;B3은 Arg-Lys-Gln-Lys-(Arg)5, Arg-Lys-(Arg)3-Gln-(Arg)3, Arg-(Lys)2-Arg-Gln-(Arg)4, Arg-(Lys)2-Gln-(Arg)5, Arg-(Lys)2-(Arg)2-Gln-(Arg)3, Arg-(Lys)2-(Arg)3-Gln-(Arg)2, Arg-(Lys)2-(Arg)4-Gln-Arg, Arg-(Lys)2-(Arg)5-Gln, Arg-Gln-(Lys)2-(Arg)5, Arg-Gln-(Arg)7, Arg-Gln-(Arg)8, (Arg)2-Lys-(Arg)2-Gln-(Arg)3, (Arg)2-Gln-(Arg)6, (Arg)2-Gln-(Arg)7, (Arg)3-Gln-(Arg)5, (Arg)3-Gln-(Arg)6, (Arg)4-Gln-(Arg)4, (Arg)4-Gln-(Arg)5, (Arg)5, (Arg)5-Gln-(Arg)3, (Arg)5-Gln-(Arg)4, (Arg)6, (Arg)6-Gln-(Arg)3, (Arg)7, (Arg)7-Gln-(Arg)2, (Arg)8, (Arg)8-Gln-Arg, (Arg)9, (Arg)9-Gln, (D-Arg)5, (D-Arg)6, (D-Arg)7, (D-Arg)8, (D-Arg)9, Gln-Arg-(Lys)2-(Arg)5, 또는 Gln-(Arg)8, Gln-(Arg)9이거나, 삭제되는 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염..
- 제 2항에 있어서,A1은 A6c, Gaba, Nle, Met, Phe, D-Phe, D-2-Nal, hPhe, Chg, D-Chg, Cha, hCha, hPro, hLeu, Nip, β-hMet 또는 Oic이거나, 삭제되며;A3은 Gly, Glu, Ala, β-Ala, Gaba, Aib, D-Ala, D-Abu, D-Val, D-Leu, D-Ile, D-Met, D-Nle, D-Cha, D-Phe, D-Tyr, D-Trp 또는 D-Tle이거나, 삭제되며;A4는 His이며;A5는 D-Phe, D-1-Nal, D-2-Nal, D-Trp, D-Bal, D-(X1,X2,X3,X4,X5)Phe 또는 D-(Et)Tyr이며;A6은 Arg 또는 hArg이며;A7은 Trp, 1-Nal, 2-Nal, Bal, Bip 또는 D-Trp이며;A8은 Gly, A5c, A6c, Ala, β-Ala, Gaba, Apn, Ahx 또는 Aha이거나, 삭제되며;A9는 Cys, D-Cys, hCys, D-hCys, Pen, D-Pen 또는 Lys이며;A10은 Pro 또는 Thr이거나, 삭제되며;A11은 Pro이거나, 삭제되며;A12는 Lys 또는 Arg이거나, 삭제되며;A13은 Asp이거나 또는 삭제되는 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 3항에 있어서, R2 및 R3은 각각 독립적으로 H 또는 아실인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 4항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2- Gln-(Arg)3-NH2;Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Aib-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala- (Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3- NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)2-Lys-(Arg)2-Gln- (Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln- (Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Gly-(Arg)5-Gln- (Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly- (Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln- (Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln- (Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln- (Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4- NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2; Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2; 또는Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2.
- 제 5항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5- Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Aib-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala--Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp--β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5- Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr- Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5- Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2 ;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln- (Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4- NH2; 또는Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2.
