AU2008200692B2 - Eliciting a dopamine receptor agonist effect with somatostatin-dopamine chimeric analogs - Google Patents
Eliciting a dopamine receptor agonist effect with somatostatin-dopamine chimeric analogs Download PDFInfo
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GRIFFITH HACK PATENTS. TRADE MARKS, IP LAW SPECIFICATION OF PATENT APPLICATION COUNTRY AUSTRALIA TYPE Patent TITLE ELICITING A DOPAMONE RECEPTOR AGONIST EFFECT WITH SOMA TOSTATIN-DOPAMINE CHIMERIC ANALOGS APPLICANT SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES, S.A.S.
AUSTRALIA Patents Act 1990 COMPLETE SPECIFICATION Standard Patent Applicant (s) SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES, S.A.S. Invention Title: ELICITING A DOPAMONE RECEPTOR AGONIST EFFECT 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: ELICITING A DOPAMINE RECEPTOR AGONIST EFFECT WITH SOMATOSTATIN-DOPAMINE CHIMERIC ANALOGS Background of the Invention 5 [001] The present invention is drawn to somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use. 10021 Dopamine is a catecholamine neurotransmitter that has been implicated in the pathogenesis of both Parkinson disease and schizophrenia. Dopamine and related molecules have been shown to inhibit the growth of several types of malignant tumors 10 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 dopamine receptors on endothelial cells. Dopamine has recently been reported to strongly and selectively inhibit at non-toxic levels the vascular permeabilizing and 15 angiogenic activities of VPF/VEGF. 10031 Somatostatin (SS), a tetradecapeptide has been shown to have potent inhibitory effects on various secretory processes in tissues such as pituitary, pancreas 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 20 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 binds to the five distinct receptor (SSTR) subtypes with relatively high and equal affinity for each subtype. 25 [0041 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 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 30 are expressed in normal and neoplastic human tissues, conferring different tissue affinities for various SS analogues and variable clinical response to their therapeutic effects. H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 2 [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 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 5 ("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 not type 2 receptor has been associated with treating prolactin secreting adenomas. Other indications associated with activation of the somatostatin receptor subtypes 10 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, irritable bowel syndrome, Dumping syndrome, watery diarrhea syndrome, AIDS related diarrhea, chemotherapy-induced diarrhea, acute or chronic pancreatitis and 15 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 gastrointestinal bleeding. Preferably, a somatostatin analog is selective for the specific somatostatin receptor subtype or subtypes responsible for the desired biological 20 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 human parafollicular C cells and medullary thyroid carcinoma (MTC). MTC is a tumor originating from thyroid parafollicular C cells that produces calcitonin (CT), 25 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. Another recent study has shown that SS and SS analogs, in particular, SSTR- 1 and SSTR-2, can inhibit the proliferation of tumor cells, suggesting that specific SSTR 30 subtypes can function in MTC cell growth regulation. The development and characterization of SSTR subtype analogues that selectively effect MTC cell growth is useful for clinical and therapeutic applications. H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 3 Summary of the Invention 10071 The present invention is based on our discovery of somatostatin-dopamine chimeric analogs, comprising compounds that retain both somatostatin and dopamine 5 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 activity when compared to native somatostatin and dopamine, either alone or in combination. 10 10081 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 pharmaceutically acceptable salt thereof. 10091 In a first embodiment of the first aspect, the chimeric analog comprises 15 formula (I), Y- (L)m Z (W)" N.-R1 R3 H R2" 20 x N R4 (I) wherein: 25 100101 X is H, Cl, Br, I, F, -CN, C 1
.
10 alkyl, CI- 10 heteroalkyl, C 2
-
10 alkenyl, C 2
-
1 0 alkynyl, substituted CI.
10 alkyl, substituted C 1
I
10 heteroalkyl, substituted C 2
-
10 alkenyl, or substituted C 2
-
1 0 alkynyl; [00111 RI is H, C 1
.
1 0 alkyl, CI 10 heteroalkyl, C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted
C
1
.
1 0 alkyl, substituted C 1
.
0 heteroalkyl, substituted C 2
-
10 alkenyl, substituted C 2
-
1 0 30 alkynyl, or -CN; H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 100121 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; [00131 R4 is H, C 1
.
10 alkyl, CI 10 heteroalkyl, C 2
-
1 0 alkenyl, C 2
-
10 alkynyl, substituted 5 C 1
.
1 0 alkyl, substituted C 1
.
1 0 heteroalkyl, substituted C 2
-
10 alkenyl, or substituted C 2
-
10 alkynyl; [00141 Y is -0-, -C(O)- , -S-, -S-(CH 2 )s-C(O)-, -S(0)-, -S(0) 2 -, -SC(O)-, -OC(O)-, N(R5)-C(O)-, or -N(R6)-; 10015] L is -(CH 2 )p-C(0)-, when Y is -S-, -S(O)-, -S(0) 2 -, -0- or -N(R6)-; or L is 10 C(O)-(CR7R8)q-C(O)-, when Y is -N(R6)-, -0-, or -S-; or L is (amino acid), when Y is -C(O)-, SC(0)-, -OC(0)-, -S-(CH 2 )s-C(0)-, or -N(R5)-C(O)-; 100161 W is -CR9,R10-; 100171 R5 and R6 each is, independently, H, CI.
1 0 alkyl, substituted C 1
.
1 o alkyl; C 1 .io heteroalkyl, substituted CI.
10 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
10 15 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted alkylaryl; 100181 R7, R8, R9, and RIO each is, independently, H, F, Cl, Br, I, CI.io alkyl, substituted CI.
1 0 alkyl; C1.io heteroalkyl, substituted C 1
.
10 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
1 0 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; 10019] i is 1-10, provided that when i is 1, then RI is not H, C14 alkyl, allyl, alkenyl or -CN, R4 is not H or -CH 3 , R5, R6, R7 and R8 each is, independently, not H or C 1
.
5 alkyl, L is not -(Doc)t-, X is not H, Cl, Br, I, F, -CN, or C 1
.
5 alkyl, or R9 and R10 each is, independently, not H; 25 [00201 m is 0 or 1; [00211 n is 0-10; 100221 pis 1-10; [00231 q is 1-5; [00241 s is 1-10; 30 [00251 t is 1-10; 100261 Z is a ligand of at least one somatostatin receptor; [00271 or a pharmaceutically acceptable salt thereof; and H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 5 100281 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. [00291 In a second aspect of the first embodiment, the chimeric analog comprises 5 formula (II), [00301 ,R5 0 (W), Y-(L)--Z N 0 -R1 R3 H K~x N R4 (II) wherein: [00301 X is H, Cl, Br, I, F, -CN, Ci-io alkyl, Ci-lo heteroalkyl, C 2
-
10 alkenyl, C 2
-
1 0 10 alkynyl, substituted Ci 10 alkyl, substituted CI- 10 heteroalkyl, substituted C 2
-
10 alkenyl, or substituted C 2
-
10 alkynyl; 100311 RI is H, C 1
.
1 0 alkyl, CI 10 heteroalkyl, C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted
CI.
10 alkyl, substituted CI 10 heteroalkyl, substituted C 2
-
10 alkenyl, substituted C 2
-
1 0 alkynyl, or -CN; 15 [00321 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, CI- 10 alkyl, CI.
10 heteroalkyl, C 2
-
1 0 alkenyl, C 2
-
1 0 alkynyl, substituted
C
1
.
