AU2008200694B2 - Method of treating acromegaly, hyperprolactinemia, portal hypertension and gastrointestinal bleeding with somatostatin-dopamine chimeric analogs - Google Patents

Method of treating acromegaly, hyperprolactinemia, portal hypertension and gastrointestinal bleeding with somatostatin-dopamine chimeric analogs Download PDF

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AU2008200694B2
AU2008200694B2 AU2008200694A AU2008200694A AU2008200694B2 AU 2008200694 B2 AU2008200694 B2 AU 2008200694B2 AU 2008200694 A AU2008200694 A AU 2008200694A AU 2008200694 A AU2008200694 A AU 2008200694A AU 2008200694 B2 AU2008200694 B2 AU 2008200694B2
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Michael Dewitt Culler
Zheng Xin Dong
Yeelana Shen
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Ipsen Pharma SAS
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Ipsen Pharma SAS
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GRIFFITH HACK PATENTS, TRADE MARKS, IP LAW SPECIFICATION OF PATENT APPLICATION COUNTRY AUSTRALIA TYPE Patent TITLE METHOD OF TREATING ACROMEGALY, HYPERPROLACTINEMIA, PORTAL HYPERTENSION AND GASTROINTESTINAL BLEEDING WITH SOMA TOSTA TIN DOPAMINE CHIMERIC ANALOGS APPLICANT SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES, S.A.S.
AUSTRALIA Patents Act 1990 COMPLETE SPECIFICATION Standard Patent Applicantss: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES, S.A.S. Invention Title: METHOD OF TREATING ACROMEGALY, HYPERPROLACTINEMIA, PORTAL HYPERTENSION AND GASTROINTESTINAL BLEEDING WITH SOMATOSTATIN DOPAMINE CHIMERIC ANALOGS The following statement is a full description of this invention, including the best method for performing it known to me/us: - 1 METHOD OF TREATING ACROMEGALY, HYPERPPROLACTINEMIA, PORTAL HYPERTENSION AND GASTROINTESTINAL BLEEDING WITH SOMATOSTATIN-DOPAMI NE CHIMERIC ANALOGS 5 Background of the Invention [0011 The present invention is drawn to somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use. [0021 Dopamine is a catecholamine neurotransmitter that has been implicated in the 10 pathogenesis of both Parkinson disease and schizophrenia. Dopamine and related molecules have been shown to inhibit the growth of several types of malignant tumors in mice, and this activity has been variously attributed to inhibition of tumor-cell proliferation, stimulation of tumor immunity or as well as effects on melanin metabolism in malignant melanomas. Recent studies demonstrated the presence of D2 15 dopamine receptors on endothelial cells. Dopamine has recently been reported to strongly and selectively inhibit at non-toxic levels the vascular permeabilizing and angiogenic activities of VPF/VEGF. [0031 Somatostatin (SS), a tetradecapeptide has been shown to have potent inhibitory effects on various secretory processes in tissues such as pituitary, pancreas 20 and gastrointestinal tract. SS also acts as a neuromodulator in the central nervous system. These biological effects of SS, all inhibitory in nature, are elicited through a series of G protein coupled receptors, of which five different subtypes have been characterized (SSTR-1 - SSTR-5). These five subtypes have similar affinities for endogenous SS ligands, but have differing distributions in various tissues. Somatostatin 25 binds to the five distinct receptor (SSTR) subtypes with relatively high and equal affinity for each subtype. [004] There is evidence that SS regulates cell proliferation by arresting cell growth via SSTR-1, -2, -3, -4, and -5 subtypes, and/or by inducing apoptosis via SSTR-3 subtype. SS and various analogues have been shown to inhibit normal and neoplastic 30 cell proliferation in vitro and in vivo via specific SS receptors (SSTR's) and possibly different postreceptor actions. In addition, there is evidence that distinct SSTR subtypes are expressed in normal and neoplastic human tissues, conferring different tissue H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 2 affinities for various SS analogues and variable clinical response to their therapeutic effects. [0051 Binding to different types of somatostatin receptor subtypes is associated with the treatment of various conditions and/or diseases. For example, the inhibition of 5 growth hormone has been attributed to the somatostatin type-2 receptor ("SSTR-2"), while the inhibition of insulin has been attributed to the somatostatin type-5 receptor ("SSTR-5"). Activation of types 2 and 5 have been associated with growth hormone suppression and more particularly growth hormone secreting adenomas (acromegaly) and thyroid stimulating hormone (TSH) secreting adenomas. Activation of type 5 but 10 not type 2 receptor has been associated with treating prolactin secreting adenomas. Other indications associated with activation of the somatostatin receptor subtypes include inhibition of insulin and/or glucagon for treating diabetes mellitus, angiopathy, proliferative retinopathy, dawn phenomenon, and nephropathy; inhibition of gastric acid secretion for treating peptic ulcers, enterocutaneous and pancreaticocutaneous fistula, 15 irritable bowel syndrome, Dumping syndrome, watery diarrhea syndrome, AIDS related diarrhea, chemotherapy-induced diarrhea, acute or chronic pancreatitis and gastrointestinal hormone secreting tumors; treatment of cancer such as hepatoma; inhibition of angiogenesis; treatment of inflammatory disorders such as arthritis; retinopathy; chronic allograft rejection; angioplasty; preventing graft vessel and 20 gastrointestinal bleeding. Preferably, a somatostatin analog is selective for the specific somatostatin receptor subtype or subtypes responsible for the desired biological response to reducing interaction with other receptor subtypes which could lead to undesirable side effects or loss of efficacy. [0061 Somatostatin and its receptors (SSTR- 1 to SSTR-5) are expressed in normal 25 human parafollicular C cells and medullary thyroid carcinoma (MTC). MTC is a tumor originating from thyroid parafollicular C cells that produces calcitonin (CT), somatostatin, and several other peptides. It was recently demonstrated that SS and SSTR's are expressed in human MTC, and SS and SS analogues were shown to induce a decrease in plasma CT levels and provide symptomatic improvement in MTC patients. 30 Another recent study has shown that SS and SS analogs, in particular, SSTR-l and SSTR-2, can inhibit the proliferation of tumor cells, suggesting that specific SSTR subtypes can function in MTC cell growth regulation. The development and H:\MaraR\Keep\SpeCi\P64463-div-SPECI.doc 7/02/06 -3 characterization of SSTR subtype analogues that selectively effect MTC cell growth is useful for clinical and therapeutic applications. Summary of the Invention 5 1007] The present invention is based on our discovery of somatostatin-dopamine chimeric analogs, comprising compounds that retain both somatostatin and dopamine activity. The chimeric analogs of the invention are considered to be useful, e.g., in vitro, for use as research tools, diagnostic assays, etc., or in vivo, for use as diagnostic or therapeutic agents. Preferred chimeric analogs of the invention display enhanced 10 activity when compared to native somatostatin and dopamine, either alone or in combination. [0081 Accordingly, in a first aspect, the invention features a chimeric analog comprising (1) at least one moiety which binds to one or more somatostatin receptor(s) and (2) at least one moiety which binds to one or more dopamine receptor(s), or a 15 pharmaceutically acceptable salt thereof. 10091 In a first embodiment of the first aspect, the chimeric analog comprises formula (I), Y- (L)m Z (W)" 20 N-R1 R3 H R2"" N R4 25 (I) wherein: [00101 X is H, Cl, Br, I, F, -CN, Ci-jo alkyl, C 1
.
10 heteroalkyl, C 2
-
10 alkenyl, C 2
-
1 0 alkynyl, substituted C 1
.
1 0 alkyl, substituted CI 10 heteroalkyl, substituted C 2
-
10 alkenyl, or substituted C 2
-
1 0 alkynyl; 30 [00111 RI is H, C 1
.
10 alkyl, C 1
.
10 heteroalkyl, C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted Cio 10 alkyl, substituted CI.
1 0 heteroalkyl, substituted C 2
-
10 alkenyl, substituted C 2
-
1 0 alkynyl, or -CN; H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 -4 [00121 R2 and R3, each is, independently, H or absent, provided that when R2 and R3 are absent a double bond is present between the carbon atoms to which they are attached; [0013] R4 is H, C 1
.
1 0 alkyl, CI.
1 0 heteroalkyl, C 2
.
10 alkenyl, C 2
-
10 alkynyl, substituted 5 CI- 10 alkyl, substituted C 1
-
1 0 heteroalkyl, substituted C 2
-
10 alkenyl, or substituted C 2
-
1 0 alkynyl; 100141 Y is -0-, -C(O)-, -S-, -S-(CH 2 )s-C(O)-, -S(O)-, -S(O) 2 -, -SC(O)-, -OC(O)-, N(R5)-C(O)-, or -N(R6)-; [00151 L is -(CH 2 )p-C(O)-, when Y is -S-, -S(O)-, -S(O) 2 -, -0- or -N(R6)-; or L is 10 C(O)-(CR7R8)-C(0)-, when Y is -N(R6)-, -0-, or -S-; or L is (amino acid), when Y is -C(0)-, SC(0)-, -OC(O)-, -S-(CH 2 )s-C(O)-, or -N(R5)-C(O)-; [00161 W is -CR9,R 10-; [00171 R5 and R6 each is, independently, H, CI.
1 0 alkyl, substituted C 1
.
1 o alkyl; C 1
.
10 heteroalkyl, substituted CI.
10 heteroalkyl, C 2
.
1 0 alkenyl, substituted C 2
.
1 o alkenyl, C 2
.
1 0 15 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted alkylaryl; [00181 R7, R8, R9, and RIO each is, independently, H, F, Cl, Br, I, C- 10 alkyl, substituted C 1
.
10 alkyl; CI.
1 0 heteroalkyl, substituted C 1 .i 0 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; or R7 and R8 can, optionally, join together to form a ring system; 20 or R9 and R10 can, optionally, join together to form a ring system; [00191 i is 2-10; [00201 m is 0 or 1; [00211 n is 0-10; 100221 p is 1-10; 25 [00231 q is 1-5; [0024] s is 1-10; [0025] t is 1-10; [00261 Z is a ligand of at least one somatostatin receptor; [00271 or a pharmaceutically acceptable salt thereof; and 2601322_1 (CHMattere) P58159.AU.3 22/03/11 -5 [00281 wherein each moiety depicted between the brackets is, independently for each occurrence, attached to an N-terminal or an internal amine group, carboxylic acid group or hydroxyl group of Z. 100291 In a second aspect of the first embodiment, the chimeric analog comprises 5 formula (II), 100301 ,R5 O W)--Y-(L, -Z N 0 -R1 R3 H R2" N R4 (II) wherein: 100301 X is H, Cl, Br, I, F, -CN, Ci.
1 o alkyl, C 1
.
10 heteroalkyl, C 2
-
10 alkenyl, C 2
-
10 10 alkynyl, substituted C 1
.
1 0 alkyl, substituted C 1
.
1 0 heteroalkyl, substituted C 2
-
10 alkenyl, or substituted C 2
.
1 0 alkynyl; 100311 RI is H, CI.
1 0 alkyl, CI.
10 heteroalkyl, C 2
-
1 0 alkenyl, C 2
-
1 0 alkynyl, substituted
C
1
.
1 0 alkyl, substituted C 1
.
10 heteroalkyl, substituted C 2
-
1 0 alkenyl, substituted C 2
-
10 alkynyl, or -CN; 15 100321 R2 and R3, each is, independently, H or absent, provided that when R2 and R3 are absent a double bond is present between the carbon atoms to which they are attached; [00331 R4 is H, C 1
.
10 alkyl, CI.
10 heteroalkyl, C 2
-
1 0 alkenyl, C 2
-
1 0 alkynyl, substituted Ci.
10 alkyl, substituted CI.
1 0 heteroalkyl, substituted C 2
-
1 0 alkenyl, or substituted C 2
-
1 0 20 alkynyl; [00341 R5 is H, Ci.io alkyl, CI.
1 0 heteroalkyl, C 2
-
1 0 alkenyl, C 2
-
10 alkynyl, substituted
CI.
10 alkyl, substituted C 1
.
1 0 heteroalkyl, substituted C 2
-
1 0 alkenyl, substituted C 2
-
1 0 alkynyl, or a group of the formula of -(CH 2 )rN(Rl 1,R12); H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 6 [00351 Y is -0-, -C(O)-, -S-, -SC(O)-, -OC(O)-, -N(R6)-C(O)-, -N(R7)-, or -N(R8) (CH2)-C(O-;' [0036] L is -(CH 2 )p-C(O)-, when Y is -S-, -0- or -N(R7)-; or L is -C(O)-(CR9R1O)q 5 C(O)-, when Y is -N(R7)-, -0-, or -S-; or L is (amino acid),, when Y is -C(0)-, SC(0)-, -OC(O)-, -N(R8)-(CH 2 )s-C(O)-, or -N(R6)-C(O)-; [0037] W is -CR9,R 10-; [0038] R6, R7, and R8 each is, independently, H, C 1
.
1 0 alkyl, substituted C 1
.
1 0 alkyl, Ci.
1 0 heteroalkyl, substituted C 1
.
10 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
10 alkenyl, 10 C 2
-
10 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; [0039] R9 and RIO each is, independently, H, Cl, Br, I, F, CI.
10 alkyl, substituted C 1 . io alkyl; CI.
10 heteroalkyl, substituted C 1
.
1 0 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; or R9 and R10 can, optionally, join together to form a ring system; 15 [0040] RI I and R12 each is, independently, H, CI.
1 0 alkyl, substituted CI.
1 0 alkyl;
CI.
1 0 heteroalkyl, substituted C 1
.
10 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
1 0 alkenyl,
C
2
-
10 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; [0041] i is 2-10; [0042] m is 0 or 1; 20 [0043] n is 2-10; [0044] p is 1-10; [0045] q is 1-5; [0046] r is 1-8 ; [0047] s is 1-10; 25 [0048] t is 1-10; [0049] v is 2-3; [0050] Z is a ligand of at least one somatostatin receptor; or [0051] a pharmaceutically acceptable salt thereof; and 2601322_1 (GHMatters) P58159.AU.3 22/03/11 -7 100521 wherein each moiety depicted between the brackets is, independently for each occurrence, attached to an N-terminal or an internal amine group, carboxylic acid group or hydroxyl group of Z. 10053] In a third embodiment of the first aspect, t he chimeric analog of claim 1, 5 wherein said chimeric analog comprises formula (III), R4-0 R1 RS-O / (W) --- Z L R2 (III) wherein: 100541 R2 is H, -N(R11)N(R12,RI 3), -N(R6R7), or -COOH; 100551 R4 and R5 each is, independently, H, C 1 .10 alkyl, substituted CI.
10 alkyl; Ci.
1 0 10 heteroalkyl, substituted C 1 .i 0 heteroalkyl, C 2
-
10 alkenyl, substituted C 2 .10 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, substituted akylaryl or R8-C(O)-; 100561 W is -CR9R10- or -(CH 2 )q-NH-(CH 2 )r-; 100571 RI, R6, R7, R8, RI 1, R12 and R13 each is, independently, H, C 1
.
1 0 alkyl, substituted C 1
.
1 0 alkyl; C 1
.
1 0 heteroalkyl, substituted C 1
.
1 0 heteroalkyl, C 2
-
10 alkenyl, 15 substituted C 2
-
10 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; 100581 R9 and RIO each is, independently, H, -OH, -CN, -NO 2 , F, Cl, Br, I, CI.
1 0 alkyl, substituted C.o 10 alkyl; C 1 .i 0 heteroalkyl, substituted CI.
10 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
.
10 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
1 0 alkynyl, akylaryl, 20 substituted alkylaryl, or aryl; 100591 X is C 1
.
10 alkyl, substituted CI.
10 alkyl; CI.
1 0 heteroalkyl, substituted C 1 .io heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
10 alkynyl, akylaryl, substituted alkylaryl, aryl, or acyl; 100601 Q is C or N; provided that when Q is N, then R2 is absent; 25 [00611 i is 1-10; 100621 n is 1-6; 10063] q is 1-6; [00641 r is 1-8; H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 8 [00651 Z is a ligand of at least one somatostatin receptor; or [00661 a pharmaceutically acceptable salt thereof; and [00671 wherein each moiety depicted between the brackets is, independently for each occurrence, attached to an N-terminal or an internal amine group or hydroxyl group of 5 Z. [00681 In a fourth embodiment of the first aspect, the chimeric analog comprises formula (IV), R2, z (W) I 0 N R3 R1 (IV) wherein: 10 [00691 RI and R2 each is, independently, H, CI.
10 alkyl, substituted C 1 .io alkyl; C 1
.
1 0 heteroalkyl, substituted C 1
.
1 0 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; [00701 R3, R4, R5, R6 and R7 each is, independently, H, -OH, -CN, -NO 2 , F, Cl, Br, I, Ci.
10 alkyl, substituted C 1 .i 0 alkyl; CI.
10 heteroalkyl, substituted Ci.
1 0 heteroalkyl, C 2 15 10 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; [00711 W is -CR4R5-; [00721 Y is -(CR6R7)m-C(O)- or acyl; [0073] m is 0-10; 20 [00741 n is 1-6; 100751 Z is a ligand of at least one somatostatin receptor; or [00761 a pharmaceutically acceptable salt thereof; and [00771 wherein each moiety depicted between the brackets is, independently for each occurrence, attached to an N-terminal or an internal amine group or hydroxyl group of 25 Z. H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 -9 [00781 In a fifth embodiment of the first aspect, the chimeric analog comprises formula (V), - R2 5p-- / (W ),- N, X R1 (V) wherein: [00791 P is -N(R3R4) or H; 10 100801 X is N or S; 100811 W is -CR5R6-; 10082] Y is -(CR7R8)m-C(O)-; 100831 RI, R3 and R4 each is, independently, H, C 1
.
1 0 alkyl, substituted Ci.
1 0 alkyl;
CI.
10 heteroalkyl, substituted C 1 .i 0 heteroalkyl, C 2 -1o alkenyl, substituted C 2
-
10 alkenyl, 15 C 2
-
1 0 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; 100841 R2, R5, R6, R7 and R8 each is, independently, H, -OH, -CN, -NO 2 , F, Cl, Br, I, C 1
.
10 alkyl, substituted Ci.
10 alkyl; C 1
.
1 0 heteroalkyl, substituted CI.
1 0 heteroalkyl, C 2 1o alkenyl, substituted C 2
-
10 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; 20 10085] i is 1-10; 100861 m is 0-10; 100871 n is 0-6; 100881 Z is a ligand of at least one somatostatin receptor; or [00891 a pharmaceutically acceptable salt thereof; and 25 100901 wherein each moiety depicted between the brackets is, independently for each occurrence, attached to an N-terminal or an internal amine group or hydroxyl group of Z. [00911 In a sixth aspect of the first embodiment, the chimeric analog comprises formula (VI), 30 Rl N -Y Z H K \ i o H:\MaraR\Keep\Speci\P64463-div-SPECIdoc 7/02/08 - 10 (VI) wherein: [00921 Y is -(CR2R3)m-C(O)- or acyl; 5 10093] RI is H, C 1
.
1 o alkyl, substituted Cl.
1 o alkyl; CI.
10 heteroalkyl, substituted CI.
1 0 heteroalkyl, C 2
.
10 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; 100941 R2 and R3 each is, independently, H, -OH, -CN, -NO 2 , F, Cl, Br, I, C 1
.
10 alkyl, substituted CI.
10 alkyl; CI.
10 heteroalkyl, substituted C 1
.
10 heteroalkyl, C 2
-
10 10 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; 100951 i is 1-10; 100961 m is 0-10; 100971 Z is a ligand of at least one somatostatin receptor; or 15 [00981 a pharmaceutically acceptable salt thereof; and 10099] wherein each moiety depicted between the brackets is, independently for each occurrence, attached to an N-terminal or an internal amine group or hydroxyl group of Z. [01001 In a seventh embodiment of the first aspect, the chimeric analog comprises 20 formula (VII), R1 P N-Y-L- Z R2 (VII) wherein: 101011 P is -N(R3R4) or H; [01021 L is -(CR5R6)m-C(O)- or acyl; 25 [0103] Y is Ci.io alkyl, substituted C 1
.
10 alkyl; CI.
10 heteroalkyl, substituted CI.
1 0 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, substituted akylaryl, or absent; 101041 RI, R2, R5 and R6 each is, independently, H, -OH, -CN, -NO 2 , F, Cl, Br, I,
C
1
.
1 0 alkyl, substituted CI.
10 alkyl; C 1
.
1 0 heteroalkyl, substituted C 1 .i 0 heteroalkyl, C 2
-
1 0 H:\MaraR\Keep\SpeCi\P64463-div-SPECI.doc 7/02/08 - 11 alkenyl, substituted C 2
.
1 0 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; 101051 R3 and R4 each is, independently, H, CI.
10 alkyl, substituted C 1 .io alkyl; Ci.io heteroalkyl, substituted C 1 .i 0 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
10 5 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; 101061 i is 1-10; [0107] m is 0-10; [01081 Z is a ligand of at least one somatostatin receptor; or [01091 a pharmaceutically acceptable salt thereof; and 10 [01101 wherein each moiety depicted between the brackets is, independently for each occurrence, attached to an N-terminal or an internal amine group or hydroxyl group of Z. [0111] In an eighth embodiment of the first aspect, the chimeric analog comprises formula (VIII), 15 R2 R3 R4 N 20 (VIII) wherein: [01121 X and Y each is, independently, -OH, -OR4 or R5-C(O)-O-; [01131 L is -(CR3R4)m-C(O)- or acyl; 101141 RI, R2, R3 and R4 each is, independently, H, -OH, F, Cl, Br, I, -CN, NO 2 , 25 CI.
10 alkyl, substituted Ci.
1 0 alkyl; Ci.
10 heteroalkyl, substituted C 1
.
10 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; or R2 and R3 can, optionally, join together to form a ring system; 101151 R5 is H, C 1
.
1 o alkyl, substituted Ci.