- 제 4항에 있어서,B1은 Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3; 또는 Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc이거나, 삭제되며;B2는 β-Ala; β-Ala-Gly; β-Ala-Tyr-Gly; (β-Ala)2; (β-Ala)2-Gly; (β-Ala)2-Tyr-Gly; Doc; Doc-Gly; Doc-Tyr-Gly; (Doc)2; (Doc)2-Gly; 또는 (Doc)2-Tyr-Gly이거나, 삭제되며;B3은 Arg-Lys-Gln-Lys-(Arg)5; Arg-Lys-(Arg)3-Gln-(Arg)3; Arg-(Lys)2-Gln-(Arg)5; Arg-(Lys)2-Arg-Gln-(Arg)4; Arg-(Lys)2-(Arg)2-Gln-(Arg)3; Arg-(Lys)2-(Arg)3-Gln-(Arg)2; Arg-(Lys)2-(Arg)4-Gln-Arg; Arg-(Lys)2-(Arg)5-Gln; (Arg)2-Lys-(Arg)2-Gln-(Arg)3; Arg-Gln-(Lys)2-(Arg)5; (Arg)5-Gln-(Arg)3; (Arg)5-Gln-(Arg)4; 또는 (Arg)6-Gln-(Arg)3이거나, 삭제되는 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 7항에 있어서,B2는 β-Ala; β-Ala-Gly; β-Ala-Tyr-Gly; Doc-Tyr-Gly; 또는 (Doc)2-Tyr-Gly이거나, 삭제되는 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 7항에 있어서,B3는 Arg-Lys-(Arg)3-Gln-(Arg)3; Arg-(Lys)2-Gln-(Arg)5; Arg-(Lys)2-Arg-Gln-(Arg)4; Arg-(Lys)2-(Arg)2-Gln-(Arg)3; Arg-(Lys)2-(Arg)3-Gln-(Arg)2; Arg-(Lys)2-(Arg)4-Gln-Arg; Arg-(Lys)2-(Arg)5-Gln; (Arg)2-Lys-(Arg)2-Gln-(Arg)3; Arg-Gln-(Lys)2-(Arg)5; (Arg)5-Gln-(Arg)3; (Arg)5-Gln-(Arg)4; 또는 (Arg)6-Gln-(Arg)3이거나, 삭제되는 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 7항에 있어서,A1 = Nle 또는 삭제되며;A2 = Cys이며;A3 = Glu 또는 D-Ala이며;A4 = His이며;A5 = D-Phe 또는 D-2-Nal이며;A6 = Arg이며;A7 = Trp, 1-Nal, 2-Nal 또는 Bal이며;A8 = Gly 또는 Ala이며;A9 = Cys이며;A10 = Pro이거나, 삭제되며;A12 = Lys 또는 Arg이거나, 삭제되는 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 10항에 있어서,A3 = Glu;A5 = D-2-Nal인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 10항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Aib-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala- (Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly- Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5- Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr- Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr- Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-Tyr-Gly-(Arg)6-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2; 또는Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-(Arg)5-Gln-(Arg)3- NH2.
- 제 11항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-Gln-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Gln-Lys-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)4-Gln-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Aib-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala- (Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Arg-Asp-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)6-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)3-Gln-(Arg)2-NH2 ;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-Gln-(Lys)2-(Arg)5-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)5-Gln-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Arg- Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2; 또는Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2.
- 제 13항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2; 또는Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2.
- 제 14항에 있어서, 하기 화합물인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2.
- 제 14항에 있어서, 하기 화합물인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2.
- 제 14항에 있어서, 하기 화합물인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2.
- 제 4항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2.
- 제 7항에 있어서,A1 = Nle, Phe, D-Phe, hPhe, Chg, D-Chg, hChg, Cha 또는 hCha이고;A2 = Cys 또는 Asp이고;A3 = D-Ala, D-Leu 또는 D-Cha이거나, 삭제되며;A5 = D-Phe 또는 D-(Et)-Tyr이고;A7 = Trp, Bal 또는 D-Trp이고;A8 = Ala, β-Ala, Gaba, Apn 또는 Ahx이거나, 삭제되며;A9 = Cys, D-Cys, Pen 또는 Lys이고;A10 = Thr이거나, 삭제되며;A11 = 삭제되며;A12 = 삭제되며;A13 = 삭제되며;단, A3 또는 A8 중 적어도 하나는 삭제되지만 둘다 삭제되진 않는 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 19항에 있어서,A1 = Nle이고;A2 = Cys이고;A3 = D-Ala이고;A5 = D-Phe이고;A7 = Trp이고;A8 = 삭제되고;A9 = Cys인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 19항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)2-Lys-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-(Arg)3-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2- Arg-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4- NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly- (Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln- (Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly- (Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc)2-(Arg)5-Gln- (Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln- (Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3- NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2; 또는Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2.