1 0 alkyl, substituted C 1
I
10 heteroalkyl, substituted C 2
-
1 0 alkenyl, or substituted C 2
-
10 20 alkynyl; [00341 R5 is H, Ci-io alkyl, Ci-jo heteroalkyl, C2.
10 alkenyl, C 2
-
10 alkynyl, substituted
CI-
10 alkyl, substituted C 1
.
1 0 heteroalkyl, substituted C 2
-
1 0 alkenyl, substituted C 2
-
10 alkynyl, or a group of the formula of -(CH 2 )rN(RI l,R12); H: \MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 6 100351 Y is -0-, -C(O)- , -S-, -SC(O)-, -OC(0)-, -N(R6)-C(O)-, -N(R7)-, or -N(R8) (CH2)s-C(0)-; [00361 L is -(CH 2 ),-C(O)-, when Y is -S-, -0- or -N(R7)-; or L is -C(O)-(CR9R1O)q C(O)-, when Y is -N(R7)-, -0-, or -S-; or L is (amino acid), when Y is -C(O)-, SC(0)-, 5 -OC(O)-, -N(R8)-(CH 2 )s-C(0)-, or -N(R6)-C(O)-; 100371 W is -CR9,R10-; 10038] R6, R7, and R8 each is, independently, H, C 1
.
1 0 alkyl, substituted CI.
10 alkyl,
C
1
.
1 0 heteroalkyl, substituted CI.
10 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
10 alkenyl,
C
2
-
1 0 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; 10 [00391 R9 and R10 each is, independently, H, Cl, Br, I, F, CI.
10 alkyl, substituted C . io alkyl; CI.
1 0 heteroalkyl, substituted CI.
10 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; or R9 and R10 can, optionally, join together to form a ring system; [0040] RI 1 and R12 each is, independently, H, CI.
10 alkyl, substituted CI.
1 0 alkyl; 15 C 1
.
1 0 heteroalkyl, substituted C 1 .i 0 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
10 alkenyl,
C
2
-
1 0 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; [00411 i is 1-10, provided that when i is 1, then RI is not H, C 14 alkyl, allyl, alkenyl or -CN, R4 is not H or -CH 3 , R5 is not C 1
.
5 alkyl group or a group of the formula of (CH 2 )rN(CH 3 ),, R6, R7, R8, R9 and RI0 each is, independently, not H or CI.
5 alkyl, L 20 is not -(Doc)t-, or X is not H, Cl, Br, I, F, -CN, or C 1
.
5 alkyl; [00421 m is 0 or 1; [00431 n is 2-10; [00441 pis 1-10; [00451 q is 1-5; 25 [0046] r is 1-8 ; [00471 s is 1-10; [00481 t is 1-10; 10049] v is 2-3; 100501 Z is a ligand of at least one somatostatin receptor; or 30 [00511 a pharmaceutically acceptable salt thereof; and H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 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. [00531 In a third embodiment of the first aspect, the chimeric analog of claim 1, 5 wherein said chimeric analog comprises formula (III), R4-0 R1 R5-O / (W),- -X- -Z L R2 (III) wherein: 100541 R2 is H, -N(RI I)N(R12,R13), -N(R6R7), or -COOH; [00551 R4 and R5 each is, independently, H, CIo 1 0 alkyl, substituted C 11 jo alkyl; Ci-io 10 heteroalkyl, substituted Cl.
1 o heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
10 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 R], R6, R7, R8, RI 1, R12 and R13 each is, independently, H, Ci.
10 alkyl, substituted CI.
10 alkyl; C 1 .i 0 heteroalkyl, substituted CI.
1 0 heteroalkyl, C 2
-
1 0 alkenyl, 15 substituted C 2 -o alkenyl, C 2
.
10 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; 100581 R9 and RIO each is, independently, H, -OH, -CN, -NO 2 , F, Cl, Br, I, Ci.io alkyl, substituted C 1 i 10 alkyl; C 1
.
10 heteroalkyl, substituted C 1
.
1 0 heteroalkyl, C 2 -10 alkenyl, substituted C 2
.
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
1 0 alkynyl, akylaryl, 20 substituted alkylaryl, or aryl; [00591 X is C 1 .io alkyl, substituted C 1
.
1 0 alkyl; CI.
10 heteroalkyl, substituted CI.
10 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
1 0 alkynyl, akylaryl, substituted alkylaryl, aryl, or acyl; [00601 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; 100631 q is 1-6; [00641 r is 1-8; H:\MaraR\Keep\Speci\P64461-div-SPEC-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. 10068] In a fourth embodiment of the first aspect, the chimeric analog comprises formula (IV), R2,N z (W), N R3 R1 (IV) wherein: 10 [00691 RI and R2 each is, independently, H, CI.
1 0 alkyl, substituted C 1 .,o alkyl; Ci-io heteroalkyl, substituted C 1
.
1 0 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
1 0 alkenyl, C 2 -10 alkynyl, substituted C 2
-
10 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, C 1
.
10 alkyl, substituted CI.
10 alkyl; Ci.
1 0 heteroalkyl, substituted CI.
1 0 heteroalkyl, C 2 15 1o alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; [00711 W is -CR4R5-; 100721 Y is -(CR6R7)m-C(O)- or acyl; [00731 m is 0-10; 20 100741 n is 1-6; [00751 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\P64461-div-SPEC.doc 7/02/08 - 9 [00781 In a fifth embodiment of the first aspect, the chimeric analog comprises formula (V), R2 5P (W),- N Z X R1 (V) wherein: [00791 P is -N(R3R4) or H; 10 [00801 X is N or S; [00811 W is -CR5R6-; [00821 Y is -(CR7R8)m-C(O)-; [00831 RI, R3 and R4 each is, independently, H, CI- 10 alkyl, substituted CI 10 alkyl; Ci 1 0 heteroalkyl, substituted CI.
1 0 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
10 alkenyl, 15 C 2
-
10 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; [00841 R2, R5, R6, R7 and R8 each is, independently, H, -OH, -CN, -NO 2 , F, Cl, Br, I, C 1
.
10 alkyl, substituted C 1
.
1 0 alkyl; CI.
1 0 heteroalkyl, substituted CIo 10 heteroalkyl, C 2 . io alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; 20 [00851 i is 1-10; [00861 m is 0-10; 100871 n is 0-6; [00881 Z is a ligand of at least one somatostatin receptor; or [00891 a pharmaceutically acceptable salt thereof; and 25 [00901 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 R1,N-Y -Z H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 10 (VI) wherein: 100921 Y is -(CR2R3)m-C(O)- or acyl; 5 [0093] RI is H, C 1 .io alkyl, substituted Ci.
10 alkyl; C 1 .i 0 heteroalkyl, substituted C 1
.
1 0 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; [0094] R2 and R3 each is, independently, H, -OH, -CN, -NO 2 , F, Cl, Br, I, C 1
.
1 0 alkyl, substituted CIo 10 alkyl; C1o heteroalkyl, substituted CI.
1 0 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; [00951 i is 1-10; 100961 m is 0-10; 100971 Z is a ligand of at least one somatostatin receptor; or 15 100981 a pharmaceutically acceptable salt thereof; and [00991 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. 101001 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; 101021 L is -(CR5R6)m-C(O)- or acyl; 25 [01031 Y is Cl.io alkyl, substituted CI.
10 alkyl; Ci.
10 heteroalkyl, substituted Ci.