1 0 alkyl; C 1
.
1 0 heteroalkyl, substituted C 1
.
10 30 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
10 alkenyl, C 2
.
1 0 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; [01161 i is 1-10; H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 12 [01171 m is 0-10; [01181 Z is a ligand of at least one somatostatin receptor; or 10119] a pharmaceutically acceptable salt thereof; and wherein each moiety depicted between the brackets is, independently for each 5 occurrence, attached to an N-terminal or an internal amine group or hydroxyl group of Z. [01201 In a ninth embodiment of the first aspect, the chimeric analog comprises formula (IX), R3 10 R4 N. 0- z R2 R1 (IX) 15 wherein: [01211 X and Y each is, independently, -OH, -OR4 or R7-C(O)-; [01221 Q is -(CR5R6)m-C(O)- or acyl; [01231 RI, R2, R3, R4, R5 and R6 each is, independently, H, -OH, F, Cl, Br, I, -CN,
NO
2 , CI.
1 0 alkyl, substituted C 1
.
1 0 alkyl; C 1
.
10 heteroalkyl, substituted C 1
.
1 0 heteroalkyl, 20 C 2
-
1 0 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; or RI and R2 can, optionally, join together to form a ring system; or R3 and R4 can, optionally, join together to form a ring system; 101241 R7 is H, CI.
10 alkyl, substituted Ci.
1 0 alkyl; C 1
.
10 heteroalkyl, substituted CI.
10 heteroalkyl, C 2
.
1 0 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
.
10 alkynyl, substituted C 2
-
10 25 alkynyl, aryl, alkylaryl, or substituted akylaryl; [01251 i is 1-10; [01261 m is 0-10; [01271 Z is a ligand of at least one somatostatin receptor; or [01281 a pharmaceutically acceptable salt thereof; and 30 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 13 [01291 wherein each moiety depicted between the brackets is, independently for each occurrence, attached to an N-terminal or an internal amine group or hydroxyl group of Z. [01301 In a tenth embodiment of the first aspect, the chimeric analog comprises 5 formula (X), R5 N y R6 R3 R7 R2 R1 R4 10 -i (X) wherein: [01311 Y is -(CR8R9)m-C(O)- or acyl; [01321 RI, R2, R3, R4, R5, R6, R7, R8 and R9 each is, independently, H, -OH, F, 15 Cl, Br, I, -CN, NO 2 , C 1
.
1 0 alkyl, substituted C 1 o 10 alkyl; C 1
.
10 heteroalkyl, substituted Cl. io heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; 101331 i is 1-10; [01341 m is 0-10; 20 [01351 Z is a ligand of at least one somatostatin receptor; or [01361 a pharmaceutically acceptable salt thereof; and [01371 wherein each moiety depicted between the brackets is, independently for each occurrence, attached to an N-terminal or an internal amine group or hydroxyl group of Z. 25 101381 In another embodiment of the first aspect, the chimeric analog comprises any of the compounds listed in Table 1; or a pharmaceutically acceptable salt thereof. [01391 In another embodiment of the first aspect, the chimeric analog comprises a compound according to the formula of: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 26013221 (GHMatters) 14/03/11 - 14 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or 15 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 101401 In a preferred embodiment of the first aspect, the chimeric analog comprises a compound according to the formula of: Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, 20 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , a pharmaceutically acceptable salt thereof. [01411 In a more preferred embodiment of the first aspect, the chimeric analog comprises a compound according to the formula of Dop2-Lys(Dop2)-DTyr-DTyr cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2; or a pharmaceutically acceptable salt 25 thereof. In another more preferred embodiment, the chimeric analog comprises a compound according to the formula of Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys Abu-Cys]-Thr-NH2; or a pharmaceutically acceptable salt thereof. 2601322_1 (GHMatters) 14/03/11 - 15 [01421 In another embodiment of the first aspect, the chimeric analog comprises a compound according to the formula of: Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], 5 or a pharmaceutically acceptable salt thereof [01431 In a second aspect, the invention features a compound useful as an intermediate in a chemical synthesis, wherein said intermediate comprises a compound according to formula (3), (6), (11), (14), (18), (21), (24), or (27) (referred to herein as 10 intermediate compound (3), (6), (11), (14), (18), (21), (24), and (27), respectively) as shown below: [0144] O 0 N HOH OH; 3Y 0 15 HN 6 OH 0 2601322 _1 (GHMlatterg) 14/03/11 - 16 Nl'- OH 0 HO 14 0 OH N CI 0O 0 18 0 N~la JOH HN-- "%N 4\ s
H
0 21 -K1 OH N O< 5 -A 24 ;or H\MaraR\Keep\Speci\P64461-div-SPECI .doc 7/02/08 - 17 H2, 0"H 0 H 27 5 or an organic or inorganic salt thereof. 101441 In a third aspect, the invention features a method of eliciting a dopamine receptor agonist effect in a subject in need thereof, wherein said method comprises administering to said subject an effective amount of a chimeric analog of the invention, wherein said chimeric analogue comprises a compound according to the formula of 10 Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X), or a pharmaceutically acceptable salt thereof; or intermediate compound (3), (6), (11), (14), (18), (21), (24), or (27), or an organic or inorganic salt thereof; and wherein said effective amount is the amount effective to elicit a dopamine receptor agonist effect in said subject. 101451 In a first embodiment of the third aspect, the chimeric analog comprises any 15 of the compounds listed in Table 1; or a pharmaceutically acceptable salt thereof. [01461 In a second embodiment of the third aspect, the chimeric analog comprises a compound according to the formula of: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 2601322_1 (GHMatters) 14/03/11 - 18 Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or 10 a pharmaceutically acceptable salt thereof. [0147] In a preferred embodiment, the chimeric analog comprises a compound according to the formula of: Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , or 15 a pharmaceutically acceptable salt thereof. [01481 In a more preferred embodiment of the third aspect, the chimeric analog comprises a compound according to the formula of Dop2-Lys(Dop2)-DTyr-DTyr cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2; or a pharmaceutically acceptable salt thereof. 20 [0149] In another more preferred embodiment of the third aspect, chimeric analogue comprises a compound according to the formula of Dop2-DLys(Dop2)-cyclo[Cys-Tyr DTrp-Lys-Abu-Cys]-Thr-NH2; or a pharmaceutically acceptable salt thereof. In a third embodiment of the third aspect, the chimeric analogue comprises a compound according to the formula of: 25 Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or a pharmaceutically acceptable salt thereof. 2601322_1 (GHMatters) 14/03/11 - 19 [01501 In a fourth aspect, the invention features a method of eliciting a somatostatin receptor agonist effect in a subject in need thereof, wherein said method comprises administering to said subject an effective amount of a chimeric analogue of the 5 invention, wherein said chimeric analogue comprises a compound according to the formula of Formula (I), (II), (Il1), (IV), (V), (VI) (VII), (VIII), (IX), or (X), or a pharmaceutically acceptable salt thereof; or intermediate compound (3), (6), (11), (14), (18), (21), (24), or (27), or an organic or inorganic salt thereof; and wherein said effective amount is the amount effective to elicit a somatostatin receptor agonist effect 10 in said subject. [01511 In a first embodiment of the fourth aspect, the chimeric analogue comprises any of the compounds listed in Table 1; or a pharmaceutically acceptable salt thereof. [01521 In a second embodiment of the fourth aspect, the chimeric analogue comprises a compound according to the formula of: 15 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 25 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 26013221 (GHMatters) 14/03/11 - 20 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or 5 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. [01531 In a preferred embodiment, the chimeric analogue comprises a compound according to the formula of: Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, 10 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 , or a pharmaceutically acceptable salt thereof. [0154] In a more preferred embodiment of the fourth aspect, the chimeric analog comprises a compound according to the formula of Dop2-Lys(Dop2)-DTyr-DTyr cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2; or a pharmaceutically acceptable salt 15 thereof. In another more preferred embodiment of the fourth aspect, chimeric analogue comprises a compound according to the formula of Dop2-DLys(Dop2)-cyclo[Cys-Tyr DTrp-Lys-Abu-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 101551 In a third embodiment of the fourth aspect, the chimeric analogue comprises a compound according to the formula of: 20 Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or a pharmaceutically acceptable salt thereof. [01561 In a fifth aspect, the invention features a method of eliciting both a dopamine receptor agonist effect and a somatostatin receptor agonist effect in a subject in need 25 thereof, wherein said method comprises administering to said subject an effective amount of a chimeric analogue of the invention, wherein said chimeric analogue comprises a compound according to the formula of Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X), or a pharmaceutically acceptable salt thereof; or 2601322_1 (GHMatters) 14/03/11 - 21 intermediate compound (3), (6), (11), (14), (18), (21), (24), or (27), or an organic or inorganic salt thereof; and wherein said effective amount is the amount effective to 5 elicit both a dopamine and a somatostatin receptor agonist effect in said subject. 101571 In a first embodiment of the fifth aspect, the chimeric analogue comprises any of the compounds listed in Table 1; or a pharmaceutically acceptable salt thereof. [01581 In a second embodiment of the fifth aspect, the chimeric analogue comprises a compound according to the formula of: 10 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 20 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or 25 a pharmaceutically acceptable salt thereof. [01591 In a preferred embodiment, the chimeric analogue comprises a compound according to the formula of: Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 2601322_1 (GHMatters) 14/03/11 - 22 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , or a pharmaceutically acceptable salt thereof. 5 101601 In a more preferred embodiment of the fifth aspect, the chimeric analog comprises a compound according to the formula of Dop2-Lys(Dop2)-DTyr-DTyr cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. In another more preferred embodiment of the fifth aspect, chimeric analogue comprises a compound according to the formula of Dop2-DLys(Dop2)-cyclo[Cys-Tyr 10 DTrp-Lys-Abu-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 101611 In a third embodiment of the fifth aspect, the chimeric analogue comprises a compound according to the formula of: Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or 15 a pharmaceutically acceptable salt thereof. [01621 In a sixth aspect, the invention features a pharmaceutical composition comprising an effective amount of a compound according to the formula of Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X), or a pharmaceutically acceptable salt thereof; or intermediate compound (3), (6), (11), (14), (18), (21), (24), or (27), or an 20 organic or inorganic salt thereof; in a pharmaceutically acceptable carrier, wherein said effective amount is the amount effective to elicit a dopamine receptor agonist effect or a somatostatin receptor agonist effect or both in a subject in need thereof. [01631 In a first embodiment of the sixth aspect, the chimeric analogue comprises any of the compounds listed in Table 1; or a pharmaceutically acceptable salt thereof. 25 [01641 In a second embodiment of the sixth aspect, the chimeric analogue comprises a compound according to the formula of: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 2601322_1 (GHMatters) 14/03/11 - 23 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop2-DPhe-cyclo[Cys-3lTyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or 15 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. [0165] In a preferred embodiment, the chimeric analogue comprises a compound according to the formula of: 20 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , or a pharmaceutically acceptable salt thereof. [01661 In a more preferred embodiment of the sixth aspect, the chimeric analog comprises a compound according to the formula of Dop2-Lys(Dop2)-DTyr-DTyr 25 cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. In another more preferred embodiment of the sixth aspect, chimeric analogue comprises a compound according to the formula of Dop2-DLys(Dop2)-cyclo[Cys-Tyr DTrp-Lys-Abu-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 2601322_1 (GHMatters) 14/03/11 - 24 [01671 In a third embodiment of the sixth aspect, the chimeric analogue comprises a compound according to the formula of: 5 Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or a pharmaceutically acceptable salt thereof. 101681 In a seventh aspect, the invention features a method of treating a disease or 10 condition in a subject, said method comprising administering to said subject a therapeutically effective amount of a chimeric analog, wherein said chimeric analog comprises a compound according to the formula of Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X); any of the compounds listed in Table 1; 15 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 26013221 (GHMatters) 14/03/11 - 25 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or a pharmaceutically acceptable salt thereof; or intermediate compound (3), (6), (11), (14), (18), (21), (24), or (27); or an organic or inorganic salt thereof; and wherein said 10 disease or disorder is selected from the list consisting of a neuroendocrine tumor; a vascular disease; a connective tissue disease; an immune disease; a disorder of the gastrointestinal tract, pancreas, kidney, or liver; a metabolic disease; a cachexia; cancer or a tumor of the lung, breast, prostate, liver, thyroid, blood; a musculoskeletal disorder;a panic disorder; and opioid overdose; and wherein said therapeutically 15 effective amount is the amount effective to treat said disease or disorder in said patient. [01691 In a first embodiment of the seventh aspect, the neuroendocrine tumor is a neuroendocrine tumor of the pituitary. In a first preferred embodiment, the neuroendocrine tumor of the pituitary is an ACTH-producing tumor. Preferably, the ACTH-producing tumor is Cushing's disease. In a second preferred embodiment, the 20 neuroendocrine tumor of the pituitary is a growth hormone producing tumor. Preferably, the growth hormone producing tumor is acromegaly. In a third preferred embodiment, the neuroendocrine tumor of the pituitary is a prolactin-producing tumor. Preferably, the prolactin-producing tumor is a prolactinoma. In a fourth preferred embodiment, the neuroendocrine tumor of the pituitary is hyperprolactinemia or 25 prolactinemia. In a fifth preferred embodiment, the neuroendocrine tumor of the pituitary is thyroid stimulating hormone (TSH) secreting tumor. In a sixth preferred embodiment, the neuroendocrine tumor of the pituitary is "nonfunctioning" pituitary adenoma. In a seventh preferred embodiment, the neuroendocrine tumor of the pituitary is gonadotropinoma. 30 [01701 In a second embodiment of the seventh aspect, the neuroendocrine tumor is carcinoid tumor. In a preferred embodiment, the carcinoid tumor causes carcinoid 2601322_1 (GHMatters) 14/03/11 - 26 syndrome. In a third embodiment of the seventh aspect, the neuroendocrine tumor is glucagonoma. In a fourth embodiment of the seventh aspect, the neuroendocrine tumor is small cell lung carcinoma. In a fifth embodiment of the seventh aspect, the neuroendocrine tumor is thyroid medullary carcinoma. In a sixth embodiment of the 5 seventh aspect, the neuroendocrine tumor is VIPoma. In a seventh embodiment of the seventh aspect, the neuroendocrine tumor is insulinoma. In an eighth embodiment of the seventh aspect, the disorder of said vascular disease is inappropriate angiogenesis. In a ninth embodiment of the seventh aspect, the disorder of said vascular disease is restenosis. In a tenth embodiment of the seventh aspect, the disorder of said vascular 10 disease is retinopathy. In a preferred embodiment, the retinopathy is diabetic retinopathy or proliferative retinopathy. In another preferred embodiment, the retinopathy is macular degeneration, preferably, age-related macular degeneration. 101711 In another embodiment of the seventh aspect, the connective tissue disease is scleroderma. In yet another embodiment of the seventh aspect, the immune disease is 15 rheumatoid arthritis. In yet another embodiment of the seventh aspect, the immune disease is inflammation. In yet another embodiment of the seventh aspect, the immune disease is fibrosis. In yet another embodiment of the seventh aspect, the immune disease is Graves' opthalmopathy. In yet another embodiment of the seventh aspect, the immune disease is allograft rejection. In yet another embodiment of the seventh aspect, 20 the disorder of the gastrointestinal tract comprises gastric acid secretion, peptic ulcers, inflammatory bowel disease (IBD), or diarrhea. In a preferred embodiment, the IBD is irritable bowel syndrome or Crohn's disease. In another preferred embodiment, the diarrhea is AIDS related or chemotherapy related or watery diarrhea syndrome. In yet another preferred embodiment, the disorder of the gastrointestinal tract is small bowel 25 syndrome, small bowel obstruction, gastroesophageal reflux, duodenogastric reflux, H. pylori proliferation, or gastrointestinal bleeding. [01721 In yet another embodiment of the seventh aspect, the metabolic disease comprises hyperlipidemia, insulin resistance, Syndrome X, obesity, diabetes, or a diabetes-related disease. In a preferred embodiment, the diabetes-related disease 30 comprises diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, or gastroparesis. H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 27 [01731 In yet another embodiment of the seventh aspect, the cachexia is cardiac cachexia, cancer cachexia, or geriatric cachexia. [01741 In yet another embodiment of the seventh aspect, the disease or disorder comprises glioma, anorexia, hypothyroidism, Graves' disease, hyperaldeosteronism, 5 systemic sclerosis, pancreatitis, external and internal pancreatic pseudocysts and ascites, pancreaticocutaneous fistula, nesidoblastosis, hyperinsulinism, gastrinoma, Zollinger Ellison Syndrome, gastrointestinal hormone secreting tumor, dawn phenomenon, dumping syndrome, hyperparathyroidism, Paget's disease, polycystic ovary disease, orthostatic hypotension, postprandial hypotension, portal hypertension, angiopathy, or 10 graft vessel bleeding. [0175] In a first related embodiment of the aspect of the invention disclosed above, the chimeric analog comprises a SSTR- 1 agonist and a dopamine receptor agonist; or a pharmaceutically acceptable salt thereof. In a first preferred embodiment, the chimeric analog further comprises a SSTR-2 agonist or a SSTR-3 agonist, or a pharamaceutically 15 acceptable salt thereof, or both. [01761 In a second preferred embodiment, the chimeric analog further comprises a SSTR-5 agonist, or a pharmaceutically acceptable salt thereof. In a third preferred embodiment, the chimeric analog further comprises a SSTR-2 agonist or a SSTR-3 agonist, or a pharmaceutically acceptable salt thereof. 20 [01771 In a more preferred embodiment, the chimeric analog comprises a SSTR-1 agonist and a dopamine receptor agonist and further comprises a SSTR-2 agonist, a SSTR-3 agonist, and a SSTR-5 agonist, or a pharmaceutically acceptable salt thereof. [01781 In a second related embodiment of the aspect of the invention disclosed above, the chimeric analog comprises a SSTR-2 agonist and a dopamine receptor 25 agonist; or a pharmaceutically acceptable salt thereof. In a preferred embodiment, the chimeric analog further comprises a SSTR-5 agonist, or a pharmaceutically acceptable salt thereof. [01791 In a third related embodiment of the aspect of the invention disclosed above, the chimeric analog comprises a SSTR-3 agonist and a dopamine receptor agonist; or a 30 pharmaceutically acceptable salt thereof. H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 28 [0180] In a fourth related embodiment of the aspect of the invention disclosed above, the chimeric analog comprises a SSTR-5 agonist and a dopamine receptor agonist; or a pharmaceutically acceptable salt thereof. [01811 In an eighth aspect, the invention features a method of treating acromegaly in 5 a subject in need thereof, wherein said method comprises administering to said subject a therapeutically effective amount of a chimeric analog, wherein said chimeric analog comprises a compound according to the formula of Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X); any of the compounds listed in Table 1; Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or 26013221 (GHMatters) 14/03/11 - 29 a pharmaceutically acceptable salt thereof; or intermediate compound (3), (6), (11), (14), (18), (21), (24), or (27); or an organic or inorganic salt thereof; and the therapeutically effective amount is the amount effective to treat acromegaly in said 5 patient. In a preferred embodiment of this aspect of the invention, the chimeric analog comprises a SSTR-5 agonist and a dopamine receptor agonist. More preferably, the chimeric analog further comprises a SSTR-2 agonist. [01821 In another preferred embodiment of this aspect, the subject has developed or is at risk of developing acromegaly. 10 [01831 In a ninth aspect, the invention features a method of treating prolactinemia in a subject in need thereof, wherein said method comprises administering to said subject a therapeutically effective amount of a chimeric analog, wherein said chimeric analog comprises a compound according to the formula of Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X); any of the compounds listed in Table 1; 15 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 25 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 26013221 (GHMatters) 14/03/11 - 30 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or 5 a pharmaceutically acceptable salt thereof; or intermediate compound (3), (6), (11), (14), (18), (21), (24), or (27); or an organic or inorganic salt thereof; and the therapeutically effective amount is the amount effective to treat prolactinemia in said patient. In a preferred embodiment of this aspect of the invention, the chimeric analog comprises a SSTR-5 agonist and a dopamine receptor agonist. More preferably, the 10 chimeric analog further comprises a SSTR-2 agonist. 101841 In another preferred embodiment of this aspect, the subject has developed or is at risk of developing prolactinemia. [01851 In some embodiments, compounds of the invention may include the structure of DopA-Lys(DopA), wherein Lys is L-lysine, unless expressly designated as DLys. A 15 is 1-13, for example, Dop1, Dop2, Dop3, Dop4, Dop5, Dop6, Dop7, Dop8, Dop9, Dop10, Dop 11, Dop12, and Dopl3. The structure of a DopA-Lys(DopA), in which A is 2 (i.e., Dop2-Lys(Dop2)), and in which A is 5 (i.e., Dop5-Lys(Dop5)), are shown below. [01861 By "Dop 1" is meant a compound having the structure of: 0 H N H 20 [01871 By "Dop2" is meant a compound having the structure of: H 25 0 H N H 2601322_1 (GH~attere) 14/03/11 - 31 10188] By "Dop3" is meant a compound having the structure of: NH 5 O =< N ^ H N I 0 0 H 10 [01891 By "Dop4" is meant a compound having the structure of: NH H N N '0 15 H [01901 By "Dop5" is meant a compound having the structure of: 20 OH OH
H
2 N 0 101911 By "Dop6" is meant a compound having the structure of: 25 N 0 N =0 N 30 H 101921 By "Dop7" is meant a compound having the structure of: H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 32 S/ 5H [0193] By "Dop8" is meant a compound having the structure of: H 10 [01941 By "Dop9" is meant a compound having the structure of: 15
H
2 N-</N]C N S/ 0 [01951 By "Dop10" is meant a compound having the structure of: 20 OH HO N H 0 25 101961 By "DopI 1" is meant a compound having the structure of: OH N 30 H 101971 By "Dop 12" is meant a compound having the structure of: H:\MaraR\Keep\peci\P64463-div-SPECI.doc 7/02/08 - 33 o 0 HO N I H 5 101981 By "Dop13" is meant a compound having the structure of: A 0 N ci 10 HO OH OH 101991 Lys(Dop2) has the structure of: 15 0 HN NH NH NN -N' 20 H 102001 Dop2-Lys(Dop2) has the structure of: 0 N HH HN H 0 O 30 [02011 Lys(Dop5) has the structure of: H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 34 0 L< QN N o - N H 0 [02021 Dop5-Lys(Dop5) has the structure of: 0 0 N o - N -H H 0 5 102031 By "Alkyl" is meant a hydrocarbon group containing one or more carbon atoms, where multiple carbon atoms if present are joined by single bonds. The alkyl hydrocarbon group may be straight-chain or contain one or more branches or cyclic groups. [02041 By "Substituted alkyl" is meant an alkyl wherein one or more hydrogen 10 atoms of the hydrocarbon group are replaced with one or more substituents selected from the group consisting of halogen (i.e., fluorine, chlorine, bromine, and iodine), -OH, -CN, -SH, -NH 2 , -NHCH 3 , -NO 2 , -CI- 2 alkyl substituted with 1 to 5 halogens,
-CF
3 , -OCH 3 , -OCF 3 , and -(CH 2 )o0-COOH. In different embodiments 1, 2, 3 or 4 substituents are present. The presence of -(CH 2 )oA-COOH results in the production of H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 35 an alkyl acid. Examples of alkyl acids containing, or consisting of, -(CH 2 )o-COOH include 2-norbornane acetic acid, tert-butyric acid and 3-cyclopentyl propionic acid. 102051 By "Heteroalkyl" is meant an alkyl wherein one of more of the carbon atoms in the hydrocarbon group are replaced with one or more of the following groups: amino, 5 amido, -0-, or carbonyl. In different embodiments 1 or 2 heteroatoms are present. 102061 By "Substituted heteroalkyl" is meant a heteroalkyl wherein one or more hydrogen atoms of the hydrocarbon group are replaced with one or more substituents selected from the group consisting of halogen, (i.e., fluorine, chlorine, bromine, and iodine), -OH, -CN, -SH, -NH 2 , -NHCH 3 , -NO 2 , -C 1
.