- 제 21항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys)2-Arg-Gln-(Arg)4-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2; 또는Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2.
- 제 19항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Arg-Lys-Arg- Arg-Gln-Arg-Arg-Arg-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-Arg-Arg-Arg-Gln-Arg-Arg-Arg-NH2.
- 제 7항에 있어서,A1 = Nle이고;A2 = Asp이고;A3 = 삭제되고;A5 = D-Phe 또는 D-2-Nal이고;A6 = Arg이고;A7 = Trp이고;A8 = 삭제되고;A9 = Lys이며;A10 = 삭제되고;A11 = 삭제되고;A12 = 삭제되고;A13 = 삭제되는 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 24항에 있어서,B1 = Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3; 또는 Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc이거나, 삭제되며;B3 = Arg-(Lys)2-(Arg)2-Gln-(Arg)3; (Arg)5-Gln-(Arg)3; 또는 (Arg)5-Gln-(Arg)4이거나, 삭제되는 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 25항에 있어서, A5 = D-2-Nal인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염.
- 제 24항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-Arg-(Lys)2- (Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala)2-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-(Arg)5-Gln-(Arg)4-NH2;Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-Gly-(Arg)5-Gln-(Arg)4-NH2; 또는Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc)2-(Arg)5-Gln-(Arg)4-NH2.
- 제 26항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2;Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys)2-(Arg)2- Gln-(Arg)3-NH2;H-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2;Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro)2-Lys-Asp-Doc-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2; 또는Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc)2-Tyr-Gly-Arg-(Lys)2-(Arg)2-Gln-(Arg)3-NH2.
- 식 (II)의 화합물 또는 약제학적으로 허용가능한 그의 염:식 (II):Ac-c(Cys-Glu-His-A1-Arg-A2-A3-Cys)-(Pro)2-Lys-Asp-NH2상기에서,A1은 D-이성체의 X-Phe 또는 2-Nal로 상기 X는 할로겐이고;A2는 Bal, 1-Nal, 2-Nal, 또는 Trp이고; 및A3은 Aib, Ala, β-Ala 또는 Gly이다.
- 제 29항에 있어서, 하기 화합물 중 어느 하나인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-4-Br-Phe-Arg-Trp-Gly-Cys)-(Pro)2-Lys-Asp-NH2 ;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro)2-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-β-Ala-Cys)-(Pro)2-Lys-Asp-NH2; 또는Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Aib-Cys)-(Pro)2-Lys-Asp-NH2.
- 제 30항에 있어서, 하기 화합물인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro)2-Lys-Asp-NH2.
- 제 30항에 있어서, 하기 화합물인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro)2-Lys-Asp-NH2.
- 제 30항에 있어서, 하기 화합물인 것을 특징으로 하는 화합물 또는 약제학적으로 허용가능한 그의 염:Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro)2-Lys-Asp-NH2.
- 약제학적으로 허용가능한 담체 또는 희석제와 함께, 제 1항 내지 제 33항중 어느 한항에 따른 화합물 또는 약제학적으로 허용가능한 그의 염을 치료학적 유효량으로 포함하는 약학 조성물.
- 제 34항에 있어서, 상기 화합물은 선택적인 멜라노코르틴-4 수용체 작용제 또는 약제학적으로 허용가능한 그의 염인 것을 특징으로 하는 약학 조성물.