1 0 heteroalkyl, C 2
-
1 0 alkenyl, substituted C 2
-
10 alkenyl, C 2
.
10 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, substituted akylaryl, or absent; [01041 RI, R2, R5 and R6 each is, independently, H, -OH, -CN, -NO 2 , F, Cl, Br, I,
C
1
.
1 0 alkyl, substituted C 1
.
1 0 alkyl; CIo 10 heteroalkyl, substituted C 1
.
10 heteroalkyl, C 2
.
1 0 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 11 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
10 alkynyl, substituted C 2
.
1 o alkynyl, aryl, alkylaryl, or substituted akylaryl; [01051 R3 and R4 each is, independently, H, C 1
.
1 0 alkyl, substituted C 1
.
1 0 alkyl; C 1 .io heteroalkyl, substituted C 1
.
1 0 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 5 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; [0106] i is 1-10; [01071 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. 101111 In an eighth embodiment of the first aspect, the chimeric analog comprises formula (VIII), 15 R2 R3 R4 N R1 Z 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; [01141 RI, R2, R3 and R4 each is, independently, H, -OH, F, Cl, Br, I, -CN, NO 2 , 25 C 1
.
10 alkyl, substituted CI- 1 0 alkyl; C 1
.
10 heteroalkyl, substituted CI.
10 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
1 0 alkynyl, substituted C 2
-
10 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 0 alkyl, substituted CI.
10 alkyl; C1.10 heteroalkyl, substituted C 1
.
1 0 30 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
10 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
10 alkynyl, aryl, alkylaryl, or substituted akylaryl; [01161 i is 1-10; H:\MaraR\Keep\Speci\P64451-div-SPEC.doC 7/02/08 - 12 [0117] m is 0-10; [01181 Z is a ligand of at least one somatostatin receptor; or [0119] 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 x N, Q0 z R2 R1 (IX) 15 wherein: [01211 X and Y each is, independently, -OH, -OR4 or R7-C(0)-; [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 , CIo 10 alkyl, substituted CI.
1 0 alkyl; CI.
10 heteroalkyl, substituted Ci 10 heteroalkyl, 20 C 2
-
10 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
1 0 alkynyl, substituted C 2 -o 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; [01241 R7 is H, CIo 1 0 alkyl, substituted CI- 10 alkyl; CI- 10 heteroalkyl, substituted CI.
10 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
-
10 alkynyl, substituted C 2
-
1 0 25 alkynyl, aryl, alkylaryl, or substituted akylaryl; [0125] i is 1-10; [0126] m is 0-10; [0127] Z is a ligand of at least one somatostatin receptor; or [01281 a pharmaceutically acceptable salt thereof; and 30 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 13 [0129] 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 Z R3 R6 7 R2R R1 R4 10 (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 , CI.
10 alkyl, substituted CI.
10 alkyl; Ci.
10 heteroalkyl, substituted C 1 . 10 heteroalkyl, C 2
-
10 alkenyl, substituted C 2
-
1 0 alkenyl, C 2
.
1 0 alkynyl, substituted C 2
-
1 0 alkynyl, aryl, alkylaryl, or substituted akylaryl; [01331 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 [01381 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-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 . Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 14 Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 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-NH2, 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-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH2, or Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. [01401 In a preferred embodiment of the first aspect, the chimeric analog comprises 20 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 Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 25 [0141] 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 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 30 Abu-Cys]-Thr-NH2; or a pharmaceutically acceptable salt thereof. In yet another more preferred embodiment, the chimeric analog comprises a compound zccording to the H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 15 formula of Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH2; or a pharmaceutically acceptable salt thereof. [0142] In another embodiment of the first aspect, the chimeric analog comprises a compound according to the formula of: 5 Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or Dop2-DTyr-DTyr-Caeg-cyclo[DCys-3Pal-DTrp-Lys-Dcys]-Thr(Bzl)-Tyr-NH 2 ; or a pharmaceutically acceptable salt thereof 10 [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 intermediate compound (3), (6), (11), (14), (18), (21), (24), and (27), respectively) as shown below: O 0 N H OH 3Y 15 0 -O0 HN 6 H OH 0 H:\MaraR\Keep\Speci\P64461-div-SPECdoC 7/02/08 - 16 OH 0 0 11. OH ON O 14 0 OH N c NIO O O O OH 18 -/ 0 OH 21 N-rC_; C 00 5 ;24 or H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 17 0 0 2 H,, N" OH H 27 or an organic or inorganic salt thereof. [01441 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 5 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 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 10 amount effective to elicit a dopamine receptor agonist effect in said subject. [01451 In a first embodiment of the third aspect, the chimeric analog comprises any 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: 15 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 . 20 Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, 25 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 18 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 , 5 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 a pharmaceutically acceptable salt thereof. 101471 In a preferred embodiment, the chimeric analog comprises a compound 10 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 Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 15 [0148] 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. 10149] In another more preferred embodiment of the third aspect, chimeric analogue 20 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 yet another more preferred embodiment of the third aspect, chimeric analogue comprises a compound according to the formula of Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr Cys]-Thr-NH2; or a pharmaceutically acceptable salt thereof.In a third embodiment of 25 the third 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], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or Dop2-DTyr-DTyr-Caeg-cyclo[DCys-3Pal-DTrp-Lys-Dcys]-Thr(Bzl)-Tyr-NH 2 ; 30 or a pharmaceutically acceptable salt thereof. H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 19 [0150] 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 invention, wherein said chimeric analogue comprises a compound according to the 5 formula of Formula (I), (I1), (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 somatostatin receptor agonist effect in said subject. 10 10151] 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. [0152] In a second embodiment of the fourth aspect, the chimeric analogue comprises a compound according to the formula of: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-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)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 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 , 30 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 20 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 a pharmaceutically acceptable salt thereof. 5 101531 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, Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , or Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or 10 a pharmaceutically acceptable salt thereof. [01541 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 thereof. In another more preferred embodiment of the fourth aspect, chimeric analogue 15 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. In yet another more preferred embodiment of the fourth aspect, chimeric analogue comprises a compound according to the formula of Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 20 101551 In a third embodiment of the fourth 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], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or Dop2-DTyr-DTyr-Caeg-cyclo[DCys-3Pal-DTrp-Lys-Dcys]-Thr(Bzl)-Tyr-NH 2 ; 25 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 thereof, wherein said method comprises administering to said subject an effective 30 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 H:\MaraR\Keep\Speci\P64461-diV-SPEC.dOC 7/02/08 - 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 elicit both a dopamine and a somatostatin receptor agonist effect in said subject. [01571 In a first embodiment of the fifth aspect, the chimeric analogue comprises 5 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: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-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 , 20 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 , 25 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 30 [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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 22 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , or Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 101601 In a more preferred embodiment of the fifth aspect, the chimeric analog 5 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 DTrp-Lys-Abu-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. In yet 10 another more preferred embodiment of the fifth aspect, chimeric analogue comprises a compound according to the formula of Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr 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: 15 Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or Dop2-DTyr-DTyr-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-Dcys] -Thr(Bzl)-Tyr-NH 2 ; or a pharmaceutically acceptable salt thereof. 20 [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 organic or inorganic salt thereof; in a pharmaceutically acceptable carrier, wherein said 25 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. 