2 alkyl substituted with 1 to 5 10 halogens, -CF 3 , -OCH 3 , -OCF 3 , and -(CH2)o-COOH. In different embodiments 1, 2, 3 or 4 substituents are present. [02071 By "Alkenyl" is meant a hydrocarbon group made up of two or more carbons where one or more carbon-carbon double bonds are present. The alkenyl hydrocarbon group may be straight-chain or contain one or more branches or cyclic groups. 15 102081 "Substituted alkenyl" refers to an alkenyl where one or more hydrogens are replaced with one or more substituents selected from the group consisting of halogen (i.e., fluorine, chlorine, bromine, and iodine), -OH, -CN, -SH, -NH 2 , -NHCH 3 , -NO 2 ,
-CI-
2 alkyl substituted with 1 to 5 halogens, -CF 3 , -OCH 3 , -OCF 3 , and -(CH 2 )o0-COOH. In different embodiments 1, 2, 3 or 4 substituents are present. 20 [02091 By "Alkynyl" is meant to a hydrocarbon group made up of two or more carbons where one or more carbon-carbon triple bonds are present. The alkynyl hydrocarbon group may be straight-chain or contain one or more branches or cyclic groups. [0210] By "Substituted alkynyl" is meant an alkynyl where one or more hydrogens 25 are replaced with one or more substituents selected from the group consisting of a halogen (i.e., fluorine, chlorine, bromine, and iodine), -OH, -CN, -SH, -NH 2 , -NHCH 3 ,
-NO
2 , -C1-2 alkyl substituted with 1 to 5 halogens, -CF 3 , -OCH 3 , -OCF 3 , and
-(CH
2 )o0-COOH. In different embodiments 1, 2, 3 or 4 substituents are present. [02111 By "Aryl" is meant an optionally substituted aromatic group with at least one 30 ring having a conjugated pi-electron system, containing up to two conjugated or fused ring systems. Aryl includes carbocyclic aryl, heterocyclic aryl and biaryl groups. Preferably, the aryl is a 5 or 6 membered ring. Preferred atoms for a heterocyclic aryl H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 36 are one or more sulfur, oxygen, and/or nitrogen. Examples of aryl include phenyl, I-naphthyl, 2-naphthyl, indole, quinoline, 2-imidazole, and 9-anthracene. Aryl substituents are selected from the group consisting of -CI4 alkyl, -C 1 4 alkoxy, halogen (i.e., fluorine, chlorine, bromine, and iodine), -OH, -CN, -SH, -NH 2 , -NO 2 , -Ci- 2 alkyl 5 substituted with 1 to 5 halogens, -CF 3 , -OCF 3 , and -(CH 2 )o4-COOH. In different embodiments the aryl contains 0, 1,2, 3, or 4 substituents. [02121 By "Acyl" is meant X'-R"-C(O)-, where R" is alkyl, substituted alkyl, heteroalkyl, substituted heteroalkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, alkylaryl, or substituted alklyaryl and X' is H or absent. 10 102131 By "Arylalkyl" or "alkylaryl" is meant an "alkyl" joined to an "aryl". [02141 By "Abu" is meant a-aminobutyric acid. 102151 By "Aepa" is meant 4-(2-aminoethyl)-1-carboxy methyl-piperazine, represented by the structure: 15 0 [02161 By "Aib" is meant a-aminoisobutyric acid. [02171 By "Ala" or A" is meant alanine. 20 102181 By "p-Ala" is meant beta-alanine. [02191 By "Arg" or "R" is meant arginine. [02201 By "Asn" or "N" is meant asparagine. [02211 By "Asp or "D" is meant aspartic acid. [02221 By "Caeg" is meant N-(2-aminoethyl)-N-(2-cytosinyl-1-oxo-ethyl)-glycine, 25 represented by the structure:
NH
2 N 0 N 300 30 -~N N RH H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 37 102231 By "Cys" or "C" is meant cysteine. [02241 By "Dab" is meant 2,4-diaminobutyric acid. [02251 By "Doc" is meant 8-amino-3, 6-dioxaoctanoic acid, represented by the structure 5 H [02261 By "Gln" or "Q" is meant glutamine. [02271 By "Glu" or "E" is meant glutamic acid. 10 102281 By "Gly" or "G" is meant glycine. [02291 By "His" or "H" is meant histidine. [02301 By "Ile" or "I" is meant isoleucine. [02311 By "Leu" or "L" is meant leucine. [02321 By "Lys" or K" is meant lysine. 15 [02331 By "Met" or "M"is meant methionine. [02341 By "1Nal"is meant p-(1-naphthyl)alanine. [02351 By "2Nal"is meant j-(2-naphthyl)alanine. [0236] By "Nle"is meant norleucine. 102371 By "Orn"is meant ornithine. 20 [02381 By "2Pal"is meant f-(2-pyridinyl)alanine. [02391 By "3Pal"is meant fi-(3-pyridinyl)alanine. [02401 By "4Pal"is meantfi-(4-pyridinyl)alanine. [02411 By "Phe" or "F"is meant phenylalanine. [02421 By "Pro" or "P"is meant proline. 25 [02431 By "Ser" or "S"is meant serine. [02441 By "Thr" or "T" is meant threonine. [0245] By "Thr-ol" is meant threoninol, represented by the structure: OH OH NZ 30 H [02461 By "Val" or "V" is meant valine. H:\MaraR\Keep\Speci\P64463-div-SPECI .doc 7/02/08 - 38 [0247] By "(N-Me)Trp" " is meant N-a-methyl-tryptophan. [02481 Certain other abbreviations used herein are defined as follows: 102491 By "Ac" is meant acetyl. [02501 By "Boc" is meant tert-butyloxycarbonyl. 5 10251] By "Bzl" is meant benzyl. [02521 By "DCM" is meant dichloromethane. [02531 By "DIC" is meant N, N-diisopropylcarbodiimide. [02541 By "DIEA" is meant diisopropylethyl amine. [02551 By "Dmab" is meant 4-{N-(1-(4,4-dimethyl-2,6-dioxocyclohexylidene)-3 10 methylbutyl)-amino} benzyl. [02561 By "DMAP" is meant 4-(dimethylamino)pyridine. 102571 By "DMF" is meant dimethylformamide. [0258] By "DNP" is meant 2,4-dinitrophenyl. [02591 By "Fmoc" is meant Fluorenylmethyloxycarbonyl. 15 102601 By "HBTU" is meant 2-(1H-benzotriazole-I-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate. [0261] By "cHex" is meant cyclohexyl. [02621 By "HOAT" is meant 0-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate. 20 [0263] By "HOBt" is meant 1-hydroxy-benzotriazole. [0264] By "Mint" is meant 4-methoxytrityl. 102651 By "NMP" is meant N-methylpyrrolidone. 102661 By "Pbf' is meant 2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl. 102671 By "tBu" is meant tert-butyl. 25 [02681 By "TIS" is meant triisopropylsilane. [0269] By "TOS" is meant tosyl. [02701 By "trt" is meant trityl. [02711 By "TFA" is meant trifluoro acetic acid. [02721 By "TFFH" is meant tetramethylfluoroforamidinium hexafluorophosphate. 30 102731 By "Trp" or "W" is meant tryptophan. 10274] By "Tyr" or "Y" is meant tyrosine. 102751 By "3ITyr" is meant 3-iodo-tyrosine. H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 39 102761 3ITyr(Dop2) has the structure of: 0H HNH S--' NN N %H HN 0 5 [02771 By a "somatostatin receptor agonist" is meant a compound that has a high binding affinity (e.g., Ki of less than 100 nM, or preferably less than 10 nM, or more preferably less than I nM) for a somatostatin receptor (e.g., as defined by the receptor binding assay described below), such as any of the different subtypes: e.g., SSTR-1, 10 SSTR-2, SSTR-3, SSTR-4, and SSTR-5, and elicits a somatostatin-like effect; for example, in an assay for the inhibition of cAMP intracellular production. [02781 By a "somatostatin selective agonist" is meant a somatostatin receptor agonist which has a higher binding affinity (i.e., lower Ki) for one somatostatin receptor subtype than for any other somatostatin receptor subtype, such as, for example, a 15 somatostatin SSTR-2 selective agonist. [02791 By a "dopamine receptor agonist" is meant a compound that has a high binding affinity (e.g., Ki of less than 100 nM, or preferably less than 10 nM, or more preferably less than I nM) for a dopamine receptor (e.g., as defined by the receptor binding assay described below), such as any of the different subtypes: e.g., Dl, D2, D3, 20 D4, and D5 receptors. Detailed Description [0280] The invention features somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use for the treatment of neoplasia, acromegaly, and other 25 conditions. [0281] Various somatostatin receptors (SSTR's) have been isolated (e.g., SSTR-1, SSTR-2, SSTR-3, SSTR-4, and SSTR-5). Somatostatin agonists are those compounds H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 40 that bind to at least one SSTR (e.g., SSTR-1 agonist, SSTR-2 agonist, SSTR-3 agonist, SSTR-4 agonist or a SSTR-5 agonist). [02821 Further examples of somatostatin agonists are those covered by formulae or those specifically recited in the publications set forth below, each of which is hereby 5 incorporated by reference in its entirety. PCT Application No. WO 03/057214 (2003) U.S. Application No. 20030191134 (2003) U.S. Application No. 20030083241 (2003) PCT Application No. WO 02/10215 (2002) 10 U.S. Patent No. 6,316,414 (2001) PCT Application No. WO 99/22735 (1999) PCT Application No. WO 98/08100 (1998) PCT Application No. WO 98/44921 (1998) PCT Application No. WO 98/45285 (1998) 15 PCT Application No. WO 98/44922 (1998) EP Application No. P5 164 EU (Inventor: G. Keri); Van Binst, G. et al. Peptide Research 5:8 (1992); Horvath, A. et al. Abstract, "Conformations of Somatostatin Analogs Having Antitumor Activity", 22nd European peptide Symposium, September 13-19, 1992, 20 Interlaken, Switzerland; PCT Application No. WO 91/09056 (1991); EP Application No. 0 363 589 A2 (1990); U.S. Patent No. 4,904,642 (1990); U.S. Patent No. 4,871,717 (1989); 25 U.S. Patent No. 4,853,371 (1989); U.S. Patent No. 4,725,577 (1988); U.S. Patent No. 4,684,620 (1987); U.S. Patent No. 4,650,787 (1987); U.S. Patent No. 4,603,120 (1986); 30 U.S. Patent No. 4,585,755 (1986); EP Application No. 0 203 031 A2 (1986); U.S. Patent No. 4,522,813 (1985); H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 41 U.S. Patent No. 4,486,415 (1984); U.S. Patent No. 4,485,101 (1984); U.S. Patent No. 4,435,385 (1984); U.S. Patent No. 4,395,403 (1983); 5 U.S. Patent No. 4,369,179 (1983); U.S. Patent No. 4,360,516 (1982); U.S. Patent No. 4,358,439 (1982); U.S. Patent No. 4,328,214 (1982); U.S. Patent No. 4,316,890 (1982); 10 U.S. Patent No. 4,310,518 (1982); U.S. Patent No. 4,291,022 (198 1); U.S. Patent No. 4,238,481 (1980); U.S. Patent No. 4,235,886 (1980); U.S. Patent No. 4,224,199 (1980); 15 U.S. Patent No. 4,211,693 (1980); U.S. Patent No. 4,190,648 (1980); U.S. Patent No. 4,146,612 (1979); U.S. Patent No. 4,133,782 (1979); U.S. Patent No. 5,506,339 (1996); 20 U.S. Patent No. 4,261,885 (1981); U.S. Patent No. 4,728,638 (1988); U.S. Patent No. 4,282,143 (198 1); U.S. Patent No. 4,215,039 (1980); U.S. Patent No. 4,209,426 (1980); 25 U.S. Patent No. 4,190,575 (1980); EP Patent No. 0 389 180 (1990); EP Patent No. 0 505 680 (1982); EP Patent No. 0 083 305 (1982); EP Patent No. 0 030 920 (1980); 30 PCT Application No. WO 88/05052 (1988); PCT Application No. WO 90/12811 (1990); PCT Application No. WO 97/01579 (1997); H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 42 PCT Application No. WO 91/18016 (1991); U.K. Application No. GB 2,095,261 (1981); and French Application No. FR 2,522,655 (1983). [02831 Note that for all somatostatin agonists described herein, each amino acid 5 residue represents the structure of -NH-C(R)H-CO-, in which R is the side chain (e.g.,
CH
3 for Ala). Lines between amino acid residues represent peptide bonds that join the amino acids. Also, where the amino acid residue is optically active, it is the L-form configuration, unless the D-form is expressly designated. For clarity, disulfide bonds (e.g., disulfide bridge) that exist between two free thiols of Cys residues are not shown. 10 Abbreviations of the common amino acids are in accordance with IUPAC-IUB recommendations. Synthesis of Somatostatin Agonists [02841 The methods for synthesizing peptide somatostatin agonists are well 15 documented and are within the ability of a person of ordinary skill in the art. For example, peptides are synthesized on Rink amide MBHA resin (4-(2'4' dimethoxyphenyl-Fmoc-aminomethyl)-phenoxyacetamido-norleucyl-MBHA resin) using a standard solid phase protocol of Fmoc chemistry. The peptide-resin with free amino functional at the N-terminus is then treated with the corresponding compound 20 containing dopamine moiety. The final product is cleaved off from resin with TFA water/triisopropylsilane (TIS) mixture. [02851 For example, synthesis of H-D-Phe-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-NH 2 , can be achieved by following the protocol set forth in Example I of European Patent Application 0 395 417 Al. The synthesis of somatostatin agonists with a substituted N 25 terminus can be achieved, for example, by following the protocol set forth in PCT Publication No. WO 88/02756, PCT Publication No., WO 94/04752, and/or European Patent Application No. 0 329 295. [02861 Peptides can be and were cyclized by using iodine solution in MeOH/water and purified on C 18 reverse-phase preparative HPLC, using acetonitrile 30 0.1 %TFA/water-0. 1 %TFA buffers. Homogeneity was assessed by analytical HPLC and mass spectrometry and determined to be >95% for each peptide. H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 43 [02871 Certain uncommon amino acids were purchased from the following vendors: Fmoc-Doc-OH and Fmoc-AEPA-OH were purchased from Chem-Impex International, Inc. (Wood Dale, IL, USA). Fmoc-Caeg (Bhoc)-OH was purchased from PerSeptive Biosystems (Framingham, MA, USA). Bhoc stands for benzhydryloxycarbonyl. 5 Synthesis of Dopamine Agonists [0288] The methods for synthesizing many dopamine agonists are also well documented and are within the ability of a person of ordinary skill in the art. Further synthetic procedures are provided in the following reaction schemes and examples. H.\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08
-
44 OH CH 2 0 N"Rl N Rl N Rl H H H H"" H'''H% 12 3 Scheme 1 HN -CH 2 (Cl 4) N Rl (Cl 14 )CHONaH N-Rl FPH"H I N 3 4H Scheme 2 OH0 SJ-\ H H . sI-yidn NR hydrolysis, OH- R 2. CH 3 C(O)SH H H Hl" H 5 H:\maraR\Keep\speci\P64463-diV-SPECI .dOC 7/02/08 - 45 Scheme 3: O O
NH
2 HN CR7R8)q4 OH N-R1 Base N-R1 H IH H",, H" (CR7R8) NN H o O O H 3 10' Scheme 4: OH O N 0 N'R N,N'-dissuccinimidyl -R1 H carbonate N H". H 3 H" N H N H 1 - 11' Scheme 5: NH2 HN O N-R1 NN'-dissuccinimidyl H carbonate N'R1 H"' H H"" N H / N H 12' H:\MaraR\Keep\speci\P64463-div-SPECI.doc 7/02/08 - 46 Scheme 6: OH OH s s N-Rl N-Rl H oxidation H H"' H" N N H H 6' 13' Scheme 7: OH OH 00 N'Rl N-Rl H oxidation H H'' H'' N N H H 6' 14' H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 47 Scheme 8: H H 1) Boc 2 O/DCM R5NCS R5-N N S H2N SH H2N S 2) Ac 2 /Base 0 S O 3)50% TFA in DCM HN, R5 R5 O N< 0 SH HN 0 OH.1 O N4 -S I 9R5-N=--N SY O N'-R1 -0 OH (f H hydrolysis 0 N-'-R1 O HH' H N \.H"" H N 15' H I H N H 2' Scheme 9: H H
H
2 N OH 1) Boc 2 O/DCM H 2 N O R5NCS R5-N N 2) Ac 2 O/Base 0 3)50% TFA in DCM HN R5 OH- ~ ~1iO< R~N~R5 ~ O N NOH HN O 0 N OH. O N 4O- : R5-N=--N O O R OH H hydrolysis N-R1 O HH O H NN H H HI N 16' H -- / N H 2 HM:\araR\Keep\speci\P64463-div-SPECIdoc 7/02/08 - 48 Scheme 10: H2N OH 1) Boc20/DCM H Nf a R5NCS R5 H0
H
2 N ,UN ) H2N~<> .CH 3 R5 A-41 CI1 2) MeOH/DIC/DMAP/pyridine 3) 50% TFA in DCM I HgO H ,R5 O O 'H3 heat 0 N R5 -N=-=N H O N 1 OH hydrolysis with base H 0 N or enzymaticN hydrolysis (e.g., H esterase) H H 17' 2' H HN HN N O1 N H H H H 18' (see Scheme 11) 19' (see Scheme 11) H:\MaraR\Keep\SpeCi\P64463-div-SPECI.doc 7/02/08 - 49 Scheme 11: ,R5 HN' OH O' N 41-S/ 0 N SH 1) BrCH 2 C(O)OEt/Base 0 IN 0 N-R1 N'R1 2) Hydrolysis, OH- H H H"' H". N N H H 15' 20' Scheme 12: ,R5 HN R5 0 N 4lj NH 2 0&I N (CR9R10 q4 Base H OH O N'R1 0 O H (CR9R1 NO'R H"' H Hl" N H N H 21' H:\MaraR\Keep\Speci\P64463-div-SPECI .doc 7/02/08 - 50 Scheme 13: HN R5 HN R5 O Oy O N0NH2 N iN O N,N'-disuccinimidyl H 0 O Ncarbonate H H H"" H.. N N H H 22' Scheme 14: HN R5 HNR5 O O O N iOH N,N'-disuccinimidyl O N 4?O O' carbonate O N.-R1 *ON'R1 H H H"" H" N N H H 16' 23' Scheme 15: HN R5 1) Br-CH 2
-COOCH
3 HN R5 H H H"" H"" N N H H 16' 24' H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 51 Scheme I H H NCH3 Reduction H3 H NH Ra-Ni or H" DMF-pyridine/Pd-C, H2 HN N H Lysergol Dihydrolysergol Reduction R'COCI/pyridine/DMAP R' H 1)CNBr NR 2) Zn-dust or H
NC
3 Ra-Ni/H 2 H 3) R-I/K 2
CO
3 H H" 4) OH H N H R=C 1 , alkyl, allyl, or alkenyl 1) MsCl/pyridine 2) HS(CH 2 )pCO 2 Rl
(CH
2 )pCO 2 H .(CH2)PCO2R1 N,R NR H 1) OH~ H 2) H 3 0+H H" H H H (I) Compounds 6', 7', and 8' can be synthesized using the synthetic scheme above: OH OH OH O S 0 S N-R1 H N N H" , H H H"'" H' q N I H N N H H 6 77 8/ H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 52 Scheme II H, N ---.-- . J R" H N n " H 0 NK
BOC
2 0
BOC
2 0/Base base hydrolysis N oBoc Boc H R1 0 DIC/DCM Base H H H ~,-Boc HR1 R" BcR"'-HN H 0 a 1) H+ O H 2) BrCH 2
CO
2 BzI H 3) R'NCO 4. [H] or enzymatic H hydrolysis (e.g., esterase) H H 18' Where R" and R" are, independently, H or C ,-C 4 alkyl H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 53 Scheme III OH NH 2 N Rl---D.N 1 N R H 1) MsCI/pyridine H H" 2) H %"0 N N- K- N H 04H 0 3) NH 2
NH
2 , H 2 0 (CR7R8) 0 HN (CRA~)q-COOH N Rl H HH H H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 54 Scheme IV:
-(CH
2 )nCO 2 H NR H + Partially protected somatostatin ligand on resin or H" in solution N 1) couple (1) 2) deprotect and cleave (ligand on resin) (From Scheme 1) or deprotect (ligand in solution)
(CH
2 )nCO-Somatostatin / Derivative N -R H HH '& N H OH R'"-HN N - n' OH 0 N R1 Partially protected somatostatin ligand on resin or H + in solution H" N "1) couple H 2) deprotect and cleave (ligand on resin) or deprotect (ligand in solution) (From Scheme 11) R"'-HN N n 0- Somatostatin / Derivative N R1 H H N H H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 55 Scheme V: 0 HNL
.