- 제 35항에 있어서, 상기 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-1 수용체, 인간 멜라노코르틴-3 수용체 및 인간 멜라노코 르틴-5 수용체에 비하여 15배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진, 선택적인 멜라노코르틴-4 수용체 작용제 또는 약제학적으로 허용가능한 그의 염인 것을 특징으로 하는 약학 조성물.
- 제 36항에 있어서, 상기 멜라노코르틴-4 수용체의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비해 17배 이상 높은 것으로 EC50에 의해 특정화되는 것을 특징으로 하는 약학 조성물.
- 제 36항에 있어서, 상기 멜라노코르틴-4 수용체의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비해 90배 이상 높은 것으로 EC50에 의해 특정화되는 것을 특징으로 하는 약학 조성물.
- 제 36항에 있어서, 상기 멜라노코르틴-4 수용체의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-5 수용체에 비해 200배 이상 높은 것으로 EC50에 의해 특정화되는 것을 특징으로 하는 약학 조성물.
- 제 36항에 있어서, 상기 멜라노코르틴-4 수용체의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-5 수용체에 비해 3000배 이 상 높은 것으로 EC50에 의해 특정화되는 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 일반 염증, 염증성 장 질환, 뇌 염증, 패혈증 및 패혈증 쇼크로 이루어진 군으로부터 선택되는 급성 또는 만성 염증 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물
- 제 34항에 있어서, 류마티스 관절염, 통풍성 관절염 및 다발성 경화증으로 이루어진 군으로부터 선택되는, 자가면역성 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 비만, 섭식 장애 및 프레더 윌리 증후군으로 이루어진 군으로부터 선택되는, 체중 증가를 수반하는 대사 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 43항에 있어서, 비만이 치료되는 것을 특징으로 하는 약학 조성물.
- 제 43항에 있어서, 섭식 장애가 치료되는 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 음식물 섭취 감소에 유용한 것을 특징으로 하는 약학 조 성물.
- 제 34항에 있어서, 체중 감소에 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 음식물 섭취 감소 및 체중 감소에 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 식욕 부진, 다식증, AIDS성 소모증, 악액질, 암 악액질 및 허약 노인의 쇠약증으로 이루어진 군으로부터 선택되는, 체중 감소를 수반하는 대사 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 49항에 있어서, 악액질 치료에 유용한 것을 특징으로 하는 약학 조성물.
- 제 49항에 있어서, 다식증 치료에 유용한 것을 특징으로 하는 약학 조성물.
- 제 49항에 있어서, AIDS성 소모증 또는 허약 노인의 쇠약증 치료에 유용한 것을 특징으로 하는 약학 조성물.
- 제 49항에 있어서, 악액질 또는 암 악액질 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 음식물 섭취 증가에 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 체중 증가에 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 음식물 섭취 증가 및 체중 증가에 유용한 것을 특징으로 하는 약학 조성물.
- 제 54항에 있어서, 상기 화합물은 하기 화합물 군으로부터 선택되는 것을 특징으로 하는 음식물 섭취 증가에 유용한 약학 조성물:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는약제학적으로 허용가능한 그의 염.
- 제 55항에 있어서, 상기 화합물은 하기 화합물 군으로부터 선택되는 것을특징으로 하는 체중 증가에 유용한 약학 조성물:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는악제학적으로 허용가능한 그의 염.
- 제 56항에 있어서, 상기 화합물은 하기 화합물 군으로부터 선택되는 것을 특징으로 하는 음식물 증가 및 체중 증가에 유용한 약학 조성물:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는약제학적으로 허용가능한 그의 염.