101631 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. [01641 In a second embodiment of the sixth aspect, the chimeric analogue comprises 30 a compound according to the formula of: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 23 Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-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 , 10 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-NH2, 15 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 20 a pharmaceutically acceptable salt thereof. [01651 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 , Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , or 25 Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-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 cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt 30 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-NH2; or a pharmaceutically acceptable salt thereof. In yet H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 24 another more preferred embodiment of the sixth aspect, chimeric analogue comprises a compound according to the formula of Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 10167] In a third embodiment of the sixth aspect, the chimeric analogue comprises a 5 compound according to the formula of: Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or Dop2-DTyr-DTyr-Caeg-cyclo[DCys-3Pal-DTrp-Lys-Dcys]-Thr(Bzl)-Tyr-NH 2 ; or 10 a pharmaceutically acceptable salt thereof. 101681 In a seventh aspect, the invention features a method of treating a disease or 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), 15 (VI) (VII), (VIII), (IX), or (X); any of the compounds listed in Table 1; Dop2-DPhe-Doc-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DPhe-Doc-DPhe-cyclo[Cys-31Tyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 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 , 30 Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH2, H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 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 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or Dop2-DTyr-DTyr-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-Dcys] -Thr(Bzl)-Tyr-NH 2 ; or a pharmaceutically acceptable salt thereof; or intermediate compound (3), (6), (11), 10 (14), (18), (21), (24), or (27); or an organic or inorganic salt thereof; and wherein said 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 15 disorder;a panic disorder; and opioid overdose; and wherein said therapeutically effective amount is the amount effective to treat said disease or disorder in said patient. 101691 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 20 ACTH-producing tumor is Cushing's disease. In a second preferred embodiment, the 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 25 embodiment, the neuroendocrine tumor of the pituitary is hyperprolactinemia or 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 30 is gonadotropinoma. [01701 In a second embodiment of the seventh aspect, the neuroendocrine tumor is carcinoid tumor. In a preferred embodiment, the carcinoid tumor causes carcinoid H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 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. [01711 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\P64461-div-SPEC.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. 10175] In a first related embodiment of the aspect of the invention disclosed above, the chimeric analog comprises a SSTR-l 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-I 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\P64461-div-SPEC.doc 7/02/08 - 28 [01801 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. 10181] 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-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH2, Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-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 , 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], 30 Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or Dop2-DTyr-DTyr-Caeg-cyclo[DCys-3Pal-DTrp-Lys-Dcys]-Thr(Bzl)-Tyr-NH2; or H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 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 patient. In a preferred embodiment of this aspect of the invention, the chimeric analog 5 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. [01831 In a ninth aspect, the invention features a method of treating prolactinemia in 10 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-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-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 , 25 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-NH2, Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys)-Thr-NH2, 30 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 30 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or Dop2-DTyr-DTyr-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-Dcys]-Thr(Bzl)-Tyr-NH 2 ; 5 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 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 10 comprises a SSTR-5 agonist and a dopamine receptor agonist. More preferably, the chimeric analog further comprises a SSTR-2 agonist. [01841 In another preferred embodiment of this aspect, the subject has developed or is at risk of developing prolactinemia. 101851 In some embodiments, compounds of the invention may include the structure 15 of DopA-Lys(DopA), wherein Lys is L-lysine, unless expressly designated as DLys. A is 1-13, for example, Dopl, Dop2, Dop3, Dop4, Dop5, Dop6, Dop7, Dop8, Dop9, DoplO, Dop11, Dop12, and Dop13. 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. 20 [01861 By "DopI" is meant a compound having the structure of: 0 H [01871 By "Dop2" is meant a compound having the structure of: 25 HN /-I 0 H N H H\MaraR\Keep\Speci\P64461-div-SPECdoc 7/02/08 - 31 10188] By "Dop3" is meant a compound having the structure of: NH 5 O= H N 00 H H 10 [01891 By "Dop4" is meant a compound having the structure of: NH H N N O 15 0 H 10190] By "Dop5" is meant a compound having the structure of: 20 OH OH
H
2 N 0 [01911 By "Dop6" is meant a compound having the structure of: 25 N 0 N=0 N 30 H H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 32 [01921 By "Dop7" is meant a compound having the structure of: N/ 5 H 2 N'.NH H [01931 By "Dop8" is meant a compound having the structure of: 10 H [0194] By "Dop9" is meant a compound having the structure of: 15 HN-<
H
2 N KjN 0 101951 By "Dop10" is meant a compound having the structure of: 20 OH HO N. N H 25 [01961 By "Dop 11" is meant a compound having the structure of: OH 0 N N 30 H 0 H:\MaraR\Keep\Speci\P64461-div-SPECdoC 7/02/08 - 33 [01971 By "Dopl2" is meant a compound having the structure of: 0" 0 HO NH,, N H0 5 [0198] By "Dopl13" is meant a compound having the structure of: 10 NN 20 N r HO OH OH [0199] Lys(Dop2) has the structure of: 15 HN S7''N 'HH N HH 20 -N N * 'HH 300 [02001 Dop2-Lys(Dop2) has the structure of: 0 H NHN 25 HHOI 30H [020] Ly(Dop) hs th strctur of H:MrRKe\peiP46-i-SESo /20 - 34 0 \ZN N o .- N H 0 [02021 Dop5-Lys(Dop5) has the structure of: 0 0 N o ...- ,N s 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 )o-4-COOH. In different embodiments 1, 2, 3 or 4 substituents are present. The presence of -(CH 2 )o4-COOH results in the production of H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 35 an alkyl acid. Examples of alkyl acids containing, or consisting of, -(CH 2
)
0 4 -COOH include 2-norbomane acetic acid, tert-butyric acid and 3-cyclopentyl propionic acid. [02051 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 , -CI- 2 alkyl substituted with I to 5 10 halogens, -CF 3 , -OCH 3 , -OCF 3 , and -(CH 2
)
04 -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 [0208] "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 ,
-C
1
-
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 102091 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. [02101 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 , -CI- 2 alkyl substituted with I to 5 halogens, -CF 3 , -OCH 3 , -OCF 3 , and
-(CH
2 )o-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\peci\P64461-div-SPEC.doc 7/02/08 - 36 are one or more sulfur, oxygen, and/or nitrogen. Examples of aryl include phenyl, 1-naphthyl, 2-naphthyl, indole, quinoline, 2-imidazole, and 9-anthracene. Aryl substituents are selected from the group consisting of -CI.4 alkyl, -C 1 4 alkoxy, halogen (i.e., fluorine, chlorine, bromine, and iodine), -OH, -CN, -SH, -NH 2 , -NO 2 , -C 1 2 alkyl 5 substituted with 1 to 5 halogens, -CF 3 , -OCF 3 , and -(CH 2 )o-4-COOH. In different embodiments the aryl contains 0, 1,2, 3, or 4 substituents. 102121 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". [0214] By "Abu" is meant a-aminobutyric acid. [0215] 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. 102171 By "Ala" or A" is meant alanine. 20 10218] By "f-Ala" is meant beta-alanine. 10219] By "Arg" or "R" is meant arginine. 102201 By "Asn" or "N" is meant asparagine. [02211 By "Asp or "D" is meant aspartic acid. 102221 By "Caeg" is meant N-(2-aminoethyl)-N-(2-cytosinyl- 1 -oxo-ethyl)-glycine, 25 represented by the structure:
NH
2 N O N 30 1T 3 0 I N N , H H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 37 102231 By "Cys" or "C" is meant cysteine. 102241 By "Dab" is meant 2,4-diaminobutyric acid. 102251 By "Doc" is meant 8-amino-3, 6-dioxaoctanoic acid, represented by the structure 5 H 102261 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. 102291 By "His" or "H" is meant histidine. [0230] By "Ile" or "I" is meant isoleucine. [0231] 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 "lNal"is meant p-(1-naphthyl)alanine. [02351 By "2Nal"is meant p-(2-naphthyl)alanine. [0236] By "Nle"is meant norleucine. [02371 By "Orn"is meant ornithine. 20 [02381 By "2Pal"is meantfi-(2-pyridinyl)alanine. [02391 By "3Pal"is meantfl-(3-pyridinyl)alanine. [02401 By "4Pal"is meant f-(4-pyridinyl)alanine. 102411 By "Phe" or "F"is meant phenylalanine. [0242] By "Pro" or "P"is meant proline. 25 102431 By "Ser" or "S"is meant serine. [02441 By "Thr" or "T" is meant threonine. [02451 By "Thr-ol" is meant threoninol, represented by the structure: ',,, OH OH 30 H 102461 By "Val" or "V" is meant valine. H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 38 [02471 By "(N-Me)Trp" " is meant N-a-methyl-tryptophan. [02481 Certain other abbreviations used herein are defined as follows: [02491 By "Ac" is meant acetyl. 102501 By "Boc" is meant tert-butyloxycarbonyl. 5 [02511 By "Bzl" is meant benzyl. 102521 By "DCM" is meant dichloromethane. 10253] By "DIC" is meant N, N-diisopropylcarbodiimide. 102541 By "DIEA" is meant diisopropylethyl amine. 102551 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. [02571 By "DMF" is meant dimethylformamide. 102581 By "DNP" is meant 2,4-dinitrophenyl. 102591 By "Fmoc" is meant Fluorenylmethyloxycarbonyl. 15 [0260] By "HBTU" is meant 2-(1 H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate. [02611 By "cHex" is meant cyclohexyl. 102621 By "HOAT" is meant O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate. 20 [02631 By "HOBt" is meant I -hydroxy-benzotriazole. [02641 By "Mmt" is meant 4-methoxytrityl. 102651 By "NMP" is meant N-methylpyrrolidone. [02661 By "Pbf' is meant 2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl. [0267] By "tBu" is meant tert-butyl. 