I(CRyRB)q-COOH N ,R1 H + Partially protected somatostatin ligand on resin or H in solution N 1) couple 2) deprotect and cleave (ligand on resin) (11) or deprotect (ligand in solution) (From Scheme Ill) 0 HNl (CR7R,)q-CO-Somatostatin / Derivative N R1 NH H N H H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 56 Scheme VI: OH O N -,R1 H2N,,,, N R1 H H Curtius H reaction ~- N N H H N, N'-disuccinimidyl carbonate/base 0 0 o NO OH O HN,,,,, ,R1 HN,,,,, N R1 H 1) Sarcosine/base H H 2) H+ H N N H H H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 57 Synthesis of Somatostatin-Dopamine Chimers 102891 Somatostatin-dopamine chimers may be synthesized according to the following reaction schemes and examples. Starting material and intermediates for such compounds are commercially available or are prepared using standard methods, e.g., 5 see Pharmazie 39, 537 (1984); collect Czech. Chem. Commun. 33, 577 (1966); Helv. Chim. Acta 32, 1947, (1949), U.S.P. 5,097,031; USP 3,901,894; EP 0003667; and USP 4,526,892. Methods for the synthesis of peptides are known to the skilled artisan (e.g., see Stewart et al., Solid Phase Synthesis, Pierce Chemical, 2 "d Ed. 1984; G.A. Grant; Synthetic peptide; WH., Freenand Co., New York, 1992; M. Bodenszky A. Bodanszky, 10 The Practice of Peptide Synthesis, Spring Venlag. N.Y. 1984). [02901 Other somatostatin-dopamine chimers that suppress growth hormone and prolactin secretion and are useful in the treatment of acromegaly are described in Saveanu et al. (J. Clin. Endocrin. and Metab. 87:5545-5552, 2002), hereby incorporated by reference. 15 102911 The following examples are provided to illustrate the invention. They are not meant to limit the invention in any way. Example 1: Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 [02921 The Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr 20 NH 2 peptide was automatically synthesized on an ACT 396 peptide synthesizer (Advanced ChemTech, Louisville, KY) using Fluorenylmethyloxycarbonyl (Fmoc) chemistry. A RINK AMIDE 4-methylbenzylhydrylamine (MBHA) resin (Novabiochem., San Diego, CA) with substitution of 0.66 mmol/g was used (sub: 0.66 mmol/g, 76 mg, 50 ptmol scale). The Fmoc amino acids used are Fmoc-DTrp(Boc)-OH, 25 Fmoc-Lys(Boc)-OH, Fmoc-Thr(But)-OH, Fmoc-DPhe-OH, Fmoc-Cys(Trt)-OH, and Fmoc-DLys(Dde))-OH from NOVABIOCHEM (San Diego, CA) and Fmoc-31Tyr-OH from CHEM-IMPEX INTERNATIONAL, Inc. (Wood Dale, IL). The synthesis was carried out on a 50 pmol scale. For each reaction cycle, the ACT 396 peptide synthesizer was programmed to perform: (1) washing with N-methylpyrrolidone (NMP) 30 twice; (2) removing Fmoc protecting group with 20% piperidine in NMP for I X 5 min and 1 X 25 min; (3) washing with NMP twice; and (4) double coupling with 4 X fold excess of Fmoc protected amino acid (0.20 mmol), HOBt (0.2 mmol), and N, N' H.\MaraR\Kcep\Speci\P64463-div-SPECI.doc 7/02/08 - 58 diisopropylcarbodiimide (DIC) (0.2 mmol) in NN-dimethylformamide (DMF) for 1 hour per coupling. The resin was coupled successively according to the sequence. [02931 After the peptide chain was assembled, the Fmoc group was removed and the resin was washed completely using NMP and dichloromethane (DCM). The resin was 5 transferred into a reaction vessel on a shaker and treated with 2% hydrozine in DMF for 2 X 30 minutes to remove Dde protecting group in the side chain of DLys. After washing successively with DMF, MeOH and DCM, the resin was shaken overnight with Dop2-OH (54 mg, 3.0 eq), bromo-tris-pyrrolidino-phosphonium hexafluorophosphate (PyBrop, 82 mg, 3.4 eq), 1-hydroxy-7-azabenzotriazole (HOAT, 0.4 mg, 3.0 eq), 10 pentalflurophenol (18.4 mg, 4 eq), DMAP (0.25 mL of 0.1 M in DMF, 1.0 eq) and diisopropylethyl amine (DIEA) (53 p.L, 4 eq). [02941 After washing successively with DMF, MeOH and DCM, the resin was treated with a mixture of TFA (4.75 mL), H 2 0 (0.4 mL), and triisopropylsilane (TIS, 0.425 mL) for 2 hours. The resin was removed by filtration. The filtrate was poured 15 into 70 mL of ether. The precipitate formed was filtered off and washed thoroughly with ether. This crude product was dissolved in 5 mL of aqueous acetic acid solution (water/acetic acid = 1:1). The solution was then diluted with 50 mL of H 2 0 and 20 mL of acetonitrile, to which was added, dropwise, iodine in methanol until the solution acquired a sustained yellow hue. The solution was stirred slowly for 1 hour and the 20 reaction was terminated by adding aqueous Na 2
S
2 0 3 solution. The crude product was purified on reverse-phase preparative HPLC using a column of C 18 DYNAMAX 100A 0 (4 x 43 cm, Varian, Walnut Creek, CA). The column was eluted with a liner gradient from 90% A and 10% B to 60% A and 40% B in an hour where A was 0.1% TFA in water and B was 0.1% TFA in acetonitrile. Fractions containing a major 25 component by ultraviolet (UV) absorption were pooled and lyophilized. The purity was 95.7% based on an analytical HPLC analysis. Electro-spray ionization mass spectrometry (ESI mass) analysis gave the molecular weight at 1982.6 (in agreement with the calculated molecular weight of 1983.3). 30 Example 2: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr
NH
2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 59 102951 The Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys] Thr-NH 2 compound was synthesized substantially according to the procedure described for the synthesis of Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys] 5 Thr-NH 2 (as described above in Example 1) with the following changes. After the assembly of the peptide chain, the resin was transferred into a reaction vessel on a shaker and treated with 25% piperidine in DMF for 30 minutes to remove the Fmoc protecting group at the N-terminus. After washing successively with DMF, MeOH and DCM, the resin was shaken overnight with Dop2-OH (3.0 eq), PyBrop (3.4 eq), HOAT 10 (3.0 eq), DMAP (1.0 eq) and DIEA (4 eq). After cleavage and purification, the desired product was found to have a purity of 95% based on an analytical HPLC analysis. ESI mass analysis gave the molecular weight at 2145.9 (in agreement with the calculated molecular weight of 2145.6). 15 Example 3: Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr
NH
2 [02961 The titled compound was synthesized substantially according to the procedure described for the synthesis of Dop2-DPhe-Doc-DPhe-c[Cys-3ITyr(Dop2) DTrp-Lys-Val-Cys]-Thr-NH 2 (described above in Example 2) except that Fmoc 20 Lys(Fmoc)-OH was used for the coupling of the last Lys residue at the N-terminus. The product was found to be homogenous and the purity was 93.9% by HPLC. ESI mass analysis gave the molecular weight at 2020.9 (in agreement with the calculated molecular weight of 2020.1). 25 [02971 Example 4: Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 2601322_1 (GHMatters) 14/03/11 - 60 The titled compound was synthesized substantially according to the procedure described for the synthesis of Dop2-DPhe-Doc-DPhe-c[Cys-3 ITyr(Dop2)-DTrp-Lys Val-Cys]-Thr-NH 2 (described above in Example 2) except that Fmoc-DLys(Fmoc)-OH 5 was used for the coupling of the last Lys residue at the N-terminus. The product was found to be homogenous and the purity was 99.9% by HPLC. ESI mass analysis gave the molecular weight at 1693.6 (in agreement with the calculated molecular weight of 1694.23). Example 5: Synthesis of intermediate compound (3) 10 OH O O>O HO .. o NO N N HH N H 2 2 HH 3YOH 15 0 102981 A mixture of R(-)norapomorphine compound I (from Sigma, 200 mg, 0.79 mmol) and p-toluenesulfonic acid monohydrate (451 mg, 2.37 mmol) in acetone (20 mL) is stirred at room temperature overnight. The solvent is removed under reduced pressure. The residue is dissolved in methylene chloride (30 mL) and washed with 20 saturated NaHCO 3 aqueous solution (2 times) and brine (2 times), dried over anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding acetonide- R(-)norapomorphine, yielding compound 2. 102991 To a mixture of compound 2 (167 mg, 0.57 mmol) and NN 25 diisopropylethylamine (219 mg, 1.7 mmol) in methylene chloride (20 mL) is added dropwise bromoacetic acid (236 mg, 1.7 mmol) at 0 0 C. The mixture is then warmed to room temperature and stirred for 6 hours. The solution is washed with brine (2 times), dried over anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding intermediate compound 3. 30 Example 6: Synthesis of intermediate compound (6) OH N- N 0 N H H N 2601322 (GHM t $)NL4/03/11 4 5HH 6H OH - 61 103001 The mixture of R(-)norapomorphine 4 (200 mg, 0.748 mmol), 2 methylpropene (83.9 mg, 1.50 mmol), and a catalytic amount of concentrated H 2
SO
4 in
CH
2 Cl 2 (20 mL) is stirred at room temperature overnight. The solution is washed with saturated NaHCO 3 in aqueous solution (2 times) and brine (2 times), dried over 5 anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding compound 5. 103011 To a mixture of compound 5 (150 mg, 0.486 mmol) and NN diisopropylethylamine (188 mg, 1.46 mmol) in methylene chloride (20 mL) is added dropwise bromoacetic acid (203 mg, 1.46 mmol) at 0 0 C. The mixture is then warmed 10 to room temperature and stirred for 6 hours. The solution is washed with brine (2 times) and dried over anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding intermediate compound 6. 15 Example 7: Synthesis of intermediate compound (11) NH N---- OH 0 20 N ON =0 &N &N H H 10 11 103021 To a mixture of indolone 10 (WO 9415918, 218 mg, 1.00 mmol) and N,N 25 diisopropylethylamine (258 mg, 2.0 mmol) in methylene chloride (20 mL) is added 4 iodobutyric acid (214 mg, 1.0 mmol). The resulting solution is stirred at room temperature overnight. The solution is concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding intermediate compound 11. 30 Example 8: Synthesis of intermediate compound (14) 2601322_1 (GHMatters) 14/03/11 - 62 0 0 OH 0 N-OH 5 12 13 14 [03031 To a mixture of 1 -adamantanamine hydrochloride 12 (Aldrich, 187 mg, 1.00 mmol) and NN-diisopropylethylamine (387 mg, 3.0 mmol) in methylene chloride (20 10 mL) is added 4-iodobutyric acid (214 mg, 1.0 mmol). The resulting solution is stirred at room temperature overnight. The solution is washed with brine (2 times), dried over anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding compound 13. 103041 To a solution of compound 13 (190 mg, 0.8 mmol) in dioxane (6 mL) and 15 water (3 mL) is added IN NaOH (1.0 mL) at 0 0 C. To the resulting solution is added di-tert-butyl dicarbonate (192 mg, 0.88 mmol) over 30 min. The mixture is stirred at room temperature for 12 hours. Dioxane is removed under reduced pressure. To the resulting water solution is added ethyl acetate. The pH of the solution is adjusted to about pH 3 by adding 0.2 N HCI solution at 0 0 C. The organic layer is separated, 20 washed with water (twice), dried over anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding intermediate compound 14. Example 9: Synthesis of intermediate compound (18) 25 0 H OH N N ClCl CO CI HO H OQ 0 03o 30H 15 O )\O16 17 A \ 117 18 [03051 The mixture of fenoldopam 15 (from Sigma, 306 mg, 1.00 mmol) and p toluenesulfonic acid monohydrate (476 mg, 2.50 mmol) in acetone (30 mL) is stirred at room temperature overnight. The solvent is removed under reduced pressure. The 2601322_1 (GHMatters) 14/03/11 - 63 residue is dissolved in methylene chloride (30 mL) and washed with saturated NaHCO 3 aqueous solution (2 times) and brine (2 times), dried over anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding acetonide- fenoldopam 16. 5 [0306] A mixture of acetonide- fenoldopam 16 (277 mg, 0.80 mmol), 2 methylpropene (67.0 mg, 1.20 mmol), and a catalytic amount of concentrated H 2
SO
4 in
CH
2 Cl 2 (20 mL) is stirred at room temperature overnight. The solution is washed with saturated NaHCO 3 aqueous solution (2 times) and brine (2 times) and dried over anhydrous MgSO 4 , filtered and concentrated in vacuo. The residue is purified by using 10 column chromatography on silica, yielding compound 17. [03071 To a mixture of 17 (201 mg, 0.50 mmol) and NN-diisopropylethylamine (129 mg, 1.0 mmol) in methylene chloride (20 mL) is added 4-iodobutyric acid (107 mg, 0.5 mmol). The resulting solution is stirred at room temperature overnight. The solution is washed with brine (2 times), dried over anhydrous MgSO 4 , filtered and 15 concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding intermediate compound 18. Example 10: Synthesis of intermediate compound (21) 20 N K OH OH H 2 N NH< a F H N - < N H,, - , O N o H H-." o 19 20 21 25 [03081 To a solution of 19 (169 mg, 1.0 mmol) in dioxane (20 mL) and water (10 mL) is added 4-iodobutyric acid (214 mg, 1.0 mmol). The resulting solution is stirred for 24 hours. During this period of time, the pH of the solution is kept at 7-8 by adding 0.5 N NaOH solution. The solvents are removed under reduced pressure. The residue is purified using column chromatography on silica, yielding compound 20. 30 [03091 To a solution of 20 (179 mg, 0.7 mmol) in dioxane (6 mL) and water (3 mL) is added lN NaOH (2.1 mL) at 0 0 C. To the resulting solution is added di-tert-butyl dicarbonate (336 mg, 1.54 mmol) over the course of 30 minutes. The mixture is stirred at room temperature for 12 hours. Dioxane is removed under reduced pressure. To the 2601322_1 (GHMatters) 14/03/11 - 64 resulting water solution is added ethyl acetate. The pH of the solution is adjusted to about pH 3 by the addition of 0.2 N HCl solution at 0 0 C. The organic layer is separated, washed with water (twice), dried over anhydrous MgSO 4 , filtered and concentrated in vacuo. The residue is purified by using column chromatography on 5 silica, yielding intermediate compound 21. Example 11: Synthesis of intermediate compound (24) 0 OH OH H 10 N- N O
H
2 N 2NNH ]: 2 N N , o o 22 24 15 103101 To a solution of 22 (169 mg, 1.0 mmol) in dioxane (20 mL) and water (10 mL) is added 4-iodobutyric acid (214 mg, 1.0 mmol). The resulting solution is stirred for 24 hours. During this period of time, the pH of the solution is kept at 7-8 by adding 0.5 N NaOH solution. The solvents are removed under reduced pressure. The residue is purified using column chromatography on silica, yielding compound 23. 20 [03111 To a solution of 23 (179 mg, 0.7 mmol) in dioxane (6 mL) and water (3 mL) is added IN NaOH (1.4 mL) at 0 0 C. To the resulting solution is added di-tert-butyl dicarbonate (168 mg, 0.77 mmol) over the course of 30 minutes. The mixture is stirred at room temperature for 12 hours. The pH of the solution is adjusted to about 4-5 by addition of 0.2 N HCl solution at 0 0 C. The solution is concentrated in vacuo. The 25 residue is purified by using column chromatography on silica, yielding intermediate compound 24. Example 12: Synthesis of intermediate compound (27) 30 H ,0" 0" H 0' NH H,1, H,,, 3 0 NH O OH 25 26 27 2601322_1 (GHmatters) 14/03/11 - 65 [03121 A mixture of 25 (205 mg, 1.00 mmol), 2-methylpropene (84 mg, 1.50 mmol), and concentrated H 2
SO
4 in CH 2 Cl 2 (20 mL) is stirred at room temperature overnight. The solution is washed with saturated NaHCO 3 in aqueous solution (2 times) and brine 5 (2 times) and dried over anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified using column chromatography on silica, yielding compound 26. [03131 To a mixture of 1-adamantanamine hydrochloride 2 (209 mg, 0.8 mmol) and N,N-diisopropylethylamine (310 mg, 2.4 mmol) in methylene chloride (20 mL) is added 4-iodobutyric acid (171 mg, 0.8 mmol). The resulting solution is stirred at room 10 temperature overnight. The solution is concentrated in vacuo. The residue is purified using column chromatography on silica, yielding intermediate compound 27. Synthesis of other compounds 103141 The compounds listed below can be synthesized according to the procedures 15 described above. 10315] For the introduction of DopI, Dop2, Dop3 or Dop4 residue(s) into peptides, Dopl-OH, Dop2-OH, Dop3-OH or Dop4-OH (WO 02/100888 Al) was used during the syntheses, respectively. [03161 For the synthesis of the Dop5 containing peptides, Fmoc-Dopa(acetonide) 20 OH (Novabiochem, San Diego, CA) was used. [03171 For the Dop6 residue in peptides, compound I1 is used during the synthesis. [0318] For the Dop7 residue in peptides, compound 21 is used during the synthesis. [0319] For the Dop8 residue in peptides, compound 14 is used during the synthesis. [03201 For the Dop9 residue in peptides, compound 24 is used during the synthesis. 25 [03211 For the Dop10 residue in peptides, compound 3 is used during the synthesis. [0322] For the Dop II residue in peptides, compound 6 is used during the synthesis. [03231 For the Dop12 residue in peptides, compound 27 is used during the synthesis. [03241 For the Dop 13 residue in peptides, compound 18 is used during the synthesis. 30 103251 Table 1 lists somatostatin-dopamine chimeric analogs likely to have somatostatin and dopamine activity in vitro or in vivo. Table 1 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 66 Dop5-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 Dop6-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 5 Dop7-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop8-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop9-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop I O-DPhe-cyclo [Cys-Tyr-DTrp-Lys.-Abu-Cys] -Thr-NH 2 Dop 11 -DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 10 Dop I 2-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop I 3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop5 -cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]l-Thr-NH 2 Dop6-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop7-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-N H 2 15 Dop8-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop9-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop 1 O-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop I11 -cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop I 2-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 20 Dop 1 3-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop5-D2NaI-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 Dop6-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 Dop7-D2NaI-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 Dop8-D2Na1-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 25 Dop9-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys]-Thr-NH 2 2601322_1 (GHatters) 14/03/11 - 67 Dop I 0-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop 1 -D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop 1 2-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop 13-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 5 Dop5-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop6-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop7-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop8-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop9-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 10 Dop1 0-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop 11-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop1 2-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop 13-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop5-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI 15 Dop6-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop7-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop8-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop9-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop1 O-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 20 Dop I I-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop I 2-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop 13-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop5-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop6-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 25 Dop7-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop8-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop9-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop 1 0-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop 1 -cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 30 Dop I 2-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop 13-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 68 Dop6-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop7-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 5 Dop8-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop 1 O-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop 11-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop12-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 10 Dopl3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop5-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop6-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop7-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop8-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 15 Dop9-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 DopI0-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop 1 -cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop12-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop13-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 20 Dop5-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop6-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop7-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop8-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop9-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 25 Dop1O-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop 11-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 2601322_1 (GHMatters) 14/03/11 - 69 Dop I 2-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop 1 3-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 5 Dop5 -cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop6-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop7-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop8-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop9-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 10 Dop I O-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop] 1-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop]I2-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop13 -cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 15 Dop6-Caeg-cyclo [DCys- 3 Pal-DTrp- Lys- DCys] -Thr(Bz)-Tyr-NH 2 Dop7-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop8 -Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 Dop9-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop I -Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 20 Dop 1I -Caeg-cyclo [DCys-3 PaI-DTrp- Lys- DCys] -Thr(Bzl)-Tyr-NH 2 DoplI2-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop 13 -Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 2601322_1 (GHMattere) 14/03/11 - 70 Dop5-Caeg-cyclo[~DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2 Dop6-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 5 Dop7-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 Dop8-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzO)-Tyr-NH 2 Dop9-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 Dop I O-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 Dopl 11-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 10 DopI 2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 Dop13 -Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-SerBzl)-Tyr-NH 2 Dop5 -cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 Dop6-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 Dop7-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 15 Dop8-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 Dop9-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 DopI O-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop I11 -cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 DoplI2-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 20 Dop 13 -cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 Dop5 -DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop6-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop7-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop8-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 25 Dop9-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop I O-DPhe-cyclo [Cys- Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop I11 -DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop 1 2-DPhe-cyc lo [Cys- Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 2601322 _1 (GHmaters) 14/03/11 - 71 Dop 13-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2 Dop6-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop7-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 5 Dop8-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop9-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2 Dop 1 0-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop 1l-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2 Dop 1 2-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 10 Dop 13-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 15 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -Lys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop 1 -Lys(Dop l)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 20 Dop 1 -Lys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -DLys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -DLys(Dop l)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 25 Dop 1 -DLys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop I -DLys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -DLys(Dop l)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 30 Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 72 Dopl -Lys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop1 -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop 1 -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 5 Dop 1 -Lys(Dopl)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop 1 -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dopl -Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dopl-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 10 Dopl -Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dopl -Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 15 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 20 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 25 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 30 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol H:\MaraR\Keep\Speci\P64463-div-SPECI.dOC 7/02/08 - 73 Dop2-Lys(Dop2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 5 Dop2-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop3-Lys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 10 Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop3-DLys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop3-DLys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 15 Dop3-DLys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop3-DLys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop3-DLys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop3-Lys(Dop3)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 20 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2 25 Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop3-Lys(Dop3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 30 Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop3-Lys(Dop3)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 74 Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 5 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop4-DLys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop4-DLys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop4-DLys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 10 Dop4-DLys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop4-DLys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2 Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 15 Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2 Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 20 Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop4-Lys(Dop4)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 25 Dop4-Lys(Dop4)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 30 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5-DLys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 75 Dop5-DLys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 5 Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 10 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop5-Lys(Dop5)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI 15 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop5-Lys(Dop5)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 20 Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop6-DLys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 25 Dop6-DLys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop6-DLys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop6-DLys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop6-Lys(Dop6)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 30 Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 H:\MaraR\Kecp\Speci\P64463-div-SPECI.doc 7/02/08 - 76 Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2 Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI 5 Dop6-Lys(Dop6)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop6-Lys(Dop6)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 