- 제 34항에 있어서, 피부 암 및 암 악액질로 이루어진 군으로부터 선택되는, 신생물 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 자궁내막증, 자궁 출혈, 성 기능 장애, 발기 부전 및 여 성의 성 반응 감소로 이루어진 군으로부터 선택되는, 생식기 또는 성 관련 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 장기 이식 거부 반응, 허혈증 및 재관류 손상, 상처 및 척수 손상, 및 화학요법, 방사선요법, 일시 고정화, 영구 고정화 및 투석으로 이루어진 군으로부터 선택되는 의학 시술로 인한 체중 감소로 이루어진 군으로부터 선택되는, 유기체의 치료 또는 상해가 원인인 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 출혈성 쇼크, 심장 쇼크, 저혈량성 쇼크, 심혈관 장애 및 심장 악액질로 이루어진 군으로부터 선택되는, 심혈관 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 급성 호흡 곤란 증후군, 폐 섬유증, 만성 폐색성 폐 질환 및 천식으로 이루어진 군으로부터 선택되는, 폐 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 면역 관용 강화 및 알러지로 이루어진 군으로부터 선택되는, 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 건선, 피부 색소 형성 감소증, 여드름 및 켈로이드(keloid) 형성으로 이루어진 군으로부터 선택되는, 피부 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 불안, 우울증, 기억 장애 및 신경성 통증으로 이루어진 군으로부터 선택되는, 행동 체계, 중추 신경계 또는 신경 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 신장 악액질 및 나트륨뇨증으로 이루어진 군으로부터 선택되는, 신장 질환 또는 의학적 상태를 치료하는데 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 난소 무게, 태반 발생, 프로락틴 분비, FSH 분비, 자궁내 태아 성장, 출산, 정자 형성, 티록신 분비, 알도스테론 합성과 분비, 체온, 혈압, 심장 박동수, 혈관 긴장도, 뇌혈류, 혈당 수치, 피지 분비, 페로몬 분비, 동기 부여, 학습 및 행동, 통증 인지, 신경 보호 및 신경 성장 조절에 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 골 대사, 골 형성 및 골 발생 조절에 유용한 것을 특징으로 하는 약학 조성물.
- 제 34항에 있어서, 알코올 섭취 저해, 알코올 섭취 감소, 알코올 중독 치료 또는 알코올 남용 치료에 유용한 것을 특징으로 하는 약학 조성물.
- 제 71항에 있어서, 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취 저해에 유용한 약학 조성물.
- 제 71항에 있어서, 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취 감소에 유용한 약학 조성물.
- 제 71항에 있어서, 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 중독 치료에 유용한 약학 조성물.
- 제 71항에 있어서, 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 남용 치료에 유용한 약학 조성물.
- 제 72항에 있어서, 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-1 수용체, 인간 멜라노코르틴-3 수용체 및 인간 멜라노코르틴-5 수용체에 비하여 15배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취 저해에 유용한 약학 조성물.
- 제 76항에 있어서, 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비하여 17배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취 저해에 유용한 약학 조성물.
- 제 76항에 있어서, 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비하여 90배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취 저해에 유용한 약학 조성물.
- 제 76항에 있어서, 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-5 수용체에 비하여 200배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취 저해에 유용한 약학 조성물.
- 제 76항에 있어서, 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-5 수용체에 비하여 3000배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취 저해에 유용한 약학 조성물.
- 치료가 필요한 개체에서 알코올 섭취를 저해시키는데 유용한 약제 제조에 있어서의, 치료학적 유효량의, 제 1항 내지 제 33항중 어느 한항에 따른 멜라노코르틴-4 수용체 작용제 또는 약제학적으로 허용가능한 그의 염의 용도.
- 치료가 필요한 개체에서 알코올 섭취를 감소시키는데 유용한 약제 제조에 있어서의, 치료학적 유효량의, 제 1항 내지 제 33항중 어느 한항에 따른 멜라노코르틴-4 수용체 작용제 또는 약제학적으로 허용가능한 그의 염의 용도.
- 치료가 필요한 개체에서 알코올 중독을 치료하는데 유용한 약제 제조에 있어서의, 치료학적 유효량의, 제 1항 내지 제 33항중 어느 한항에 따른 멜라노코르틴-4 수용체 작용제 또는 약제학적으로 허용가능한 그의 염의 용도.