25 102681 By "TIS" is meant triisopropylsilane. [02691 By "TOS" is meant tosyl. [02701 By "trt" is meant trityl. [02711 By "TFA" is meant trifluoro acetic acid. [0272] By "TFFH" is meant tetramethylfluoroforamidinium hexafluorophosphate. 30 102731 By "Trp" or "W" is meant tryptophan. [02741 By "Tyr" or "Y" is meant tyrosine. [0275] By "3ITyr" is meant 3-iodo-tyrosine. H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 39 [02761 3ITyr(Dop2) has the structure of: 0- H H NN 5 102771 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. [0278] 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., DI, D2, D3, 20 D4, and D5 receptors. Detailed Description [02801 The invention features somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use for the treatment of neoplasia, acromegaly, and other 25 conditions. 102811 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\P64461-div-SPEC.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 (200 1) 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\P64461-div-SPEC.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 (1981); 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 (1981); 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\P64461-div-SPEC.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 102841 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 C18 reverse-phase preparative HPLC, using acetonitrile 30 0.1 %TFA/water-0. I %TFA buffers. Homogeneity was assessed by analytical HPLC and mass spectrometry and determined to be >95% for each peptide. H:\MaraR\Keep\Speci\P64461-div-SPEC.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 [02881 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. OH OH 2 0 ; N-Rl N-Rl N-R1 H H H N N H'" H "'H 1 2 3 Scheme 1 2
HN-CH
2
(C,-
4 ) N-Rl H (C 1
.
4 )CHO, NaBH, N-R1 N H 3 4 Scheme 2 OH O H N-Rl 1. MsCI-pyridine hydrolysis, OH H R NR1 -R1 H''' H H 2. CH 3 C(O)SH H H' H' N 1 H 10 5 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 44 Scheme 3: O O
NH
2 HN CR7) OH N'R1 Base N-R1 H HH H"" H" (CR7R8) N\ N IN N H O O O H H0 0 0 H 10 Scheme 4: 0 OH N O 0 N.--R1 N,N'-dissuccinimidyl 0 H carbonate N H'" H 0 H" N\ N H N H 1 ~ 11' Scheme 5:
NH
2 HN O N.-R1 N,N'-dissuccinimidyl 0 H carbonate N-R1 H" H H N H N 3 H 12' H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 45 Scheme 6: OH OH s s Y 0 P 0 N'Rl N'RI H oxidation H H" H N N H H 6' 13' Scheme 7: OH OH s O='S J<\ O 0 N-R1 N-Rl H oxidation H H""_ _ _ H' N N H H 6' 14' H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 46 Scheme 8: H H 1) Boc 2 O/DCM R5NCS R5-N N S H2N SH H2N S 2) Ac 2 O/Base 0 3)50% TFA in DCM HN' R5 -R5 O N SH HN' O5 OH- 0 N - 1i, "n S R5-N--N S N'R OH HH H ON K'. \H"'' H HH H NN 15'H N H 2' Scheme 9: H H H2N OH 1) Boc 2 O/DCM H 2 N OR5NCS R5-N N nO 2) Ac 2 O/Base O 3)50% TFA in DCM HN' R5 R5R O"N ~OH HN OH- 0 N< R5-N=-=N____O O N -R :OH H- H hydrolysis N.-R1 H 0 Hee NHR1 H N t4H H N 16' H N H 2' H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 47 Scheme 10: 0 0 0
H
2 N OH 1) Boc 2 O/DCM - H 2 N H R5NCS 5 H _____I___________CH R5 -N e " H3 2) MeOH/DIC/DMAP/pyridine S 3) 50% TFA in DCM R HgO HN 0 n H H N 'R5 S0'CH 3 heat R5-N O CH3 O N _R1 0 R5-"- n H H "'' N 1 OH hydrolysis with base H 0 N or enzymatic hydrolysis (e.g., H esterase) H H 17' 2' H HN5 HN5 OH 0 07O N R N H H H H 1' (see Scheme 11) 19' (see Scheme II) H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 48 Scheme 11: R5 OH H'R5 HN'R OH O NSH 1) BrCH 2 C(O)OEt/Base 0 0 -R1 N-R1 2) Hydrolysis, OH- H H H" H"" N N H H 15'20 20' Scheme 12: HN ' R5 O N -tiNH 2 CR9R10 Base H OH 0 N-R1 0 O H (CR9R10 NR1 H"" H H"' 0 0 O N H N H 21' H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 49 Scheme 13: HN R5 HNR5 0 O O N'nNH 2 O N' iN 0' N,N'-disuccinimidyl H O O carbonate N'R1 0 N'R1 H H H"" H'" N N H H 22' Scheme 14: HN, R5 HNR5 O O ,,N ON'UOH N,N'-disuccinimidyl O N' )0 O' carbonate o N-R1 O N-R1 H H H'"' H'"' N N H H 16' 23' Scheme 15: HN 1) Br-CH 2
-COOCH
3 HN OH N - S H 2) Hydrolysis N 0 o N-R1 0 NR1 H H H"" H" N N H H 16' 24' H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 50 Scheme I H H NCH3 Reduction NCH 3 H NH Ra-Ni or H DMF-pyridine/Pd-C, H 2 H N H Lysergol Dihydrolysergol Reduction R'COCI/pyridine/DMAP R' H 1)CNBr -R 2) Zn-dust or H N-CH3 Ra-Ni/H 2 H 3) R-I/K 2
CO
3 H H4)0 OH-. H N H R=C 1
_
5 alkyl, allyl, or alkenyl 1) MsCI/pyridine 2) HS(CH 2 )pCO 2 R
(CH
2 )pCO 2 H A(CH 2 )pCO 2
R
1 N,R N ,R H 1) OH- H 2) H 3 0+H H H" H H (1) Compounds 6', 7, and 8' can be synthesized using the synthetic scheme above: OH OH OH S O SS O O N-Rl H N N H H 6H' 7' 8 H: \MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 51 Scheme II H JN N - "-- -n R HH H NK B 0BOC20/Base
BOC
2 0 0 base hydrolysis N 0 Boc Boc H R1 0 DIC/DCM Base H H " - "Boc ,R1 R" _ R"'-HN H 0 R 1) H+ 0 H 2) BrCH 2
CO
2 BzlI H 3) R" NCO 4. [H] or enzymatic H hydrolysis (e.g., esterase) H H 18' (I) Where R" and R" are, independently, H or C 1
-C
4 alkyl H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 52 Scheme III OH
NH
2 H 1) MsCI/pyridine H H H N- K' N H H 0 3) NH 2
NH
2 , H 2 0 (CR7RO) 0 HN,0(CRyRd)q-COOH ,R1 H H" ~- N H (111) H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 53 Scheme IV: ,- (CH 2 )nCO 2 H NR H + Partially protected somatostatin ligand on resin or H in solution S N H I1) couple (2) ) deprotect and cleave (ligand on resin) (From Scheme 1) or deprotect (ligand in solution)
(CH
2 )nCO-Somatostatin / Derivative NR H H N H R"'-HN N -OH 0 N R1 Partially protected somatostatin ligand on resin or H + in solution H" 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 NR1 H H" N H H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 54 Scheme V: 0 HN) .A(CR7R,)q-COOH N ,R1 H + Partially protected somatostatin ligand on resin or H" in solution 1) couple HI / 2) deprotect and cleave (ligand on resin) or deprotect (ligand in solution) (From Scheme Il) 0 HN)L(CR7R,),-CO-Somatostatin Derivative N ,R1 H H ~- N H H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 55 Scheme VI: JH R1 H2N,,,, NR1 H H H Curtius H reaction -- N N H H N,N'-disuccinimidyl carbonate/base I 0 10 OY N 0 0o HN,,,,, N R1 HN,,,,, ,R1 H 1) Sarcosine/base N H H 2) H+ H N N H H H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 56 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). 102901 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 [02911 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 102921 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 imol 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 imol 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 1 X 5 min and I 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\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 57 diisopropylcarbodiimide (DIC) (0.2 mmol) in NN-dimethylformamide (DMF) for I hour per coupling. The resin was coupled successively according to the sequence. 102931 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 pL, 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 C18 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\P64461-div-SPEC.doc 7/02/08 - 58 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] Thr-NH 2 (as described above in Example 1) with the following changes. After the 5 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 (3.0 eq), DMAP (1.0 eq) and DIEA (4 eq). After cleavage and purification, the desired 10 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). Example 3: Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr 15 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 Lys(Fmoc)-OH was used for the coupling of the last Lys residue at the N-terminus. The 20 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). Example 4: Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 25 10297] 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 1). The purity of the final product was 93.9% based on an analytical HPLC analysis. ESI mass analysis gave the molecular weight at 1514.50 (in agreement with the calculated molecular weight of 30 1514.63). H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 59 Example 5: Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 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-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). 10 Example 6: Synthesis of intermediate compound (3) OH * 0- HO 0 N N H H N H OH 15 1 2 HH3 O 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 20 pressure. The 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- R(-)norapomorphine, yielding compound 2. 25 102991 To a mixture of compound 2 (167 mg, 0.57 mmol) and NN 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 30 purified by using column chromatography on silica, yielding intermediate compound 3. H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 60 Example 7: Synthesis of intermediate compound (6) OH I I 0 -- 5 N H H N N 4 5 H H 6 H KyOH 0 103001 The mixture of R(-)norapomorphine 4 (200 mg, 0.748 mmol), 2 10 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 anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding compound 5. 15 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 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 20 residue is purified by using column chromatography on silica, yielding intermediate compound 6. Example 8: Synthesis of intermediate compound (11) 25 NH OH 0 N N H H 10 11 30 103021 To a mixture of indolone 10 (WO 9415918, 218 mg, 1.00 mmol) and NN 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 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 61 temperature overnight. The solution is concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding intermediate compound 11. Example 9: Synthesis of intermediate compound (14) 5 00 OH O OH 12 13 14 10 [03031 To a mixture of I -adamantanamine hydrochloride 12 (Aldrich, 187 mg, 1.00 mmol) and NN-diisopropylethylamine (387 mg, 3.0 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 washed with brine (2 times), dried over 15 anhydrous MgSO 4 , filtered, and concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding compound 13. [03041 To a solution of compound 13 (190 mg, 0.8 mmol) in dioxane (6 mL) and 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 20 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, 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 25 intermediate compound 14. Example 10: Synthesis of intermediate compound (18) 0 H OH NN N 30 ci0c 0 0~c I . Cl Cl: OH O O--0C OH15 OH O 16 %17 + 18 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 62 103051 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 residue is dissolved in methylene chloride (30 mL) and washed with saturated NaHCO 3 5 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. 10306] 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 10 CH 2