10 Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop7-DLys(Dop7)-DPhe-cyclo(Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 15 Dop7-DLys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop7-Lys(Dop7)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 20 Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop7-Lys(Dop7)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop7-Lys(Dop7)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 25 Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop8-DLys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop8-DLys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop8-Lys(Dop8)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 30 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 77 Dop8-Lys(Dop8)-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop8-Lys(Dop8)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop8-Lys(Dop8)- cyclo[Cys-Tyr-DTrp-Lys-VaI-Cys] -Trp-NH 2 Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 5 Dop9-Lys(Dop9)-cyclollCys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop9-DLys(Dop9)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop9-DLys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop9-Lys(Dop9)-D2NaI-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 Dop9-Lys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 10 Dop9-Lys(Dop9)-DPhe-cyclollCys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 Dop9-Lys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop9-Lys(Dop9)-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 15 Dop9-Lys(Dop9)- cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 Dop I -Lys(DoplI )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop IO-Lys(DoplI )-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 DopI1O-DLys(Dopl1 )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 DopI1 -DLys(Dopl1 )-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 20 DopI1O-Lys(Dopl1 )-D2NaI-cyclo [Cys-Tyr-DTrp-Lys-.Val-Cys]-Thr-NH 2 DopI1 -Lys(Dop I )-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 DopI1 -Lys(Dopl1 )-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 Dopl I -Lys(Dop I 0)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Na1-NH 2 Dopl 1 -Lys(Dop 1 0)-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 25 Dopl I -Lys(Dop 1 0)-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-o1 Dopl I -Lys(Dop I 0)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys] -Trp-NH 2 DopI 0-Lys(DopIO)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2 Dopl 11-Lys(Dopl 11)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dopl 11-Lys(Dopl II)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 30 Dop I I -DLys(Dop I 1 )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop I I -DLys(Dop II )-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl 11-Lys(Dopl 11)-D2Na1-cyclo[Cys-Tyr-DTrp-Lys-VaI-Cys]-Thr-NH 2 H'\MaraR\Keep\Speci\P64463-div-SPECI .doc 7/02/08 - 78 Dop l l-Lys(Dopl l)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop I l-Lys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop 11-Lys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop 11 -Lys(Dop 11)-DPhe-cyclo(Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 5 Dop 11-Lys(Dop 11)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dopl -Lys(Dopl l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop I 1-Lys(Dopl 1)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2 Dop 1 2-Lys(Dop I 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop12-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 10 Dop12-DLys(Dopl2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop 1 2-DLys(Dop 1 2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop 1 2-Lys(Dop I 2)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop I 2-Lys(Dop I 2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop I 2-Lys(Dop I 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 15 Dop I 2-Lys(Dop I 2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2 Dop I 2-Lys(Dop I 2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop 1 2-Lys(Dop I 2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop I 2-Lys(Dop I 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop12-Lys(Dop12)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 20 Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 Dop13-Lys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop13-DLys(Dop1O)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop13-DLys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop13-Lys(Dop13)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 25 Dop13-Lys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop13-Lys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop13-Lys(DopI3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop13-Lys(Dop13)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 30 Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop13-Lys(Dop13)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop I -Lys(Dop l)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2 H:\MaraR\Keep\Speci\P64463-div-SPECI .doc 2/02/08 - 79 Dop I -Lys(Dop 1 )-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 Dop I -DLys(Dopl1)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop 1 -DLys(Dop I )-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 Dop 1 -Lys(Dop I )-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 5 Dop I -Lys(DoplI)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 Dop 1 -DLys(Dop 1 )-Lys-Caeg-cyclo[DCys-3 PaI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop I -DLys(DoplI)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 Dop 1 -Lys(Dop I )-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 Dop I -Lys(Dop 1 )-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 10 Dop I -DLys(Dop 1 )-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 Dop 1 -DLys(Dop 1 )-Aepa-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop 1 -Lys(Dop 1I)- Lys-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCys] -Thr(Bzl)-Tyr
NH
2 Dop I -Lys(DoplI)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr 15 NH 2 Dop I -DLys(Dop 1 )-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH4 2 Dop I -DLys(Dop I )-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr
NH
2 20 Dop2-Lys(Dop2)-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DC ys] -Thr(Bzl)-Tyr-NH 2 Dop2-Lys(Dop2)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 Dop2-DLys(Dop2)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop2-DLys(Dop2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2 Dop2-Lys(Dop2)-Lys-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys] -Thr(Bz1)-Tyr-NH 2 25 Dop2-Lys(Dop2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 Dop2-DLys(Dop2)- Lys-Caeg-cyclo [DCys-3 Pal- DTrp- Lys-DCys] -Thr(Bz)-Tyr-N H 2 Dop2-DLys(Dop2)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2 Dop2-Lys(Dop2)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bz)-Tyr-NH 2 Dop2-Lys(Dop2)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 30 Dop2-DLys(Dop2)-Aepa-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop2-DLys(Dop2)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 1l\MaraR\Keep\Speci\P64463-div-SPECI .doc 7/02/08 - 80 Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH1 2 Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH1 2 5 Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr
NH
2 Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH1 2 Dop3 -Lys(Dop3)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 10 Dop3 -Lys(Dop3)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 Dop3 -Lys(Dop3 )-Lys-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCys] -Thr(BzI)-Tyr-NH 2 Dop3 -Lys(Dop3 )-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 Dop3 -Lys(Dop3 )-Aepa-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop3 -Lys(Dop3)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 15 Dop3 -DLys(Dop3 )-Caeg-cyclo[DCys-3 PaI-DTrp-Lys-DCys]-Thr(BzI)-Tyr-NH 2 Dop3 -DLys(Dop3 )-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 Dop3 -DLys(Dop3 )-Lys-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop3 -DLys(Dop3 )-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop3 -DLys(Dop3 )-Aepa-Caeg-cyclolDCys-3 Pal-DTrp-Lys-DCysl-Thr(Bzl)-Tyr-NH 2 20 Dop3 -DLys(Dop3 )-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(3z)-Tyr-NH2 Dop4-Lys(Dop4)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop4-Lys(Dop4)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 Dop4-Lys(Dop4)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 Dop4-Lys(Dop4)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 25 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH1 2 Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr 30 NH1 2 Dop4-DLys(Dop4)-Caeg-cyclo [DCys-3 Pal- DTrp-Lys- DCys] -Thr(BzI)-Tyr-NH 2 Dop4-DLys(Dop4)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 81 Dop4-DLys(Dop4)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop4-DLys(Dop4)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop4-DLys(Dop4)-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop4-DLys(Dop4)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 5 Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr
NH
2 Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr
NH
2 Dop5-Lys(Dop5)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 10 Dop5-Lys(Dop5)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop5-DLys(Dop5)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop5-DLys(Dop5)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop5-Lys(Dop5)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2 Dop5-Lys(Dop5)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 15 Dop5-DLys(Dop5)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop5-DLys(Dop5)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop6-Lys(Dop6)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop6-Lys(Dop6)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop6-DLys(Dop6)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 20 Dop6-DLys(Dop6)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop6-Lys(Dop6)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop6-Lys(Dop6)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop6-DLys(Dop6)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop6-DLys(Dop6)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 25 Dop7-Lys(Dop7)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2 Dop7-Lys(Dop7)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop7-Lys(Dop7)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop7-Lys(Dop7)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop8-Lys(Dop8)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 30 Dop8-Lys(Dop8)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop8-Lys(Dop8)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop8-Lys(Dop8)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 82 Dop9-Lys(Dop9)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop9-Lys(Dop9)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop9-Lys(Dop9)-Lys-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop9-Lys(Dop9)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 5 Dop 1 O-Lys(Dop I 0)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop 1 O-Lys(Dop1 0)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 DopI O-Lys(Dop1 0)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop 1 O-Lys(Dop1 0)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop 1 I-Lys(Dop l )-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 10 Dop 11-Lys(Dopl l)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 DopI I-Lys(DopI1 )-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dopl1 -Lys(Dop11)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop 1 2-Lys(Dop 1 2)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop12-Lys(Dop12)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 15 Dopl2-Lys(Dopl2)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop12-Lys(Dopl2)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop13-Lys(Dop13)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop13-Lys(Dop13)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop 13-Lys(Dop I 3)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2 20 Dop13-Lys(Dop13)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop1-Lys(Dopl)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop1-Lys(Dop1)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl-DLys(Dopl)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop1-DLys(Dop1)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 25 Dopl-Lys(Dopl)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys)-Thr-NH 2 Dop1-DLys(Dop1)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 30 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 71/02/08 - 83 Dop3-Lys(Dop3)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop3-Lys(Dop3)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 5 Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys-Thr-NH2 Dop5-Lys(Dop5)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5-DLys(Dop5)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 10 Dop5-DLys(Dop5)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5-DLys(Dop5)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop6-Lys(Dop6)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 15 Dop6-DLys(Dop6)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop6-DLys(Dop6)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2 Dop6-Lys(Dop6)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop6-DLys(Dop6)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop7-Lys(Dop7)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2 20 Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2 Dop7-Lys(Dop7)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2 Dop8-Lys(Dop8)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop9-Lys(Dop9)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 25 Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop 1 O-Lys(Dop1 0)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop I O-Lys(Dop1 0)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop I1-Lys(Dop1 I)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop 11 -Lys(Dop I1)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2 30 Dop12-Lys(Dop12)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop13-Lys(DopI3)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 84 Dop 13-Lys(Dop1 3)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -DPhe-cyclo[Cys-3ITyr(Dop1)-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dopl)-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 5 Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -DLys(Dop l)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 10 Dopl -Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 15 Dopl-DLys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH2 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 20 Dopl -Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 25 Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 30 Dopl -Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl-DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH2 H:\MaraR\Keep\Speci\P64463-div-SPECI-doc 7/02/08 - 85 Dop 1 -DLys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 5 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Example 1 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 10 Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 15 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 20 Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 25 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH2 Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 30 Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 86 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop3 -Lys(Dop3 )-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 5 Dop3 -Lys(Dop3)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop4-Lys(Dop4)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop5 -DLys(Dop5)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop5 -Lys(Dop5)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 10 Dop5-DLys(Dop5 )-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5 -Lys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 15 Dop5 -DLys(Dop5)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop5 -Lys(Dop5)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5 -DLys(Dop5 )-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 DopS -Lys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 20 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop5 -DLys(Dop5 )-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5 -DLys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 lTyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop5-DLys(Dop5 )-DPhe.-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-N H 2 25 Dop5 -Lys(Dop5)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 Dop5 -DLys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop5-Lys(Dop5)-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 Dop5-DLys(Dop5 )-DTyr-DTyr-cyclo[Cys-3lTyr-DTrp-Lys-Val-Cys]-Thr-NH 2 30 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 Dop6-Lys(Dop6)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop7-Lys(Dop7)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 H:\MaraR\Keep\speci\P64463-div-SPECIdOC 7/02/08 - 87 Dop8-Lys(Dop8)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop9-Lys(Dop9)-cyclo(Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 DopI O-Lys(Dop I 0)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop 11-Lys(Dop 11)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 5 Dop12-Lys(Dopl2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop13-Lys(Dopl3)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop6-Lys(Dop6)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop7-Lys(Dop7)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 10 Dop9-Lys(Dop9)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop1O-Lys(Dop1O)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop 11-Lys(Dop 11)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop12-Lys(Dop12)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop13-Lys(Dopl3)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 15 [03261 Some of the compounds of the instant invention have at least one asymmetric center. Additional asymmetric centers may be present in the molecule depending upon the nature of the various substituents of the molecule. Each such asymmetric center will produce two optical isomers and it is intended that all such optical isomers, as 20 separated, pure or partially purified optical isomers, racemic mixtures or diastereomeric mixtures thereof, are included within the scope of the instant invention. 103271 The compounds of the instant invention generally can be provided in the form of their pharmaceutically acceptable acid addition salts, such as the salts derived from using inorganic and organic acids. Examples of such acids are hydrochloric, 25 nitric, sulfuric, phosphoric, formic, acetic, trifluoroacetic, propionic, maleic, succinic, D-tartaric, L-tartaric, malonic, methane sulfonic and the like. In addition, certain compounds containing an acidic function such as a carboxy can be isolated in the form of their inorganic salt in which the counter-ion can be selected from sodium, potassium, lithium, calcium, magnesium and the like, as well as from organic bases. 30 [03281 The pharmaceutically acceptable salts can be formed by taking about 1 equivalent of a compound of the invention and contacting it with about I equivalent or H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 88 more of the appropriate corresponding acid of the salt which is desired. Work-up and isolation of the resulting salt is well-known to those of ordinary skill in the art. 103291 The compounds of this invention can be administered by oral, parenteral (e.g., intramuscular, intraperitoneal, intravenous or subcutaneous injection, or implant), 5 nasal, vaginal, rectal, sublingual or topical routes of administration and can be formulated with pharmaceutically acceptable carriers to provide dosage forms appropriate for each route of administration. Accordingly, the present invention features pharmaceutical compositions comprising, as an active ingredient, at least one compound of the invention in association with a pharmaceutically acceptable carrier. 10 103301 Solid dosage forms for oral administration include capsules, tablets, pills, powders and granules. In such solid dosage forms, the active compound is admixed with at least one inert pharmaceutically acceptable carrier such as sucrose, lactose, or starch. Such dosage forms can also comprise, as is normal practice, additional substances other than such inert diluents, e.g., lubricating agents such as magnesium 15 stearate. In the case of capsules, tablets and pills, the dosage forms may also comprise buffering agents. Tablets and pills can additionally be prepared with enteric coatings. 103311 Liquid dosage forms for oral administration include pharmaceutically acceptable emulsions, solutions, suspensions, syrups, the elixirs containing inert diluents commonly used in the art, such as water. Besides such inert diluents, 20 compositions can also include adjuvants, such as wetting agents, emulsifying and suspending agents, and sweetening, flavoring and perfuming agents. [03321 Preparations according to this invention for parenteral administration include sterile aqueous or non-aqueous solutions, suspensions, or emulsions. Examples of non aqueous solvents or vehicles are propylene glycol, polyethylene glycol, vegetable oils, 25 such as olive oil and corn oil, gelatin, and injectable organic esters such as ethyl oleate. Such dosage forms may also contain adjuvants such as preserving, wetting, emulsifying, and dispersing agents. They may be sterilized by, for example, filtration through a bacteria-retaining filter, by incorporating sterilizing agents into the compositions, by irradiating the compositions, or by heating the compositions. They can also be 30 manufactured in the form of sterile solid compositions which can be dissolved in sterile water, or some other sterile injectable medium immediately before use. H;\MaraR\Keep\Speci\P64463-div-SPECI.doc '7/02/08 - 89 [03331 Compositions for rectal or vaginal administration are preferably suppositories which may contain, in addition to the active substance, excipients such as coca butter or a suppository wax. [03341 Compositions for nasal or sublingual administration are also prepared with 5 standard excipients well known in the art. [0335] In general, an effective dose of an active ingredient in the compositions of this invention may be varied; however, it is necessary that the amount of the active ingredient be such that a suitable dosage form is obtained. The selected dosage depends upon the desired therapeutic effect, on the route of administration, and on the duration 10 of the treatment, all of which are within the realm of knowledge of one of ordinary skill in the art. Generally, dosage levels of between 0.0001 to 100 mg/kg of body weight daily are administered to humans and other animals, e.g., mammals. 103361 Preferred dosage ranges are from 0.01 to 10.0 mg/kg of body weight. Such dosages may be administered, for example, daily as a single dose or divided into 15 multiple doses. Somatostatin Receptor Specificity and Selectivity Assay 103371 Specificity and selectivity of the somatostatin analogues used to synthesize the somatostatin-dopamine chimers was determined by a radioligand binding assay on 20 CHO-KI cells stably transfected with each of the SSTR subtypes, as follows. Somatostatin analogs are also described in U.S. Patent Application Publication No. 02210006790. The complete coding sequences of genomic fragments of the SSTR 1 (e.g., Genbank accession No. M81829), SSTR 2 (e.g., Genbank accession No. M81830), SSTR 3 (e.g., Genbank accession No. L07062), and SSTR 4 (e.g., Genbank 25 accession No. AL049651) genes and a cDNA clone for SSTR 5 (e.g., Genbank accession No. D16827) was subcloned into the mammalian expression vector pCMV (Life Technologies, Milano, Italy). Other SSTR sequences are known to the skilled artisan. Clonal cell lines stably expressing SSTR's 1-5 were obtained by transfection into CHO-KI cells (ATCC, Manassas, Va, USA) using the calcium phosphate co 30 precipitation method (Davis L, et al., 1994 In: Basic methods in Molecular Biology, 2nd edition, Appleton & Lange, Norwalk, CT, USA: 611-646). The plasmid pRSV-neo (ATCC) was included as a selectable marker. Clonal cell lines were selected in RPMI H.\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 90 1640 media containing 0.5 mg/mI of G418 (Life Technologies, Milano, Italy), ring cloned, and expanded into culture. 103381 Membranes for in vitro receptor binding assays were obtained by homogenizing the CHO-KI cells expressing the SSTR's subtypes in ice-cold 50 mM 5 Tris-HCI and centrifuging twice at 39000 g (10 min), with an intermediate resuspension in fresh buffer. The final pellets were resuspended in 10 mM Tris-HCl for assay. 103391 For the SSTR 1, 3, 4, and 5 assays, aliquots of the membrane preparations were incubated 90 minutes at 25*C with 0.05 nM [' 2 1I-Tyrl 1]SS-14 in 50 mM HEPES (pH 7.4) containing 10 mg/ml bovine serum albumin (BSA), 5 mM MgC 2 , 200 KIU/ml 10 Trasylol, 0.02 mg/ml bacitracin, and 0.02 mg/ml phenylmethylsuphonyl fluoride. The final assay volume was 0.3 ml. [03401 For the SSTR 2 assay, 0.05 nM [15I]MK-678 was employed as the radioligand and the incubation time was 90 minutes at 25 *C. The incubations were terminated by rapid filtration through GF/C glass microfibre filters (Whatman Co.) (pre 15 soaked in 0.3% polyethylenimine) using a BRANDEL filtration manifold. Each tube and filter was washed three times with 5 ml aliquots of ice-cold buffer. Specific binding was defined as the total radioligand bound minus that bound in the presence of 1000 nM SS-14 for SSTR 1, 3, 4, and 5, or 1000 nM MK-678 for SSTR2. 20 Dopamine Receptor Specificity and Selectivity Assay [03411 Specificity and selectivity for the dopamine-2 receptor of the dopamine analogues used to synthesize the somatostatin-dopamine chimers may be determined by a radioligand binding assay as follows. [03421 Crude membranes were prepared by homogenization of frozen rat corpus 25 striatum (Zivic Laboratories, Pittsburgh, PA) in 20 ml of ice-cold 50 mM Tris-HCl with a BRINKMAN POLYTRON cell disrupter (setting 6, 15 sec). Buffer was added to obtain a final volume of 40 ml, and the homogenate was centrifuged in a SORVAL SS 34 rotor at 39,000 g for 10 minutes at 0-4 *C. The resulting supernatant was decanted and discarded. The pellet was rehomogenized in ice-cold buffer, pre-incubated at 37 *C 30 for 10 min, diluted, and centrifuged as before. The final pellet was resuspended in buffer and held on ice for the receptor binding assay. H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 7/02/08 - 91 [0343] For assay, aliquots of the washed membrane preparations and test compounds were incubated for 15 minutes (37 'C) with 0.25 nM [ 3 HI]spiperone (16.5 Ci.mmol, New England Nuclear, Boston, MA) in 50 mM Tris HCl, 120 mM NaCl, 5 mM KCI, 2 mM CaCl 2 , 1 mM MgCI2. The final assay volume was 1.0 ml. The incubations were 5 terminated by rapid filtration through GF/B glass fibre filters using a Brandel filtration manifold. Each tube and filter was then washed three times with 5-ml aliquots of ice cold buffer. Specific binding was defined as the total radioligand bound minus that bound in the presence of 1000 nM (+) butaclamol. 10 Inhibition of cAMP Intracellular Production [0344] The agonist activity of a somatostatin test compound is determined by the following assay. [0345] CHO-KI cells expressing human somatostatin (SRIF-14) subtype receptors are seeded in 24-well tissue culture plates in RPMI 1640 media with 10% fetal calf 15 serum (FCS). [0346] Cells at 105 cells/well are washed 2 times by 0.5 ml RPMI 1640 media. Hank's balanced salt solution supplemented with 0.5mM 3-isobutyl-1-methylxanthine ("IBMX"), and the cells are incubated for 30 minutes at 37*C. Cyclic AMP production is stimulated by the addition of 10 ptM forskolin ("FSK") (Sigma Chemical Co., St. 20 Louis, MO) for 30 minutes at 37*C. [03471 The agonist effect of a compound is measured by the addition of the test compound (1010 M to 10-6 M) for five minutes prior to the addition of FSK (10 p.M). The reaction is terminated by the addition of 500 ul of ice-cold absolute alcohol, and the supernatant is transferred to a 12x75 mm glass tube for cAMP determination. cAMP is 25 measured using radioimmunoassay kit (Perkin-Elmer, Boston, MA). Other Embodiments [0348] Various modifications and variations of the described method and system of the invention will be apparent to those skilled in the art without departing from the 30 scope and spirit of the invention. Although the invention has been described in connection with specific desired embodiments, it should be understood that the invention as claimed should not be unduly limited to such specific embodiments. R:\MaraR\Keep\Speci\P64463-div-SPECI.doC 7/02/08 - 92 Indeed, various modifications of the described modes for carrying out the invention that are obvious to those skilled in the fields of medicine, immunology, pharmacology, endocrinology, or related fields are intended to be within the scope of the invention. [03491 All publications mentioned in this specification, including PCT/US02/17859, 5 are herein incorporated by reference to the same extent as if the disclosure of each independent publication was explicitly provided herein. In the claims which follow and in the preceding description of the invention, except where the context requires otherwise due to express language or necessary implication, the word "comprise" or variations such as "comprises" or 10 "comprising" is used in an inclusive sense, ie. to specify the presence of the stated features but not to preclude the presence or addition of further features in various embodiments of the invention. It is to be clearly understood that although prior art publication(s) are referred to herein, this reference does not constitute an admission that any of these 15 documents forms part of the common general knowledge in the art in Australia or in any other country. H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08