- 치료가 필요한 개체에서 알코올 남용을 치료하는데 유용한 약제 제조에 있어서의, 치료학적 유효량의, 제 1항 내지 제 33항중 어느 한항에 따른 멜라노코르틴-4 수용체 작용제 또는 약제학적으로 허용가능한 그의 염의 용도.
- 필요한 개체에게 제 1항 내지 제 33항중 어느 한항에 따른 멜라노코르틴-4 수용체 작용제 또는 약제학적으로 허용가능한 그의 염을 치료학적 유효량으로 투여하는 단계를 포함하는, 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하는 방법.
- 제 85항에 있어서, 상기 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 방법.
- 제 86항에 있어서, 상기 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-1 수용체, 인간 멜라노코르틴-3 수용체 및 인간 멜라노코르틴-5 수용체에 비하여 15배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 방법.
- 제 87항에 있어서, 멜라노코르틴-4 수용체 작용제의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비하여 17배 이상 높은 것으로 EC50에 의해 특정화된 것을 특징으로 하는 방법.
- 제 87항에 있어서, 멜라노코르틴-4 수용체 작용제의 기능적 활성은 인간 멜 라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비하여 90배 이상 높은 것으로 EC50에 의해 특정화된 것을 특징으로 하는 방법.
- 제 87항에 있어서, 멜라노코르틴-4 수용체 작용제의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-5 수용체에 비하여 200배 이상 높은 것으로 EC50에 의해 특정화된 것을 특징으로 하는 방법.
- 제 87항에 있어서, 멜라노코르틴-4 수용체 작용제의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-5 수용체에 비하여 3000배 이상 높은 것으로 EC50에 의해 특정화된 것을 특징으로 하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 일반 염증, 염증성 장 질환, 뇌 염증, 패혈증 및 패혈증 쇼크로 이루어진 군으로부터 선택되는 급성 또는 만성 염증 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 류마티스 관절염, 통풍성 관절염 및 다발성 경화증으로 이루어진 군으로부터 선택되는 자가면역성 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 비만, 섭식 장애 및 프레더 윌리 증후군으로 이루어진 군으로부터 선택되는 체중 증가를 수반하는 대사 질환 또는 의학적 상태를 치료하는 방법.
- 제 94항에 있어서, 비만이 치료되는 것을 특징으로 하는 방법.
- 제 94항에 있어서, 섭식 장애가 치료되는 것을 특징으로 하는 방법.
- 제 85항에 따라 음식물 섭취를 감소시키는 방법.
- 제 85항에 따라 체중을 감소시키는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 음식물 섭취와 체중을 감소시키는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 식욕 부진, 다식증, AIDS성 소모증, 악액질, 암 악액질 및 허약 노인의 쇠약증으로 이루어진 군으로부터 선택되는 체중 감소를 수반하는 대사 질환 또는 의학적 상태를 치료하는 방법.
- 제 100항에 있어서, 악액질이 치료되는 것을 특징으로 하는 방법.
- 제 100항에 있어서, 다식증이 치료되는 것을 특징으로 하는 방법.
- 제 100항에 있어서, AIDS성 소모증 또는 허약 노인의 쇠약증이 치료되는 것을 특징으로 하는 방법.
- 제 100항에 있어서, 악액질 또는 암 악액질이 치료되는 것을 특징으로 하는 방법.
- 제 85항에 따라 음식물 섭취를 증가시키는 방법.
- 제 85항에 따라 체중을 증가시키는 방법.
- 제 85항에 따라 음식물 섭취와 체중을 증가시키는 방법.
- 제 105항에 있어서, 상기 화합물은 하기 화합물 군으로부터 선택되는 것을 특징으로 하는 방법:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는약제학적으로 허용가능한 그의 염.
- 제 106항에 있어서, 상기 화합물은 하기 화합물 군으로부터 선택되는 것을 특징으로 하는 방법:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는약제학적으로 허용가능한 그의 염.