CI
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 column chromatography on silica, yielding compound 17. 103071 To a mixture of 17 (201 mg, 0.50 mmol) and NN-diisopropylethylamine 15 (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 concentrated in vacuo. The residue is purified by using column chromatography on silica, yielding intermediate compound 18. 20 Example 11: Synthesis of intermediate compound (21) O 0 OH OH HN-l N-</~ H-JKNY r-F 25 H H 0 H 19 20 21 01< [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 30 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. H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 63 [03091 To a solution of 2 (179 mg, 0.7 mmol) in dioxane (6 mL) and water (3 mL) is added IN 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 5 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 silica, yielding intermediate compound 21. 10 Example 12: Synthesis of intermediate compound (24) 0 0 OH N OH NQN O
H
2 N-K< 'k>NH :, 2 N N o s 22 24 [03101 To a solution of 22 (169 mg, 1.0 mmol) in dioxane (20 mL) and water (10 20 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. 103111 To a solution of 23 (179 mg, 0.7 mmol) in dioxane (6 mL) and water (3 mL) 25 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 residue is purified by using column chromatography on silica, yielding intermediate 30 compound 24. Example 13: Synthesis of intermediate compound (27) H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 64 NH H,,'H " HO H NH O OH H -IN H H 525 26 27 103121 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
CI
2 (20 mL) is stirred at room temperature overnight. The solution is washed with saturated NaHCO 3 in aqueous solution (2 times) and brine 10 (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. 103131 To a mixture of 1-adamantanamine hydrochloride 26 (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 is 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 20 described above. 10315] For the introduction of DopI, Dop2, Dop3 or Dop4 residue(s) into peptides, DopI-OH, Dop2-OH, Dop3-OH or Dop4-OH (WO 02/100888 Al) was used during the syntheses, respectively. 10316] For the synthesis of the Dop5 containing peptides, Fmoc-Dopa(acetonide) 25 OH (Novabiochem, San Diego, CA) was used. 103171 For the Dop6 residue in peptides, compound _1 is used during the synthesis. 103181 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. 103201 For the Dop9 residue in peptides, compound 24 is used during the synthesis. 30 [03211 For the Dop10 residue in peptides, compound 3 is used during the synthesis. 103221 For the Dopi I residue in peptides, compound 6 is used during the synthesis. [03231 For the Dop12 residue in peptides, compound 27 is used during the synthesis. [0324] For the Dopl3 residue in peptides, compound 18 is used during the synthesis. H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 65 [03251 Table 1 lists somatostatin-dopamine chimeric analogs likely to have somatostatin and dopamine activity in vitro or in vivo. Table 1 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 5 Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Ac)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop2-DLys(Ac)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 10 Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop3-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop4-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop6-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 15 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 Dop1O-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop 11 -DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 20 Dop12-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop13-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 25 Dop8-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop9-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop10-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 30 Dopl3-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop5-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop6-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 66 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 Dop 1 O-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 5 Dop I -D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2 Dopi 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 Dop6-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 10 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 Dop1 0-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop 11-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 15 Dopl 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 Dop6-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop7-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI 20 Dop8-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop9-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop 1 O-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop 1 -DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop I 2-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 25 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-oI Dop7-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop8-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 30 Dop9-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop1 0-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop 11-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 67 Dop 1 2-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol Dop 1 3-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-NH 2 Dop6-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 5 Dop7-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop8-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2 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 Dopl 11-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 10 DoplI2-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-NH 2 Dop13 -DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-NH 2 Dop5 -cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 Dop6-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI -NH 2 Dop7-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2NaI -NH 2 15 Dop8-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop9-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 DopI1 -cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop I1-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 DoplI2-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-NH 2 20 Dop13 -cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-NH 2 DoplI-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop2-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 DoplI-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 25 Dop3 -Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop4-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop3 -DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop4-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5 -DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 30 Dop6-DPhe-cyclo [Cys-3ITyr-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 H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 68 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 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 5 Dop 1 3-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop3 -cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop4-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop5-cyclo [Cys-3 I Tyr- DTrp- Lys-Thr-Cys] -Thr-NH 2 Dop6-cyclo [Cys-3 I Tyr- DTrp-Lys-Thr-Cys] -Thr-NH 2 10 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 Dopl1 0-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop 11I -cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 15 Dop 1 2-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 DopI 13-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl1 -Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 Dop2-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dop3 -Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 20 Dop4-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop I -Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop2-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys]-Thr(Bzl)-Tyr-NH2 Dop3 -Aepa-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCys]-Thr(Bz)-Tyr-N H2 Dop4-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 25 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 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-NH 2 Dop9-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(BzI)-Tyr-NH 2 30 Dop I O-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop I11 -Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 DoplI2-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 69 Dop 13 -Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop 1 -Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop3-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 5 Dop4-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 DopI -Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop2-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop3-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop4-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 10 Dop5-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 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 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 15 DopI O-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop 11 -Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop 1 2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop 13-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-SerBzl)-Tyr-NH 2 Dop5-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 20 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 Dop I 0-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 25 Dopl 1-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 DopI 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-NH 2 30 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 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 70 Dop 1 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 5 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 Dop9-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 10 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 Dop12-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop13-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 15 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 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 20 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dopl-Lys(DopI)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 