Claims (8)

1. A method of treating acromegaly in a subject in need thereof, wherein said 5 method comprises administering to said subject a therapeutically effective amount of a chimeric analog, wherein said chimeric analog comprises a compound according to the formula of: Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X) as set forth herein; or a pharmaceutically acceptable salt thereof; 10 wherein the compound is selected from: Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , DopIO-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11 -DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 13-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop5-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 2601322_1 (GHMatters) 14/03/11 - 94 Dop I 0-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 12 -cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 2-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5 13-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop5-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop7-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop9-D2Na-cyclo[Cys-Tyr-DTrp-Lys-Va-Cys]-Thr-NH 2 , 10 Dop 1 O-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 12 -D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 2-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I 3-D2Na-cyclo[Cys-Tyr-DTrp-Lys-Va-Cys]-Thr-NH 2 , Dop5-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 Dop6-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop9-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 0-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 20 Dop 1 -cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I 2-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5 13-cyclo[Cys-Tyr-DTrp-Lys-VaT-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 25 Dop7-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop8-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 O-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 12 -DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 30 Dop I 2-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5 3-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5\-cyclo[Cys-Phe-DTMe-Lys-Thr-Cys]-Thr-oi, H:\maraR\Keep\speci\P64463-div-SPECI .doc 13/02/08 - 95 Dop6-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, Dop7-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, Dop8-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, Dop9-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, 5 Dop 1 0-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop I 2-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 3-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, Dop5 -DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 10 Dop6-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop7-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , Dop8-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , Dop9-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop I O-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 15 Dop I11 -DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop I 2-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , Dop 1 3-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop5 -cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop6-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 20 Dop7-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop9-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop I 0-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop I1I -cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 25 Dop I 2-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopl 13-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 26013221 (GHMatterS) 14/03/11 - 96 Dop5 -DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 5 Dop7-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-N H 2 , Dop8-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I O-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I11 -DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop 1 2-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I 3-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5 -cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop8-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 0-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , DopI 1-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I2-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 Dopi 3-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop6-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(BzI)-Tyr-NH 2 , 2601322 _1 (Omattera) 14/03/11 - 97 Dop7-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 5 Dop8-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop9-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bz)-Tyr-NH 2 , Dop 1 O-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop 11 -Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop 1 2-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , 10 Dop 1 3-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop5-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop6-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , Dop7-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop8-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , 15 Dop9-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop 1 0-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , DopI 11-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , DoplI2-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop13 -Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-SerBzl)-Tyr-NH 2 , 20 Dop5 -cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop6-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop7-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop8-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop9-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , 25 DopI1O-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop I1-cyclollCys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dopl12-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , 30 2601322_1 (GHmatters) 14/03/11 - 98 Dop1 3-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop5-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys)-Thr-NH 2 , Dop7-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop8-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 O-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11 -DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 2-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop 13-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop9-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 0-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11 -cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 2-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 13 -cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl-Lys(Dop1)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dop1)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 99 Dopl -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop 1 -Lys(Dop 1)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -DLys(Dop 1)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop 1 -DLys(Dop 1)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -DLys(Dop 1)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop I -DLys(Dop I)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 10 Dop I -Lys(Dop I)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys) -Thr-NH 2 , Dop 1 -Lys(Dop 1)-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys) -Thr NH 2 , Dop I -Lys(Dop 1)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , 15 Dop I -Lys(Dop I)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop 1 -Lys(Dop I )-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop 1 -Lys(Dop 1 )-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal NH 2 , Dop I -Lys(Dop 1)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 20 Dop 1 -Lys(Dop I)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl -Lys(Dopl)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop1 -Lys(Dop1)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop1 -Lys(Dop1)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop1 -Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 25 DopI-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dopl -Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop 1 -Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 100 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 5 NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 10 NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, 15 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, 20 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 25 Dop2-Lys(Dop2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop2-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 30 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 101 Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 5 NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop3-DLys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop3-DLys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, 15 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, 20 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 25 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop3-Lys(Dop3)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp 30 NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 102 Dop4-Lys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 5 Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 10 NH 2 , Dop4-DLys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr 15 NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal 20 NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop4-Lys(Dop4)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 25 Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop4-Lys(Dop4)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , 30 Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 103 Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop5-DLys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop5-Lys(Dop5)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH 2 , 15 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 20 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, 25 Dop5-Lys(Dop5)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 104 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 5 NH 2 , Dop6-DLys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr 10 NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal 15 NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 20 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop6-Lys(Dop6)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , 25 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-DLys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-DLys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop7-Lys(Dop7)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 105 Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-Lys(Dop7)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 5 Dop7-Lys(Dop7)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-DLys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-DLys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop8-Lys(Dop8)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 15 Dop8-Lys(Dop8)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop8-Lys(Dop8)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop9-DLys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-DLys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys)-2Nal-NH 2 , 25 Dop9-Lys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-Lys(Dop9)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys)-Trp-NH 2 , Dop9-Lys(Dop9)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 30 DopIO-Lys(Dop1)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop1O-Lys(Dop10)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop10-DLys(Dop10)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 106 Dopl 0-DLys(Dop1 0)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop1 0-Lys(Dop 1 0)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 10-Lys(Dop1 0)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop1 0-Lys(Dop 1 0)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop10-Lys(Dop10)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop10-Lys(Dop10)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop10-Lys(Dop10)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop1 0-Lys(Dop1 0)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 10 DopI0-Lys(Dop10)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 11 -Lys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl1 -Lys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11 -DLys(Dop11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dopl l)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop 11 -Lys(Dop1 1)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop 11-Lys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 11-Lys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopl -Lys(Dop l1)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 20 Dopl1 -Lys(Dop 11 )-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 11 -Lys(Dop 11 )-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopi1 -Lys(Dopl 1)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop 11-Lys(Dop 11)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, 25 Dop12-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-DLys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-DLys(Dopl2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopi 2-Lys(Dop 1 2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dopl 2-Lys(Dop 1 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop1 2-Lys(Dop 1 2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopl 2-Lys(DopI 2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 107 Dop I 2-Lys(Dop 1 2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, DopI 2-Lys(Dop 1 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 1 2-Lys(Dop 12)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 13-Lys(Dop 13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop 1 3-Lys(Dop 1 3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 13-DLys(Dop1 0)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 13-DLys(Dop 13)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 13-Lys(Dop 13)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Dop 13-Lys(Dop 1 3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I 3-Lys(Dop 1 3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 13-Lys(Dop 1 3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop 13-Lys(Dop 13)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 13-Lys(Dop 1 3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 15 Dop 1 3-Lys(Dop 1 3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop13-Lys(Dop13)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 1 -Lys(Dop 1)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop1-Lys(Dop1)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop I -DLys(Dop 1)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr 20 NH 2 , Dopl-DLys(Dop1)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop 1 -Lys(Dop I)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop1-Lys(Dop1)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 25 NH 2 , Dopl-DLys(Dopl)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop1-DLys(Dop1)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 30 Dop I -Lys(Dop I)-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 108 Dop 1 -Lys(Dop 1 )-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH- 2 , Dop I -DLys(DoplI)-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp-Lys- DCys] -Thr(Bz) Tyr-NH 2 , 5 Dop 1 -DLys(Dop 1 )-Aepa-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , Dop I -Lys(Dop I )- Lys-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dopi. -Lys(Dop l)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI) 10 Tyr-NH 2 , Dop 1 -DLys(Dop 1 )-Lys-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys] Thr(Bzl)-Tyr-NH 2 , Dop I -DLys(Dop 1 )-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] Ser(Bzl)-Tyr-NH 2 , 15 Dop2-Lys(Dop2)-Caeg-cycloIIDCys-3Pal-DTrp-Lys-DCys]-Thr(BzO)-Tyr-NH2, Dop2-Lys(Dop2)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop2-DLys(Dop2)-Caeg-cyc lo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop2-DLys(Dop2)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, 20 Dop2-Lys(Dop2)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop2-Lys(Dop2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop2-DLys(Dop2)- Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI)-Tyr 25 NH 2 , Dop2-DLys(Dop2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , Dop2-Lys(Dop2)-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DC ys] -Thr(Bzl)-Tyr NH- 2 , 30 Dop2-Lys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , H:\maraR\Keep\speci\P64463-div-SPECI.doc 13/02/08 - 109 Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , 5 Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz) Tyr-NH 2 , Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclIo [DCys-3 PalI-DTrp-Lys- DCys] 10 Thr(13zi)-Tyr-NH 2 , Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] Ser(Bzl)-Tyr-NH 2 , Dop3-Lys(Dop3)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2, Dop3 -Lys(Dop3)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, 15 Dop3 -Lys(Dop3)- Lys-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(BzO-Tyr NH 2 , Dop3 -Lys(Dop3)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop3 -Lys(Dop3)-Aepa-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys] -Thr(BzI)-Tyr 20 NH 2 , Dop3 -Lys(Dop3)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH- 2 , Dop3 -DLys(Dop3 )-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH- 2 , 25 Dop3-DLys(Dop3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop3 -DLys(Dop3)- Lys-Caeg-cycl o[DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH- 2 , Dop3 -DLys(Dop3)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , 30 Dop3 -DLys(Dop3 )-Aepa-Caeg-cyc lo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , H:\MaraR\Keep\speci\P64463-div-SPECI.doc 13/02/08 - 110 Dop3 -DLys(Dop3)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl) Tyr-NH 2 , Dop4-Lys(Dop4)-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 , Dop4-Lys(Dop4)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , 5 Dop4-Lys(Dop4)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 Dop4-Lys(Dop4)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCysJ-Ser(Bzl)-Tyr NH 2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCysJ -Thr(BzI)-Tyr 10 NH 2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(BzI) Tyr-NH 2 , 15 Dop4-Lys(Dop4).-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , Dop4-DLys(Dop4)-Caeg-cyc lo [DCys- 3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop4-DLys(Dop4)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr-NH 2 , 20 Dop4-DLys(Dop4)-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop4-DLys(Dop4)-Lys-Caeg-cyclo [DCys-.Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH- 2 , Dop4-DLys(Dop4)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl) 25 Tyr-NH 2 , Dop4-DLys(Dop4)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl) Tyr-NH- 2 , Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] Thr(BzI)-Tyr-NH 2 , 30 Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] Ser(BzI)-Tyr-NH 2 , Dop5 -Lys(Dop5)-Caeg-cyc lo [DCys-3 PalI-DTrp- Lys-DC ys] -Thr(BzI)-Tyr-N H 2 , H:\maraR\Keep\speci\P64463-div-SPECI.doc 13/02/08 Dop-Ls(op5-Cegcyco[~-P11-Dr-yDysSe(z)T-N2 Dop5 -Lys(Dop5)-Caeg-cycloDCys-Pe-DTrp-Lys-DCys] -er(Bzl)-Tyr- 2 NH 2 , Dop5-DLys(Dop5)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys-Ser(Bz)-Tyr-NH2, 5 DopS-Lys(Dop5)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop5-Lys(Dop5)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop5 -DLys(Dop5)-Lys-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-Tyr 10 NH4 2 , Dop5 -DLys(Dop5)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop6-Lys(Dop6)-Caeg-cyc lo [DCys-3 Pal -DTrp-Lys-DCys] .Thr(Bzl)-Tyr-N H 2 , Dop6-Lys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, 15 Dop6-DLys(Dop6)-Caeg-cyc lo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop6-DLys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop6-Lys(Dop6)-Lys-Caeg-cyclolDCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , 20 Dop6-Lys(Dop6)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop6-DLys(Dop6)-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH- 2 , Dop6-DLys(Dop6)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 25 NH- 2 , Dop7-Lys(Dop7)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2, Dop7-Lys(Dop7)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop7-Lys(Dop7)-Lys-Caeg-cyclo[DCys-3 PaI-DTrp-Lys-DCys]-Thr(BzI)-Tyr NH- 2 , 30 Dop7-Lys(Dop7)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCysI-Ser(BzI)-Tyr NH- 2 , Dop8-Lys(Dop8)-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys]-Thr(BzI)-Tyr-NH2, H* \MaraR\Keep\Speci\P64463-div-SPECI .doc 13/02/08 - 112 Dop8-Lys(Dop8)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop8-Lys(Dop8)-Lys-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop8-Lys(Dop8)-Lys-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr 5 NH 2 , Dop9-Lys(Dop9)-Caeg-cyc lo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop9-Lys(Dop9)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop9-Lys(Dop9)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , 10 Dop9-Lys(Dop9)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , Dop I O-Lys(Dop 1 O)-Caeg-cyclollDCys-3 Pal-DTrp-Lys-DCys]l-Thr(BzI)-Tyr NH 2 , Dop I O-Lys(Dopl 1 )-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr 15 NH 2 , Dopl O-Lys(DoplI 0)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , Dop 1 0-Lys(Dopl I )-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , 20 Dopl 11-Lys(Dopl 11)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop I 1 -Lys(Dopl I l)-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , DopI I -Lys(Dopl I1)-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI) 25 Tyr-NH 2 , Dop 11I -Lys(Dop 11 )-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop I 2-Lys(Dop I 2)-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , 30 Dopl2-Lys(Dopl 2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , IA \maraR\Keep\speci\P64463-div-SPECI .doc 13/02/08 - 113 Dop I 2-Lys(Dop 1 2)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , Dop 1 2-Lys(Dop I 2)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 5 Dop I 3-Lys(DoplI3)-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bz)-Tyr NH 2 , Dop I 3-Lys(Dop 1 3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop I 3-Lys(Dopl 3)-Lys-Caeg-cyclo [DCys-3 Pal- DTrp- Lys-DCys] -Thr(Bz) 10 Tyr-NH- 2 , Dop 1 3-Lys(Dop 1 3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH- 2 , Dop 1 -Lys(Dop 1 )-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , DoplI -Lys(Dop 1 )-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , 15 Dopl1 -DLys(Dop 1 )-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop 1 -DLys(Dopl1)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop 1 )-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopi. -DLys(Dopl )-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-CysI-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , 20 Dop2-Lys(Dop2)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-DLys(Dop2)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-Lys(Dop2)-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-DLys(Dop2)-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop3 -Lys(Dop3)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop3 -Lys(Dop3 )-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop3 -Lys(Dop3)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop4-Lys(Dop4)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, 30 Dop4-Lys(Dop4)-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop5 -Lys(DopS)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , HE\MaraR\Keep\speci\P64463-div-SPECi .doc 13/02/08 - 114 Dop5-DLys(Dop5)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop5-Lys(Dop5)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop6-Lys(Dop6)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop6-DLys(Dop6)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop6-Lys(Dop6)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop6-DLys(Dop6)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop8-Lys(Dop8)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 15 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 10-Lys(Dop 1 0)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop O-Lys(Dop1 0)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 DopI 1-Lys(Dop I1)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop 11-Lys(Dop 11)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop12-Lys(Dopl2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop13-Lys(Dop13)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 25 Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl-DPhe-cyclo[Cys-3ITyr(Dop1)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DPhe-Doc-DPhe-cyclo[Cys-31Tyr(Dopl)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop] -DLys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 115 Dopl -Lys(Dop l)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop I)-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 5 Dop I -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop 1 -DLys(Dop 1)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dopl -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , 10 Dopl -DLys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 , Dopl -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr 20 NH 2 , Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dopl -DLys(Dop I )-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , 25 Dopl -DLys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 116 Dop I -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop 1 -DLys(Dop l)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DLys(Dop 1)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr 5 NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys}-Thr-NH 2 , 15 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , 20 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys] Thr-NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , 25 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 117 Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr 5 NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-31Tyr-DTrp-Lys-Val-Cys]-Thr 20 NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Aepa-DPhe-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop5-DLys(Dop5)-DPhe-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 118 Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr 15 NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH2, 20 Dop5-DLys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 25 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-CysI-Thr NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop9-Lys(Dop9)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 O-Lys(Dop 1 0)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11-Lys(Dop 11)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 119 Dop I 2-Lys(Dop I 2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 13-Lys(Dop I 3)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop6-Lys(Dop6)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop O-Lys(Dop 1 0)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop 11-Lys(Dop 11)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop12-Lys(Dopl2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or Dopl 3-Lys(Dop13)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]- Thr-NH 2 ; or a pharmaceutically acceptable salt thereof; wherein said therapeutically effective amount is the amount effective to treat 15 acromegaly in said patient.