- 제 107항에 있어서, 상기 화합물은 하기 화합물 군으로부터 선택되는 것을 특징으로 하는 방법:Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-Pro-Pro-Lys-Asp-Doc-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-Pro-Pro-Lys-Asp-NH2;Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-Pro-Pro-Lys-Asp-β-Ala-Tyr-Gly-Arg-Arg-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2; 또는약제학적으로 허용가능한 그의 염.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 피부 암 및 암 악액질로 이루어진 군으로부터 선택되는 신생물 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 자궁내막증, 자궁 출혈, 성 기능 장애, 발기 부전 및 여성의 성 반응 감소로 이루어진 군으로부터 선택되는 생식기 또는 성 관련 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 장기 이식 거부 반응, 허혈증 및 재관류 손상, 상처 및 척수 손상, 및 화학요법, 방사선요법, 일시 고정화, 영구 고정화 및 투석으로 이루어진 군으로부터 선택되는 의학적 시술로 인한 체중 감소로 이루어진 군으로부터 선택되는 유기체의 치료 또는 상해가 원인인 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 출혈성 쇼크, 심장 쇼크, 저혈량성 쇼크, 심혈관 장애 및 심장 악액질로 이루어진 군으로부터 선택되는 심혈관 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 급성 호흡 곤란 증후군, 폐 섬유증, 만성 폐색성 폐 질환 및 천식으로 이루어진 군으로부터 선택되는 폐 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 면역 관용 강화 및 알러지로 이루어진 군으로부터 선택되는 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 건선, 피부 색소 형성 감소증, 여드름 및 켈로이드 형성으로 이루어진 군으로부터 선택되는 피부 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 불안, 우울증, 기억 장애 및 신경성 통증으로 이루어진 군으로부터 선택되는 행동 체계, 중추 신경계 또는 신경 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 신장 악액질 및 나트륨뇨증으로 이루어진 군으로부터 선택되는 신장 질환 또는 의학적 상태를 치료하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 난소 무게, 태반 발생, 프로락틴 분비, FSH 분비, 자궁내 태아 성장, 출산, 정자 형성, 티록신 분비, 알도스테론 합성과 분비, 체온, 혈압, 심장 박동수, 혈관 긴장도, 뇌혈류, 혈당 수치, 피지 분비, 페로몬 분비, 동기 부여, 학습 및 행동, 통증 인지, 신경 보호 및 신경 성장을 조절하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 골 대사, 골 형성 및 골 발생을 조절하는 방법.
- 제 85항에 따라 멜라노코르틴 수용체로부터 작용제 또는 길항제 작용을 도출하여, 알코올 섭취를 저해, 알코올 섭취를 감소, 알코올 중독을 치료 또는 알코올 남용을 치료하는 방법.
- 제 122항에 있어서, 상기 약학 조성물의 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취를 저해하는 방법.
- 제 122항에 있어서, 상기 약학 조성물의 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취를 감소시키는 방법.
- 제 122항에 있어서, 상기 약학 조성물의 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 중독을 치료하는 방법.
- 제 122항에 있어서, 상기 약학 조성물의 화합물은 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 남용을 치료하는 방법.
- 제 123항에 있어서, 상기 약학 조성물의 화합물은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-1 수용체, 인간 멜라노코르틴-3 수용체 및 인간 멜라노코르틴-5 수용체에 비하여 15배 이상 높은 것으로 EC50에 의해 특정화된 기능적 활성을 가진 선택적인 멜라노코르틴-4 수용체 작용제인 것을 특징으로 하는 알코올 섭취를 저해하는 방법.
- 제 127항에 있어서, 멜라노코르틴-4 수용체 작용제의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비하여 17배 이상 높은 것으로 EC50에 의해 특정화된 것을 특징으로 하는 방법.
- 제 127항에 있어서, 멜라노코르틴-4 수용체 작용제의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-3 수용체에 비하여 90배 이상 높은 것으로 EC50에 의해 특정화된 것을 특징으로 하는 방법.