DopI-Lys(Dop1)-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 DopI-Lys(DopI)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 25 Dopl-Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop1-DLys(Dop1)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop1-DLys(Dop1)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop1-DLys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop I -DLys(Dop I )-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 30 Dopl-DLys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop1-Lys(Dop1)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop1-Lys(DopI)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 71 Dop I -Lys(Dop l)-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 Dop 1 -Lys(Dop 1)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop 1 -Lys(Dop 1)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 5 Dop 1 -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop 1 -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop I -Lys(Dop 1)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop 1 -Lys(Dop 1)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop I -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI 10 Dop 1 -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI Dop I -Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 Dop1-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-NH2 Dop] -Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 15 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 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 20 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 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 25 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 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 30 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 H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 72 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-oI Dop2-Lys(Dop2)-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI 5 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-oI 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 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 10 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-VaI-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-N H 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]l-Thr-NH 2 15 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 Dop3 -DLys(Dop3)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 20 Dop3 -DLys(Dop3 )-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop3 -Lys(Dop3)-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 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-NH 2 25 Dop3 -Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop3 -Lys(Dop3 )-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 Dop3-Lys(Dop3)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-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-oI 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 HA:MaraR\Keep\Speci\P64461-div-SPECdoC 7/02/08 - 73 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 Dop3-Lys(Dop3)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2 5 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-NH 2 Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 10 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 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 15 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-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-NH 2 20 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 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 25 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 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 Dop5-Lys(Dop5)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 74 Dop5 -Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-N H 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 5 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)-D2NaI-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 10 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 Dop5 -Lys(Dop5)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-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-2Na-NH2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 15 Dop5-Lys(Dop5)-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI 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-oI Dop5 -Lys(Dop5)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 20 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-VaI-Cys]-Trp-NH 2 Dop6-Lys(Dop6)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-CysJ-Thr-NH 2 Dop6-Lys(Dop6)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 25 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 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 30 Dop6-DLys(Dop6)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop6-Lys(Dop6)-D2NaI-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 Dop6-Lys(Dop6)-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Hi:\MaraR\Keep\Speci\P64461-div-SPECdoC 7/02/08 - 75 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 Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 5 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 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-oI 10 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 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 15 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 Dop7-Lys(Dop7)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 20 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 Dop7-Lys(Dop7)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI 25 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 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 30 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 H.\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 76 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-CysJ-Thr-oI Dop8-Lys(Dop8)-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol 5 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 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 10 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 Dop9-Lys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 Dop9-Lys(Dop9)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thir-Cys]-2Na-NH2 Dop9-Lys(Dop9)-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 15 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-NH2 Dop9-Lys(Dop9)- cycloI[Cys-Tyr-DTrp-Lys-Va1-Cys] -Tmp-NH 2 Dop I -Lys(Dopl1 )-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 20 Dop I -Lys(Dopl1 )-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]l-Thr-NH 2 DopI O-DLys(Dopl 0)-DPhe-cyclollCys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2 DopI1O-DLys(Dopl1 )-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dop I -Lys(Dopl1 )-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 DopI1 -Lys(Dopl1 )-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 25 DopI1O-Lys(DoplI )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 DopI 0-Lys(DoplO)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop I -Lys(DoplIO)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI DopI1 -Lys(Dopl1 )-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI DopI1 -Lys(DoplI )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 30 Dop I -Lys(Dop 10)- cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys] -Trp-NH 2 Dopl 11-Lys(Dopl II)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 Dopl 11-Lys(Dopl 11)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 H:\MaraR\Keep\Speci\P64461-di-SPEC.doC 7/02/08 - 77 Dop 11-DLys(Dopl l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop 11-DLys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop I -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 5 Dop 11-Lys(Dopl l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dopl1 -Lys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dopl1 -Lys(Dop 11)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop 11-Lys(Dopl1 )-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dopl l-Lys(Dopl l)-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 Dop I 2-Lys(Dop 1 2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop I 2-Lys(Dop 1 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop I 2-Lys(Dop I 2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop I 2-Lys(Dop I 2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI 20 Dop I 2-Lys(Dop 1 2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop I 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 I 3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 Dop I 3-Lys(Dop I 3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 25 Dop 13-DLys(Dop I 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 Dop 13-Lys(Dop I 3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop 13-Lys(Dop 13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 30 Dop 13-Lys(Dop I 3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 Dop 13-Lys(Dop I 3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol Dop I3-Lys(DopI 3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 78 DopI 13-Lys(Dop 1 3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 Dopl13-Lys(Dop 13)- cyclo[Cys-Tyr-DTrp-Lys-VaI-Cys]-Trp-NH 2 DoplI-Lys(DoplI)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dopl1-Lys(Dopl1)-Caeg-cyclojlDCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 5 Dopl1-DLys(Dopl1)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 DoplI-DLys(Dopl1)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]l-Ser(BzI)-Tyr-NH 2 Dopl1-Lys(DoplI)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dopl1-Lys(Dopl1)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 Dop I -DLys(Dop 1 )-Lys- Caeg-cyclo [DCys-3 Pal-DTrp- Lys-DCys] -Thr(Bz)-Tyr-N H2 10 Dopl-DLys(Dopl )-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dopl1-Lys(Dopl1)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dopl1-Lys(Dopl1)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 DoplI-DLys(Dopl1)-Aepa-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dopl1-DLys(Dopl1)-Aepa-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 15 Dopl1-Lys(DoplI)-Lys-Aepa-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr
NH
2 Dopi -Lys(Dopl)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr
NH
2 Dopl1-DLys(Dopl1)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr 20 NH 2 Dopl1-DLys(Dopl1)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr
NH-