2. The method of claim 1, wherein said chimeric analog comprises a SSTR-5 agonist and a dopamine receptor agonist. 20
3. The method of claim 2, wherein said chimeric analog further comprises a SSTR 2 agonist.
4. A method of treating hyperprolactinemia in a subject in need thereof, wherein said method comprises administering to said subject a therapeutically effective 25 amount of a chimeric analog, wherein said chimeric analog comprises a compound according to the formula of: Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X) as set forth herein; or a pharmaceutically acceptable salt thereof; wherein the compound is selected from: 30 2601322_1 (GHMatters) 14/03/11 - 120 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop8-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 O-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11 -DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop1 2-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop 13-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop9-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop1 0-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop II -cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop1 2-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl 3-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop5-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop7-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop9-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 25 Dop O-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 11 -D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I 2-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 13-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 2601322_1 (GHMatters) 14/03/11 - 121 Dop6-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop7-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop9-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, 5 Dop 1 0-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I1I -cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop 1 2-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dopl 13-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, 2.0 Dop6-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop7-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop8-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop9-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop I O-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 15 Dop 11I -DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 2-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dopl 13-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, Dop5-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 20 Dop7-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop8-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop9-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop IO-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, Dop I11 -cyclo [Cys-Phe-DTrp-Lys-Thr-Cysl-Thr-oI, 25 Dopl12-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, Dop13 -cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop6-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop7-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 30 Dop8-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , DopI1O-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI .doc 13/02/08 - 122 Dop I I -DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , Dop I 2-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-CysI-2Nal-NH 2 , 5 Dop 1 3-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop5-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop6-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop7-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop8-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 10 Dop9-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , Dop I 0-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH2, Dop I1I -cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 1 2-cyclo [Cys-Tyr-DTrp-Lys-.Thr-Cys]-2Nal-NH 2 , Dop I 3-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , 15 Dop5-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop6-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop8-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop9-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dopl O-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH2, Dopl 11-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I2-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 13 -DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop5 -cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 26013221 (GI4Matters) 14/03/11 - 123 5 Dop6-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop7-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop9-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I O-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 10 DopI 1-cyclo[Cys-31ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl12-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I 3-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop5 -Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop6-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 15 Dop7-Caeg-cyclo[DCys-3 PaI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop8 -Caeg-cyclo [DCys- 3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop9-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop 1 O-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dopl 11-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 20 Dop 12 -Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop 13 -Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 26013221 (GHJatters) 14/03/11 - 124 Dop5-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop6-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop7-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 5 Dop8-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop9-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop O-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop 11 -Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop I 2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 10 DopI 3-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-SerBzl)-Tyr-NH 2 , Dop5-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop6-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop7-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop8-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 15 Dop9-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop 1 0-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dopl 1-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop1 2-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop 13-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 20 Dop5-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop O-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl1 -DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 2-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 13-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop6-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 2601322_1 (GHMatters) 14/03/11 - 125 Dop9-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 O-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I1-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I 2-cycloI[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , 5 Dopl 13-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-Lys(Dop2)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , 15 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]l-Thr-NH 2 , Dop 1 -Lys(DoplI)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop I -Lys(Dopl1)-Aepa-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dopl1)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop 1 -Lys(Dopl1)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 20 NH 2 , Dop 1 -Lys(Dop 1 )-DTyr-DTyr-cyclojlCys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop 1 -DLys(Dopl1)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop I -DLys(Dop I )-Aepa-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop 1 -DLys(Dop I )-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-N H 2 , 25 Dop 1 -DLys(Dop I )-Lys-DTyr-DTyr-cyclo [Cys-Tyr- DTrp-Lys-Abu-Cys] -Thr NH 2 , Dop 1 -DLys(Dop 1 )-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop I -Lys(Dop 1 )-D2N al-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop I -Lys(Dop 1 )-cyclo [Cys-Tyr-DTrp-Lys-Val -Cys] -Thr-N H 2 , 30 Dop 1 -Lys(Dop 1 )-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Va1-Cys] -Thr NH 2 , Dop 1 -Lys(Dop I )-DTyr-DTyr-cyclo [Cys-Tyr- DTrp-Lys-Va1 -Cys] -Thr-NH 2 , H:\maraR\Keep\sp~eci\P64463-div-SPECI .doc 13/02/08 - 126 Dop I -Lys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop I -Lys(Dop l)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop I -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , 5 Dop I -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 1 -Lys(Dop l)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop I -Lys(Dop l)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop I -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 10 Dop I -Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 1 -Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 1 -Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop 1 -Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, 15 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 20 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 30 NH 2 , Dop2-Lys(Dop2)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 127 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 5 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys}-2Nal-NH2, Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 10 Dop2-Lys(Dop2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop2-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, 15 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop3-DLys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop3-DLys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop3-Lys(Dop3)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 128 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 5 Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 10 Dop3-Lys(Dop3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop3-Lys(Dop3)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 15 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop4-DLys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop4-DLys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop4-Lys(Dop4)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 129 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 5 Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys)-Thr-ol, 10 Dop4-Lys(Dop4)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop4-Lys(Dop4)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 15 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop5 -Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, 25 Dop5-DLys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 130 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal 5 NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5 -Lys(Dop5)-cyclolCys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-o, 10 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop5-Lys(Dop5)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , 15 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 20 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 25 Dop6-DLys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , 30 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 131 Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 5 Dop6-Lys(Dop6)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop6-Lys(Dop6)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 10 Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop7-DLys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-DLys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, 20 Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-Lys(Dop7)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys)-Trp-NH2, Dop7-Lys(Dop7)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 25 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop8-DLys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-DLys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, 30 Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 132 Dop8-Lys(Dop8)-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop8-Lys(Dop8)-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, Dop8-Lys(Dop8)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop8-Lys(Dop8)- cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 , 5 Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop9-Lys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop9-DLys(Dop9)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-DLys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop9-Lys(Dop9)-D2Na1-cyclo[Cys-Tyr-DTrp-Lys-Va-Cys]-Thr-NH2, 10 Dop9-Lys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Val -Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , Dop9-Lys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop9-Lys(Dop9)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, 15 Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop9-Lys(Dop9)- cyclo[Cys-Tyr-DTrp-Lys-VaI-Cys] -Trp-NH 2 , DopI1O-Lys(DoplIO)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, DopI1O-Lys(Dopl1 )-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop IO-DLys(Dop 1O)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 20 Dop IO-DLys(Dopl1 )-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, DopI1O-Lys(Dopl1O)-D2Na-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , DopI1O-Lys(Dopl1 )-cyclo[Cys-Tyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 , Dop IO-Lys(DoplIO)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , 25 Dop IO-Lys(DoplI )-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop IO-Lys(DoplIO)-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, DopI1O-Lys(DoplI )-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, Dop IO-Lys(DoplIO)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 , DopI1 -Lys(Dop 10)- cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 , 30 Dopl 11-Lys(Dopl 11)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop I -Lys(Dopl Ii)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop I I -DLys(Dop 11 )-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , H:\maraR\Keep\speci\P64463-div-SPECI.doc 13/02/08 - 133 Dopl 1-DLys(Dopl l)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop 1l)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 11 -Lys(Dop 11 )-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop 1 I-Lys(Dop 11 )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop I I-Lys(Dop ll)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopl I -Lys(Dopl l)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 11-Lys(Dop 11)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl -Lys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 10 Dop 11 -Lys(Dop 11)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-DLys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-DLys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop12-Lys(Dop12)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop12-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 20 Dop12-Lys(Dop12)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop12-Lys(Dop12)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-Lys(DopI3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop13-DLys(Dop1O)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-DLys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-Lys(Dop13)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop13-Lys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop13-Lys(DopI3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 134 Dop 13-Lys(Dop 1 3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 13-Lys(Dop 13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop13-Lys(Dop13)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop I -Lys(Dop I)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 5 Dop I -Lys(Dop I)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop 1 -DLys(Dop 1)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop 1 -DLys(Dop 1)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop 1 -Lys(Dop I)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr 10 NH 2 , Dop 1 -Lys(Dop I )-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop 1 -DLys(Dop 1)-Lys-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 15 Dop 1 -DLys(Dop 1 )-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , DopI -Lys(Dop I)-Aepa-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop I -Lys(Dop 1)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys)-Ser(Bz)-Tyr 20 NH 2 , Dop I -DLys(Dop 1)-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , Dop 1 -DLys(Dop 1)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , 25 Dopl -Lys(Dopl)-Lys-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , Dop 1 -Lys(Dop l)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , Dop 1 -DLys(Dop l)-Lys-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys] 30 Thr(Bzl)-Tyr-NH 2 , Dop 1 -DLys(Dop 1)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] Ser(Bzl)-Tyr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 135 Dop2-Lys(Dop2)-Caeg-cyc lo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop2-Lys(Dop2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop2-D Lys(Dop2)-Caeg-cyclo [DCys-3 Pal- DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 5 Dop2-DLys(Dop2)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop2-Lys(Dop2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , 10 Dop2-DLys(Dop2)-Lys-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop2-DLys(Dop2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop2-Lys(Dop2)-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI)-Tyr 15 NH 2 , Dop2-Lys(Dop2)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , 20 Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(BzI) Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI) 25 Tyr-NH 2 , Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] Thr(BzI)-Tyr-NH 2 , Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] Ser(Bzl)-Tyr-NH 2 , 30 Dop3 -Lys(Dop3)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop3 -Lys(Dop3)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , H:\maraR\Keep\speci\P64463-div-SPECI .doc 13/02/08 - 136 Dop3-Lys(Dop3)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop3-Lys(Dop3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 5 Dop3 -Lys(Dop3)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop3-Lys(Dop3)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop3-DLys(Dop3)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr 10 NH 2 , Dop3-DLys(Dop3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop3-DLys(Dop3)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop3-DLys(Dop3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 15 NH 2 , Dop3 -DLys(Dop3)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop3-DLys(Dop3)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , 20 Dop4-Lys(Dop4)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys)-Thr(Bzl)-Tyr-NH2, Dop4-Lys(Dop4)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop4-Lys(Dop4)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 Dop4-Lys(Dop4)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 25 NH 2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 30 Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 137 -I Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , Dop4-DLys(Dop4)-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys]-Thr(BzI)-Tyr NH 2 , 5 Dop4-DLys(Dop4)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop4-DLys(Dop4)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop4-DLys(Dop4)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 10 Dop4-D Lys(Dop4)-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop4-DLys(Dop4)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp- Lys- DCys] 15 Thr(Bzl)-Tyr-NH 2 , Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] Ser(BzI)-Tyr-NH 2 , Dop5 -Lys(Dop5)-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop5-Lys(Dop5).-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, 20 Dop5 -DLys(Dop5)-Caeg-cyclo [DCys-3 Pal- DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop5-DLys(Dop5 )-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, Dop5 -Lys(Dop5)-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 25 Dop5-Lys(Dop5)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr NH- 2 , Dop5 -DLys(Dop5 )-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH1 2 , Dop5 -DLys(Dop5).-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr 30 NH 2 , Dop6-Lys(Dop6)-Caeg-cyc lo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop6-Lys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , 14\MaraR\Keep\Speci\P64463-div-SPECI .doc 13/02/08 - 138 Dop6- DLys(Dop6)-Caeg-cyclo [DCys-3 Pal -DTrp-Lys- DCys] -Thr(Bzl)-Tyr NH- 2 , Dop6-DLys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , Dop6-Lys(Dop6)-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI)-Tyr 5 NH 2 , Dop6-Lys(Dop6)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop6-DLys(Dop6)- Lys- Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DC ys] -Thr(Bzl)-Tyr NH 2 , 10 Dop6-DLys(Dop6)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop7-Lys(Dop7)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , Dop7-Lys(Dop7)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , Dop7-Lys(Dop7)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr 15 NH 2 , Dop7-Lys(Dop7)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop8- Lys(Dop8)-Caeg-cyc lo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bz)-Tyr-N H2, Dop8-Lys(Dop8)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, 20 Dop8 -Lys(Dop 8)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop8-Lys(Dop8)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop9.-Lys(Dop9)-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 25 Dop9-Lys(Dop9)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop9-Lys(Dop9)-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop9-Lys(Dop9)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , 30 Dop 1 O-Lys(Dop 1 O)-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH- 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI .doc 13/02/08 - 139 Dop1 O-Lys(Dop I 0)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , Dop I O-Lys(Dop1 0)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , 5 DopI O-Lys(Dop 1 0)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop I -Lys(Dop I )-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop 11 -Lys(Dop ll)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 10 NH 2 , Dop 11-Lys(Dop 11)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , Dop II -Lys(Dop ll)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 15 Dop 1 2-Lys(Dop I 2)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop1 2-Lys(Dop 1 2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop1 2-Lys(Dopl2)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) 20 Tyr-NH 2 , Dop 1 2-Lys(Dop1 2)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop 13-Lys(Dop 1 3)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , 25 Dop I3-Lys(DopI3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dopi 3-Lys(Dopl3)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , Dop1 3-Lys(Dop13)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 30 NH 2 , Dop1 -Lys(Dopl)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop 1 -Lys(Dop1)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 140 Dop 1 -DLys(Dop l)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop I -DLys(Dopl)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -Lys(Dopl)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I -DLys(Dop l)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop2-Lys(Dop2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop2-DLys(Dop2)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop4-Lys(Dop4)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 15 Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 20 Dop5-DLys(Dop5)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop5-Lys(Dop5)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop6-DLys(Dop6)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop6-DLys(Dop6)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 30 Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 141 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 O-Lys(Dop 1 0)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 5 Dopl O-Lys(Dop 1 0)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11-Lys(Dop 11)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop 11 -Lys(Dop 11)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dopl3-Lys(Dop13)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop1-DPhe-cyclo[Cys-3ITyr(Dopl)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dopl)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 Dop1-DLys(Dop1)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1-DLys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1-Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1-Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 DopI-Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1-DLys(Dop1)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl-Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , 25 Dop 1 -DLys(Dop 1)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I -DLys(Dop I)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr NH 2 , Dop I -DLys(Dop 1)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -DLys(Dop 1)-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr 30 NH 2 , Dop] -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 142 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dopl -DLys(Dop I )-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr 10 NH 2 , Dopl -DLys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1-Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl-Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr 20 NH 2 , Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 25 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , 30 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 143 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr 5 NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys] Thr-NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr 10 NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-31Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr 25 NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 144 Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys)-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH2, 5 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop4-Lys(Dop4)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop5-DLys(Dop5)-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3]Tyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 30 Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 145 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3lTyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr 10 NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop7-Lys(Dop7)-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 10-Lys(Dop 1 0)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11-Lys(Dop 11)-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop12-Lys(Dop12)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop13-Lys(Dop13)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop9-Lys(Dop9)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , DopIO-Lys(Dop1O)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11-Lys(Dop 11)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or Dop13-Lys(Dop13)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]- Thr-NH 2 ; or a 30 pharmaceutically acceptable salt thereof, wherein said therapeutically effective amount is the amount effective to treat prolactinemia in said patient. H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 146 5. The method of claim 4, wherein said chimeric analog comprises a SSTR-5 agonist and a dopamine receptor agonist.
5
6. The method of claim 5, wherein said chimeric analog further comprises a SSTR 2 agonist.
7. A method of treating portal hypertension in a subject in need thereof, wherein said method comprises administering to said subject a therapeutically effective 10 amount of a chimeric analog, wherein said chimeric analog comprises a compound according to the formula of: Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X) as set forth herein; or a pharmaceutically acceptable salt thereof; wherein the compound is selected from: 15 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , DopIO-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl2-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 2601322_1 (GHMatters) 14/03/11 - 147 Dop5-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop7-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop9-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop 1 0-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, 10 Dop5-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop7-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop8-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop9-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 DopI0-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 11 -D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 2-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop 1 3-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, 20 Dop6-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop8-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop9-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop I 0-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 25 Dopl 1-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop12-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop13-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 30 Dop7-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop8-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 148 Dop 1 O-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 I-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop1 2-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 13-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 5 Dop5-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop8-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 10 Dop 1 0-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 11 -cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 2-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 13-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 15 Dop6-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop7-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 1 O-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 20 DopI I -DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop1 2-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 13-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 25 Dop7-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop9-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop I 0-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 11 -cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 30 Dop I 2-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopi 3-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 2601322_1 (GHMatters) 14/03/11 - 149 Dop5 -DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 5 Dop6-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop7-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop8-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop9-DPhe-cyclo [Cys-3 lTyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 O-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 10 Dop 11 -DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I 2-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 3-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop5-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop7-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-3 lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 0-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I I -cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop I 2-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 3-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 26013221 (GI4Matters) 14/03/11 - 150 Dop5-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 5 Dop6-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop7-Caeg-cyclo [DCys- 3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop8-Caeg-cyclo[DCys-3PaI-DTrp-Lys-DCys]-Thr(Bz)-Tyr-NH 2 , Dop9-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop I O-Caeg-cyclo [DCys-3 Pal -DTrp-Lys- DCys] -Thr(Bzl)-Tyr-NH 2 , 10 DopI 11-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dopi 2-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop 1 3-Caeg-cyclo[DCys-3PaI-DTrp-Lys-DCys]-Thr(Bz)-Tyr-NH 2 , Dop5-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , Dop6-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , 15 Dop7-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop8-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , Dop9-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop I O-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop I1-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , 20 DoplI2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop I 3-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-SerBz)-Tyr-NH 2 , Dop5-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop6-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop7-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 26013221 (GHMatters) 14/03/11 - 151 Dop8-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop9-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop I 0-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop 11-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 5 Dop 1 2-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop 13-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop5-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop7-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, 10 Dop8-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I O-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11 -DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 2-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop 13-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop5-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop9-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I 0-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 12-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 2-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop2 3-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Tin-NH 2 , 30 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 152 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dopl -Lys(Dop l)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop l)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop I -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop I -DLys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 15 Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , 20 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopl -Lys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , 25 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopl -Lys(Dopl)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl -Lys(Dopl)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 30 Dop I -Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, DopI-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 153 Dop 1 -Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop 1 -Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, 10 Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys-Thr-NH2, Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 20 Dop2-Lys(Dop2)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, 25 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 30 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 154 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop2-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp 5 NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, 15 Dop3-DLys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop3-DLys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 20 Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 25 Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 30 Dop3-Lys(Dop3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 155 Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys)-Trp-NH 2 , Dop3-Lys(Dop3)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys)-Trp NH 2 , 5 Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 10 NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop4-DLys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop4-DLys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop4-DLys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 20 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, 25 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop4-Lys(Dop4)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 30 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 156 Dop4-Lys(Dop4)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, 5 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 10 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 15 Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop5-Lys(Dop5)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , 20 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , 25 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 30 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop5-Lys(Dop5)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 157 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop6-DLys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop6-DLys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 20 Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 25 Dop6-Lys(Dop6)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop6-Lys(Dop6)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 30 Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 158 Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop7-DLys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-DLys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop7-Lys(Dop7)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 10 Dop7-Lys(Dop7)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop7-Lys(Dop7)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop8-DLys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-DLys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, 20 Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop8-Lys(Dop8)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop8-Lys(Dop8)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 25 Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-DLys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-DLys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop9-Lys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 159 Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-Lys(Dop9)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop9-Lys(Dop9)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 5 Dop10-Lys(Dop10)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop1O-Lys(Dop10)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop10-DLys(Dop10)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop10-DLys(Dop10)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop10-Lys(Dop1O)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop10-Lys(Dop10)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop10-Lys(Dop10)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop1O-Lys(Dop10)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop1O-Lys(Dop1)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 15 DopI0-Lys(Dop10)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop10-Lys(Dop10)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop10-Lys(Dop10)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 11 -Lys(Dop I 1)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop 11 -Lys(Dop1 1)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dopl I -DLys(Dopl l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I -DLys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11 -Lys(Dop 11 )-D2Nal-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop 11 -Lys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 25 Dop 11-Lys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopi I -Lys(Dopl 1)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop 11-Lys(Dop 11)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 11 -Lys(Dop 11 )-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop I-Lys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 30 Dop I-Lys(DopI I)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys)-Trp-NH2, Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , DopI2-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 160 Dop I 2-DLys(Dop 1 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop 1 2-DLys(Dop1 2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 2-Lys(Dop 2)-D2Na1-cyclo[Cys-Tyr-DTrp-Lys-Va-Cys]-Thr-NH 2 , DopI 2-Lys(Dop 1 2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop 1 2-Lys(Dop 1 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop I 2-Lys(Dop 1 2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop 1 2-Lys(Dop1 2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-o , Dop 1 2-Lys(Dop1 2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop 1 2-Lys(Dop 1 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 10 Dop12-Lys(Dopl2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-Lys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-DLys(Dop1)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-DLys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop13-Lys(Dop13)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop13-Lys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop13-Lys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 20 Dop13-Lys(DopI3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop13-Lys(Dop13)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop13-Lys(DopI3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop13-Lys(Dop13)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 1 -Lys(Dop 1)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 25 Dop1-Lys(Dopl)-Caeg-cyclo(DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop 1 -DLys(Dop I)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop1-DLys(Dop1)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop 1 -Lys(Dop 1)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr 30 NH 2 , Dop1-Lys(Dopl)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , H:\Mar&R\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 161 Dop 1 -DLys(DoplI)-Lys-Caeg-cyclo[DCys-3 Pa1-DTrp-Lys-DCys]-Thr(Bz1)-Tyr NH 2 , Dop I -DLys(Dop 1 )-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 5 Dop 1 -Lys(Dop 1 )-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop I -Lys(Dop 1 )-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , Dop 1 -DLys(Dop 1 )-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI) 10 Tyr-NH 2 , Dop 1 -DLys(Dop I )-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , Dop I -Lys(Dop I )-Lys-Aepa-Caeg-cyc lo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , 15 Dop I -Lys(Dop I )-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bz) Tyr-NH 2 , Dop I -DLys(Dop 1 )-Lys-Aepa-Caeg-cyc lo [DCys- 3 Pal-DTrp- Lys- DCys] Thr(BzI)-Tyr-NH 2 , Dop 1 -D Lys(Dop I )-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp- Lys-DCys] 20 Ser(Bzl)-Tyr-NH 2 , Dop2-Lys(Dop2)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop2-Lys(Dop2)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop2-DLys(Dop2)-Caeg-cyclo [DCys-3 Pal- DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 25 Dop2-DLys(Dop2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, Dop2- Lys(Dop2)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys) -Thr(Bzl)-Tyr NH 2 , Dop2-Lys(Dop2)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr NH 2 , 30 Dop2-DLys(Dop2)-Lys-Caeg-cyc lo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , H:\Marafl\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 162 Dop2-DLys(Dop2)-Lys-Caeg-cycloIIDCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , Dop2-Lys(Dop2)-Aepa-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 59 Dop2-Lys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-N H 2 , Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl) 10 Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI) Tyr-NH 2 , 15 Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] Thr(Bzl)-Tyr-NH 2 , Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] Ser(Bzl)-Tyr-NH 2 , Dop3 -Lys(Dop3)-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bz1)-Tyr-NH2, 20 Dop3-Lys(Dop3)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bz1)-Tyr-NH2, Dop3 -Lys(Dop3)- Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop3-Lys(Dop3)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCysJ-Ser(Bzl)-Tyr NH 2 , 25 Dop3 -Lys(Dop3 )-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop3 -Lys(Dop3)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop3 -D Lys(Dop3)-Caeg-cyclo [DCys-3 Pal- DTrp-Lys- DCys] -Thr(BzI)-Tyr 30 NH 2 , Dop3 -DLys(Dop3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI .doc 13/02/08 - 163 Dop3 -DLys(Dop3 )-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH- 2 , Dop3 -DLys(Dop3)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , 5 Dop3 -DLys(Dop3 )-Aepa-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop3-DLys(Dop3)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz) Tyr-NH 2 , Dop4-Lys(Dop4)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , 10 Dop4-Lys(Dop4)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(3z1)-Tyr-NH2, Dop4-Lys(Dop4)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(BzI)-Tyr NH 2 Dop4-Lys(Dop4)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 15 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH1 2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH4 2 Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bzl) 20 Tyr-NH 2 , Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI) Tyr-NH 2 , Dop4-D Lys(Dop4)-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 25 Dop4-DLys(Dop4)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop4-D Lys(Dop4)-Lys-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop4-DLys(Dop4)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , 30 Dop4-DLys(Dop4)-Aepa-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , H:\maraR\Keep\speci\P64463-div-SPECI.doc 13/02/08 - 164 Dop4-DLys(Dop4)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI) Tyr-NH 2 , Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] Thr(Bzl)-Tyr-NH 2 , 5 Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys) Ser(Bzl)-Tyr-NH 2 , Dop5-Lys(Dop5)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2, Dop5 -Lys(Dop5)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop5 -D Lys(Dop5 )-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(BzI)-Tyr 10 NH 2 , Dop5 -DLys(Dop5)-Caeg-cycl o [DCys-Phe-DTrp- Lys- DCys] -Ser(BzI)-Tyr-NH 2 , Dop5 -Lys(Dop5)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop5 -Lys(Dop5)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr 15 NH 2 , Dop5-DLys(Dop5)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop5-DLys(Dop5)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 20 Dop6-Lys(Dop6)-Caeg-cyclo [DCys-3PaI-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2, Dop6-Lys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop6-DLys(Dop6)-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop6-DLys(Dop6)-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , 25 Dop6-Lys(Dop6)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(BzI)-Tyr NH 2 , Dop6-Lys(Dop6)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH- 2 , Dop6-DLys(Dop6)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr 30 NH 2 , Dop6-DLys(Dop6)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , H: \MaraR\Keep\Speci\P64463-div-SPECI .doc 13/02/08 - 165 Dop7-Lys(Dop7)-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop7-Lys(Dop7)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , Dop7-Lys(Dop7)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , 5 Dop7-Lys(Dop7)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop8 -Lys(Dop8)-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 , Dop8-Lys(Dop8)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop8-Lys(Dop8)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr 10 NH 2 , Dop8-Lys(Dop8)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop9- Lys(Dop9)-Caeg-cyclo [DCys-3 Pal-DTrp- Lys- DC ys] -Thr(BzI)-Tyr-N H 2 , Dop9-Lys(Dop9)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]l-Ser(Bzl)-Tyr-NH 2 , 15 Dop9-Lys(Dop9)-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop9-Lys(Dop9)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]l-Ser(Bz)-Tyr NH 2 , Dop I O-Lys(Dopl I )-Caeg-cyclo [DCys-3 Pat- DTrp-Lys-DCys] -Thr(Bzl)-Tyr 20 NH 2 , Dop 1 O-Lys(Dop 1 O)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 5 Dop I O-Lys(Dopl I )-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , 25 DopI O-Lys(DoplIO)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dopl 11-Lys(Dopl I)-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , DopI I-Lys(Dopl 11)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr 30 NH 2 , DopI 1 -Lys(Dopl 11)-Lys-Caeg-cycl o [DCys-3 PalI-DTrp- Lys-DCys] -Thr(BzI) Tyr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 166 Dop 11-Lys(Dop 11)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop 12-Lys(Dop I 2)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 5 Dopl2-Lys(Dop12)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop12-Lys(Dop1 2)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , Dop12-Lys(Dop12)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 10 NH 2 , Dop 13-Lys(Dop1 3)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , DopI 3-Lys(Dopl 3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 15 DopI 3-Lys(Dopl 3)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , DopI 3-Lys(Dopl 3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , DopI -Lys(Dopl)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, 20 DopI -Lys(Dop1)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I -DLys(Dop1)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dopl-DLys(Dop1)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -Lys(Dop1)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , DopI -DLys(Dop1)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop2-Lys(Dop2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop2-DLys(Dop2)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 167 Dop3 -Lys(Dop3)-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop4-Lys(Dop4)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, 5 Dop5-Lys(Dop5)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5 -DLys(Dop5)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , 10 Dop5-DLys(Dop5 )-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop6-DLys(Dop6)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop6-DLys(Dop6)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , 15 Dop6-Lys(Dop6)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop6-DLys(Dop6)-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop7-Lys(Dop7)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 Dop8-Lys(Dop8)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop8-Lys(Dop8)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I O-Lys(Dop 1 0)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , 25 Dop 1 O-Lys(Dopl I )-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11 -Lys(Dop 11 )-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dopl 11-Lys(Dopl 11)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dopi 2-Lys(DoplI2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dopl12-Lys(Dopl12)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop13 -Lys(Dopl13)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dopi 3-Lys(Dopl 3)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl1-DPhe-cyclo[Cys-3 ITyr(Dopl1)-DTrp-Lys-VaI-Cys] -Thr-NH 2 , H:\MaraR\Keep\speci\P64463-div-SPECI .doc 13/02/08 - 168 Dop I -DPhe-Doc-DPhe-cyclo[Cys-3 ITyr(Dop 1)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 -DLys(Dop l)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -DLys(Dop l)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dopl -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I-Lys(Dopl)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -Lys(Dop l)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I -DLys(Dop l)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop 1 -Lys(Dop l)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop 1 -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr 15 NH 2 , Dop 1 -DLys(Dop l)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dop l)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop I)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop 1 -DLys(Dop 1)-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop 1 -Lys(Dop 1)-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop 1 -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , Dop 1 -DLys(Dop 1 )-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , Dop 1 -DLys(Dop I)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr 30 NH 2 , Dop 1-DLys(Dopl)-DPhe-cyclo{Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I -DLys(Dop 1)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , H:\MaraR\Kcep\Speci\P64463-div-SPECI.doC 13/02/08 - 169 Dop 1 -Lys(DoplI)-DTyr-DTyr-cyclo [Cys-31ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 -Lys(DoplI)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I -Lys(DoplI)-Aepa-DPhe-cyclo [Cys-31ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop I -DLys(Dopl1)-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 , Dop I -Lys(Dopl1)-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 , Dop 1 -Lys(DoplI)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys]-Thr NH 2 , Dop 1 -DLys(DoplI)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH2, 10 Dop 1 -DLys(Dopl1)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys]-Thr NH 2 , Dop2-DPhe-cyclo [Cys-3 ITyr(Dop2)-DTrp-Lys-VaI-Cys] -Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 15 Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclolCys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 Dop2-DLys(Dop2)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3 lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclolCys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr 25 NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] Thr-NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr 30 NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , )4\MaraJ\Keep\Speci\P64463-div-SPECIdoc 13/02/08 - 170 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr 10 NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3lTyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 15 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 20 Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3lTyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , 25 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop3-Lys(Dop3)-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doC 13/02/08 - 171 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5 )-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 5 Dop5-Lys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr NH 2 , Dop5-.DLys(Dop5)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3 lTyr-DTrp-Lys-Thr-Cys]-Thr 10 NH 2 , Dop5-DLys(Dop5 )-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 15 Dop5-DLys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop5-Lys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr 20 NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys]-Thr-NH 2 , 25 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop5-DLys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr 30 NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 172 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , 5 Dop6-Lys(Dop6)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 0-Lys(Dopl 0)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dopi 1-Lys(Dop 11)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop13-Lys(DopI3)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , DopIO-Lys(Dop10)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , DopI1 -Lys(Dop 11)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or 20 Dop 1 3-Lys(Dop I 3)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]- Thr-NH 2 ; or a pharmaceutically acceptable salt thereof; wherein said therapeutically effective amount is the amount effective to treat portal hypertension in said patient.