- 제 127항에 있어서, 멜라노코르틴-4 수용체 작용제의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-5 수용체에 비하여 200배 이상 높은 것으로 EC50에 의해 특정화된 것을 특징으로 하는 방법.
- 제 127항에 있어서, 멜라노코르틴-4 수용체 작용제의 기능적 활성은 인간 멜라노코르틴-4 수용체에 대한 선택성이 인간 멜라노코르틴-5 수용체에 비하여 3000배 이상 높은 것으로 EC50에 의해 특정화된 것을 특징으로 하는 방법.
- 일반 염증, 염증성 장 질환, 뇌 염증, 패혈증, 패혈증 쇼크, 류마티스 관절염, 통풍성 관절염, 다발성 경화증, 체중 증가를 수반하는 대산 질환 또는 의학적 상태, 비만, 섭식 장애 및 프레더 윌리 증후군, 체중 감소를 수반하는 대사 질환 또는 의학적 상태, 식욕 부진, 다식증, AIDS성 소모증, 악액질, 암 악액질, 허약 노인의 쇠약증, 피부암, 자궁내막증, 자궁 출혈, 성 기능 장애, 발기 부전, 여성의 성 반응 감소, 장기 이식 거부 반응, 허혈증 및 재관류 손상, 상처 및 척수 손상, 화학요법, 방사선요법, 일시 고정화, 영구 고정화 또는 투석으로 이루어진 군으로부터 선택되는 의학적 시술로 인한 체중 감소, 출혈성 쇼크, 심장 쇼크, 저혈량성 쇼크, 심혈관 장애, 심장 악액질, 급성 호흡 곤란 증후군, 폐 섬유증, 만성 폐색성 폐 질환, 천식, 면역 관용 강화, 알러지, 건선, 피부 색소 형성 감소증, 여드름, 켈로이드 형성, 불안, 우울증, 기억 장애, 신경성 통증, 신장 악액질 및 나트륨뇨 증으로 이루어진 군으로부터 선택되는 질환 및/또는 의학적 상태 치료에 이용가능한 약제 제조에 있어서의, 제 1항 내지 제 33항중 어느 한항에 따른 치료학적 유효량의, 멜라노코르틴-4 수용체 작용제 또는 길항제 화합물, 또는 약제학적으로 허용가능한 그의 염의, 용도.
- 난소 무게, 태반 발생, 프로락틴 분비, FSH 분비, 자궁내 태아 성장, 출산, 정자 형성, 티록신 분비, 알도스테론 합성과 분비, 체온, 혈압, 심장 박동수, 혈관 긴장도, 뇌혈류, 혈당 수치, 피지 분비, 페로몬 분비, 동기 부여, 학습 및 행동, 통증 인지, 신경 보호, 신경 성장, 골 대사, 골 형성 및 골 발생과 같은 정상화 및 항상성 활성 조절에 유용한 약제 제조에 있어서의, 제 1항 내지 제 33항중 어느 한항에 따른 치료학적 유효량의, 멜라노코르틴-4 수용체 작용제 또는 길항제 화합물, 또는 약제학적으로 허용가능한 그의 염의, 용도.
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KR101726893B1 (ko) | 2009-06-08 | 2017-04-13 | 팔라틴 테크놀로지스 인코포레이티드 | 멜라노코르틴 수용체-특이적 펩티드 |
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RU2012108110A (ru) * | 2009-08-05 | 2013-09-10 | Ипсен Фарма С.А.С. | Применение меланокортинов для лечения дислипидемии |
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CN101921314B (zh) * | 2010-06-28 | 2012-11-21 | 华中科技大学 | 脑靶向防治老年性痴呆的神经营养因子融合多肽及制备方法 |
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RU2008104802A (ru) | 2009-08-20 |
US8349797B2 (en) | 2013-01-08 |
AU2006269321A1 (en) | 2007-01-18 |
IL188544A0 (en) | 2008-04-13 |
WO2007008684A3 (en) | 2009-05-07 |
WO2007008684A2 (en) | 2007-01-18 |
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