8. A method of treating gastrointestinal bleeding in a subject in need thereof, 25 wherein said method comprises administering to said subject a therapeutically effective amount of a chimeric analog, wherein said chimeric analog comprises a compound according to the formula of: Formula (I), (II), (III), (IV), (V), (VI) (VII), (VIII), (IX), or (X) as set forth herein; or a pharmaceutically acceptable salt thereof, 30 wherein the compound is selected from: 2601322_1 (GHmatters) 14/03/11 - 173 Dop5 -DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop6-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 . 5 Dop7-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop8-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop9-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I O-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop 11I -DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 10 Dop I 2-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dopl 13-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop7-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thir-NH 2 , 15 Dop8-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop9-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop I O-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I1-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop 1 2-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 20 Dopl 13-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop5-D2Na1-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop6-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys]-Thr-NH 2 Dop7-D2NaI-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-D2NaI-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys]-Thr-NH 2 , 25 Dop9-D2NaI-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop 1 O-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I11 -D2Na1-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop 1 2-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dopl 13-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , 30 2601322 _1 (HMatters) 14/03/11 - 174 Dop5-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop9-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 0-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 11-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I 2-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop13-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Dop5-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop8-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 15 DopIO-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 11-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop12-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl 3-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 20 Dop6-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop8-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop1 0-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 25 Dop 11 -cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop12-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 13-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 30 Dop7-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 175 Dop I O-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop I11 -DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 5 Dop 1 2-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-NH 2 , Dop 1 3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop5-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop7-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 10 Dop8-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop9-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop I O-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop I11 -cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop 1 2-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 15 Dop 1 3-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5 -DPhe-cyclo [Cys-3 lTyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop6-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop7-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop8-DPhe-cyclo[Cys-3 lTyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 Dop9-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 O-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 11I -DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I 2-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl 13-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 30 2601322_1 (GHmatters) 14/03/11 - 176 Dop5 -cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop6-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop7-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop8-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop9-cyclo[Cys-3 lTyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I O-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 DopI 1 -cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl12-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dopi 13-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop5 -Caeg-cyc lo [DCys- 3 PalI-DTrp-Lys- DCys] -Thr(Bzl)-Tyr-N H 2 , Dop6-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , 15 Dop7-Caeg-cyclo[DCys-3PaI-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , Dop8-Caeg-cyclo[DCys-3 PaI-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop9-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCys] -Thr(Bz)-Tyr-NH 2 , Dop 1 O-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop 11 -Caeg-cyclo [DCys-3 PalI-DTrp-Lys- DCys] -Thr(Bzl)-Tyr-N H 2 , 20 Dop 1 2-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , DopI 3-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bz)-Tyr-NH 2 , 25 30 26013221 (GHMatters) 14/03/13 - 177 Dop5-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop6-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 5 Dop7-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop8-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop9-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop O-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop 1 I-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 10 Dop 1 2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dopi 3-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-SerBzl)-Tyr-NH 2 , Dop5-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop6-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop7-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 15 Dop8-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop9-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop1 0-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop 1 -cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop12-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 20 Dop 13-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop5-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys)-Thr-NH 2 , Dop7-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop9-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 O-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11 -DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop12-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 13-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop5-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 2601322_1 (GHMatters) 14/03/11 - 178 Dop8-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 0-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop 1 2-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 13-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr is NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop I -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dop l)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dopl -DLys(Dop l)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -DLys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop I -DLys(Dop l)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop l)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop 1 -Lys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/06 - 179 Dop I -Lys(Dopl1)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys] -Thr-N- 2 , Dop 1 -Lys(Dopl1)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , Dop 1 -Lys(Dop 1 )-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop I -Lys(Dop 1 )-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal 5 NH 2 , Dop I -Lys(Dopl1)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop I -Lys(Dopl1)-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, Dop I -Lys(DoplI)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 -Lys(Dopl1)-Lys-DTyr-DTyr-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, 10 Dop 1 -Lys(DoplI)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop 1 -Lys(Dop2)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, DoplI-Lys(Dop2)- cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 1 -Lys(Dop2)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , 15 Dop 1 -Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-CysI-Trp-NH2, Dop2-Lys(Dop2)-DPhe-cyclollCys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 20 NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 25 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , Dop2-Lys(Dop2)-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/O8 - 180 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 10 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 15 Dop2-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop3-Lys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop3-DLys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop3-DLys(Dop3)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-DLys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 30 Dop3-DLys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 181 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 5 Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 10 Dop3-Lys(Dop3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop3-Lys(Dop3)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 15 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop4-DLys(Dop4)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DLys(Dop4)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop4-DLys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop4-Lys(Dop4)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 182 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Va1-Cys] -Thr NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, 5 Dop4-Lys(Dop4)-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, 10 Dop4-Lys(Dop4)-cyclollCys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, Dop4-Lys(Dop4)-DTyr-DTyr-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop4-Lys(Dop4)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys]-Trp-NH 2 , Dop4-Lys(Dop4)- cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 15 Dop4-Lys(Dop4)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Trp NH 2 5 Dop4-Lys(Dop4)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , DopS-Lys(Dop5)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 20 Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5 -Lys(Dop5)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , DopS-DLys(Dop5)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Tin-NH 2 , 25 Dop5-DLys(Dop5 )-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5 -DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclolCys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-D2Na1-cyclollCys-Tyr-DTrp-Lys-VaI-Cys] -Tin-NH 2 , 30 Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Va-Cys] -Tin-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 183 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal 5 NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 10 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop5-Lys(Dop5)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , 15 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 20 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop6-DLys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 25 Dop6-DLys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , 30 Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 184 Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 5 Dop6-Lys(Dop6)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop6-Lys(Dop6)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, 10 Dop6-Lys(Dop6)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop6-Lys(Dop6)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop7-DLys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop7-DLys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 20 Dop7-Lys(Dop7)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-Lys(Dop7)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop7-Lys(Dop7)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 25 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-DLys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-DLys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 185 Dop8-Lys(Dop8)-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop8-Lys(Dop8)-cyclo [Cys-Phe-DTrp-Lys-Thr.Cys]-Thr-oI, Dop8-Lys(Dop8)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys] -Trp-NH 2 , Dop8-Lys(Dop8)- cyclo[Cys-Tyr-DTrp-Lys-VaI-Cys]-Trp-NH 2 , 5 Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop9-Lys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop9-DLys(Dop9)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop9-DLys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop9-Lys(Dop9)-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 , 10 Dop9-Lys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-Lys(Dop9)-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, 15 Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 , Dop9-Lys(Dop9)- cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, DopI1O-Lys(DoplIO)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop IO-Lys(Dop I )-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , DopI1O-DLys(Dopl1O)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 20 Dop IO-DLys(Dopl1 )-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop IO-Lys(DoplIO)-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , DopI1O-Lys(DoplI )-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , DopI1 -Lys(Dopl1 )-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 25 DopI1O-Lys(Dopl1 )-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2NaI -NH 2 , Dop IO-Lys(DoplIO)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop IO-Lys(Dopl1 )-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, Dop I -Lys(Dopl1 )-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Va1-Cys]-Trp-NH 2 , Dop I -Lys(Dop 10)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 30 Dopl I -Lys(Dop II )-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dopl I -Lys(Dopl II)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl 11-DLys(Dopl 11)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , H:\MaraR\Keep\speci\P64463-div-SPECI.doc 13/02/08 - 186 Dop 11-DLys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopil -Lys(Dopl l)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dopl l)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dopl -Lys(Dopl )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 11-Lys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 1 I-Lys(Dopl l)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl1 -Lys(Dop 11)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 11 -Lys(Dop 11 )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 10 Dop 11 -Lys(Dop 11)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-DLys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop12-DLys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop12-Lys(Dop12)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop12-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 20 Dop12-Lys(Dop12)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop12-Lys(Dop12)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 13-Lys(Dop1 3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-Lys(DopI3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop 13-DLys(Dop1 0)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop13-DLys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 13-Lys(Dopl 3)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 13-Lys(Dopl 3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop 13-Lys(Dop 1 3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 13-Lys(Dop I 3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop1 3-Lys(Dop 13)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 187 Dop 13-Lys(Dop 1 3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl 3-Lys(Dop 1 3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop13-Lys(Dop13)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 1 -Lys(Dop 1)-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 5 Dopl-Lys(Dopl)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop1 -DLys(Dop I)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop1 -DLys(Dopl)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop 1 -Lys(Dop I)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzi)-Tyr 10 NH 2 , Dop I -Lys(Dop 1)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop 1 -DLys(Dop 1)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , 15 Dop 1 -DLys(Dop 1)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop I -Lys(Dop 1)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop I -Lys(Dop I )-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr 20 NH 2 , Dopi -DLys(Dopl)-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , Dopl-DLys(Dopl)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , 25 DopI -Lys(Dop1)-Lys-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , Dopi -Lys(Dopl)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , DopI -DLys(DopI)-Lys-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys] 30 Thr(Bzl)-Tyr-NH 2 , DopI -DLys(Dop I)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] Ser(Bzl)-Tyr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 188 Dop2-Lys(Dop2)-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys]-Thr(Bz)-Tyr-NH 2 , Dop2-Lys(Dop2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop2-DLys(Dop2)-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys]-Thr(BzI)-Tyr NH 2 , 5 Dop2-DLys(Dop2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop2-Lys(Dop2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , 10 Dop2-DLys(Dop2)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop2-DLys(Dop2)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop2-Lys(Dop2)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr 15 NH 2 , Dop2-Lys(Dop2)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr NH 2 , Dop2-DLys(Dop2)-Aepa-Caeg-cyc lo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , 20 Dop2-DLys(Dop2)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI) Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(BzI) Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl) 25 Tyr-NH 2 , Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] Thr(BzI)-Tyr-NH 2 , Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] Ser(Bzl)-Tyr-NH 2 , 30 Dop3 -Lys(Dop3)-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DC ys] -Thr(Bzl)-Tyr-N H 2 , Dop3 -Lys(Dop3 )-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , H:\Maraft\Keep\speci\P64463-di vSPECIdoc 13/02/08 - 189 Dop3-Lys(Dop3)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop3-Lys(Dop3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 5 Dop3 -Lys(Dop3)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop3-Lys(Dop3)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop3 -DLys(Dop3)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr 10 NH 2 , Dop3 -DLys(Dop3)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop3-DLys(Dop3)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop3-DLys(Dop3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 15 NH 2 , Dop3 -DLys(Dop3)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop3-DLys(Dop3)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , 20 Dop4-Lys(Dop4)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop4-Lys(Dop4)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop4-Lys(Dop4)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 Dop4-Lys(Dop4)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 25 NH 2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 30 Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 190 Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI) Tyr-NH- 2 , Dop4-DLys(Dop4)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , 5 Dop4-DLys(Dop4)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop4-DLys(Dop4)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop4-DLys(Dop4)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH- 2 , 10 Dop4-DLys(Dop4)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(BzI) Tyr-NH 2 , Dop4-DLys(Dop4)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl) Tyr-NH 2 , Dop4-D Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] 15 Thr(Bzl)-Tyr-NH 2 , Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] Ser(Bzl)-Tyr-NH 2 , Dop5-Lys(Dop5)-Caeg-cyclo[DCys-3 PaI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop5-Lys(Dop5)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , 20 Dop5-DLys(Dop5)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH- 2 , Dop5-DLys(Dop5)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop5-Lys(DopS)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH- 2 , 25 Dop5-Lys(Dop5)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop5-DLys(Dop5 )-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop5-DLys(Dop5 )-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr 30 NH 2 , Dop6-Lys(Dop6)-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop6-Lys(Dop6)-.Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , H:\MaraR\Keep\Speci\P64463 -div-SPEC! .doc 13/02/08 - 191 Dop6-DLys(Dop6)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop6-DLys(Dop6)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop6-Lys(Dop6)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr 5 NH 2 , Dop6-Lys(Dop6)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop6-DLys(Dop6)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , 10 Dop6-DLys(Dop6)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop7-Lys(Dop7)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop7-Lys(Dop7)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop7-Lys(Dop7)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr 15 NH 2 , Dop7-Lys(Dop7)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop8-Lys(Dop8)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop8-Lys(Dop8)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 20 Dop8-Lys(Dop8)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop8-Lys(Dop8)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop9-Lys(Dop9)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 25 Dop9-Lys(Dop9)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop9-Lys(Dop9)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop9-Lys(Dop9)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 30 Dop 1 O-Lys(Dop 1 0)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 192 Dop 1 O-Lys(Dopl I )-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop 1 O-Lys(Dop 1 O)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(BzI) Tyr-NH 2 , 5 Dop 1 O-Lys(Dop I O)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz1)-Tyr NH- 2 , Dop I1I -Lys(Dop 11 )-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DC ys] -Thr(Bzl)-Tyr NH 2 , DopI 11-Lys(Dopl 11)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr 10 NH- 2 , Dop 11 -Lys(Dop 11 )-Lys-Caeg-cyc lo [DCys-3 Pal- DTrp- Lys-DCys] -Thr(BzI) Tyr-NH- 2 , DopI 11-Lys(Dopl 11)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH- 2 , 15 Dopi 2-Lys(Dopl2)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(BzI)-Tyr NH- 2 , Dopi 2-Lys(Dopl 2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH- 2 , Dop I 2-Lys(Dop 1 2)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bz) 20 Tyr-NH 2 , DoplI2-Lys(Dopl12)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , Dopi 13-Lys(DoplI 3)-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 25 Dopl13-Lys(Dopl13)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH- 2 , Dop 13 -Lys(Dop 1 3)-Lys-Caeg-cycl o[DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dopi 3-Lys(Dopl 3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr 30 NH 2 , Dopi -Lys(DopI )-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , DoplI-Lys(DoplI)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , H:\MaraR\Keep\SpeCi\P64463-div-SPEcI.doc 13/02/08 - 193 Dopl -DLys(Dopl)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dopl -DLys(Dopl)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys-Thr-NH 2 , Dop 1 -Lys(Dopl)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -DLys(Dop l)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop2-Lys(Dop2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop2-Lys(Dop2)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop2-DLys(Dop2)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 15 Dop4-Lys(Dop4)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop4-Lys(Dop4)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 20 Dop5-DLys(Dop5)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop6-DLys(Dop6)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop6-DLys(Dop6)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop6-Lys(Dop6)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-DLys(Dop6)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 30 Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 194 Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl O-Lys(Dop I 0)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 5 Dop I O-Lys(Dop1 0)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop 11 )-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop 11-Lys(Dop 11)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl2-Lys(Dop12)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop13-Lys(Dop13)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop13-Lys(DopI3)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -DPhe-cyclo[Cys-3ITyr(Dop 1)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop 1)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 Dopl -DLys(Dop 1)-DPhe-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -DLys(Dop 1)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -Lys(Dop 1)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dopl -Lys(Dop 1)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I -DLys(Dop I)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 -Lys(Dop 1 )-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I -Lys(Dop I )-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr NH 2 , 25 Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH2, Dopl -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dopl -DLys(Dop 1)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I-DLys(Dop1)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr 30 NH 2 , Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 195 Dop 1 -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop l)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop I -DLys(Dop I)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr 10 NH 2 , Dop I-DLys(Dopl )-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I -DLys(Dop I)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop 1 -Lys(Dop 1)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 Dop 1 -Lys(Dop I)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I -Lys(Dop 1)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I -DLys(Dop 1)-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop I -Lys(Dop I)-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr 20 NH 2 , Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Tir-NH 2 , 25 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , 30 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 196 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr 5 NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys] Thr-NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr 10 NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr 25 NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 197 Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Lys(Dop4)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-Lys(Dop3)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop4-Lys(Dop4)-Aepa-DPhe-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop5-DLys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop5-DLys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 30 Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08 - 198 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr 10 NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo{Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop6-Lys(Dop6)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop7-Lys(Dop7)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 O-Lys(Dop1 0)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11 -Lys(Dop 11 )-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 Dop I 2-Lys(Dop 1 2)-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 13 -Lys(Dop 1 3)-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-Lys(Dop6)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 Dop9-Lys(Dop9)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I O-Lys(Dop 1 0)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 11-Lys(Dop 11)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or Dop13-Lys(Dop13)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]- Thr-NH 2 ;; or a 30 pharmaceutically acceptable salt thereof; wherein said therapeutically effective amount is the amount effective to treat gastrointestinal bleeding in said patient. H:\MaraR\Keep\Speci\P64463-div-SPECI.doc 13/02/08
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