2 Dop2- Lys(Dop2)-Caeg-cyc lo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 Dop2-Lys(Dop2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 25 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(BzI)-Tyr-NH 2 Dop2-Lys(Dop2)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bz)-Tyr-NH 2 Dop2-Lys(Dop2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 Dop2-DLys(Dop2)- Lys-Caeg-cyclo [DC ys-3 PalI-DTrp- Lys-DC ys] -Thr(Bzl)-Tyr-N H 2 30 Dop2-DLys(Dop2)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 Dop2-Lys(Dop2)-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 Dop2-Lys(Dop2)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 H:\MaraR\Keep\speci\P64461-div-SPEC.doc 7/02/08 - 79 Dop2-DLys(Dop2)-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2 Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr
NH
2 5 Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr
NH
2 Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyc lo [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 10 NH 2 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(Bzl)-Tyr-NH 2 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-DCys] -Ser(Bzl)-Tyr-NH 2 15 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-NH 2 Dop3 -DLys(Dop3 )-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys)-Ser(Bzl)-Tyr-NH2 Dop3-DLys(Dop3 )-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bz)-Tyr-NH 2 20 Dop3-DLys(Dop3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2 Dop3 -DLys(Dop3 )-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-N H 2 Dop3 -DLys(Dop3 )-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2 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 25 Dop4-Lys(Dop4)-Lys-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCys] -Thr(BzI)-Tyr-N H 2 Dop4-Lys(Dop4)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo[DCys-3 PaI-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 PalI-DTrp- Lys- DCys] -Thr(BzI)-Tyr 30 NH 2 Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr
NH
2 H:\maraR\Keep\speci\P64461-div-SPEC.doc 7/02/08 - 80 Dop4-DLys(Dop4)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop4-DLys(Dop4)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop4-DLys(Dop4)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop4-DLys(Dop4)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 5 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-NH2 Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr
NH
2 Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 10 NH 2 Dop5-Lys(Dop5)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop5-Lys(Dop5)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 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 15 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 Dop5-DLys(Dop5)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-N H 2 Dop5-DLys(Dop5)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop6-Lys(Dop6)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 20 Dop6-Lys(Dop6)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 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-NH 2 Dop6-Lys(Dop6)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 25 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 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-NH 2 30 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 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 81 Dop8-Lys(Dop8)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2 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 Dop9-Lys(Dop9)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 5 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(Bzl)-Tyr-NH 2 Dop 10-Lys(Dop 1 0)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop I 0-Lys(Dop1 0)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop 1 O-Lys(Dop1 0)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 10 DopI O-Lys(Dopl 0)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dopl I -Lys(Dop ll)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dopl -Lys(Dopl l)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop 11-Lys(Dopl )-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 Dopl 1-Lys(Dopl l)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 15 Dop12-Lys(Dop12)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop12-Lys(Dop12)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 Dop12-Lys(Dop12)-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-NH 2 Dop 13 -Lys(Dop 1 3)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 20 Dop13-Lys(Dop13)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dop13-Lys(Dop13)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 Dop13-Lys(Dopl3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2 Dopl-Lys(Dopl)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2 Dopl-Lys(Dopl)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 25 Dopl-DLys(Dopl)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dopl-DLys(DopI)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl-Lys(Dopl)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl-DLys(Dopl)-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 30 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 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 82 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 Dop3 -Lys(Dop3 )-cyclollCys-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 5 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-NH 2 Dop5 -Lys(Dop5)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 10 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-N H 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 Dop5-DLys(Dop5 )-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 15 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]l-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 20 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-NH 2 Dop8-Lys(Dop8)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2 25 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 Dop 1 O-Lys(Dopl 1 )-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 30 Dopl 11-Lys(Dopl 11)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 Dopl 11-Lys(Dopl 11)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 DoplI2-Lys(DoplI2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 83 Dop1 2-Lys(Dop1 2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop 1 3-Lys(Dop1 3)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 Dop 1 3-Lys(Dop 1 3)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -DPhe-cyclo[Cys-3ITyr(Dopl)-DTrp-Lys-Val-Cys]-Thr-NH 2 5 Dopl -DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dopl)-DTrp-Lys-Val-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 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-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 10 Dopl -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dopl -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 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 15 Dopl -DLys(Dop 1 )-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 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 Dopl -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 20 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-NH 2 Dopl -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 25 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 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 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\P64461-div-SPEC.doc 7/02/08 - 84 Dop1 -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop 1 -DLys(Dop1)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 Dop I -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 5 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 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-Lys(Dop2)-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Example I 10 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 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 15 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 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-31Tyr-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 20 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 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 25 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 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 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-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 85 Dop2-Lys(Dop2)-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 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 5 Dop3-Lys(Dop3)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH2 Dop4-Lys(Dop4)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop3 -Lys(Dop3)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop4-Lys(Dop4)-Aepa-DPhe-cyclolCys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 Dop5 -DLys(Dop5)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 10 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-N H 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 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 15 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 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 LCys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 20 Dop5 -DLys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]l-Thr-NH 2 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-NH 2 Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 25 Dop5-DLys(Dop5)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3lTyr-DTrp-Lys-Val-Cys]-Thr-NH2 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 30 Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 Dop5-DLys(Dop5)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Va-CysI-Thr-NH 2 Dop5-DLys(Dop5 )-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys]-Thr-NH 2 H;\MaraR\Keep\Speci\P64461-di-SPEC.dOC 7/02/06 - 86 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 5 DopI 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 Dop 12-Lys(Dop I 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 10 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 I 0-Lys(Dop I 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 15 Dop I 2-Lys(Dop 1 2)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 Dop 13 -Lys(Dop I 3)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 103261 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 20 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 separated, pure or partially purified optical isomers, racemic mixtures or diastereomeric mixtures thereof, are included within the scope of the instant invention. [03271 The compounds of the instant invention generally can be provided in the 25 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, 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 30 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. H.\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 87 [03281 The pharmaceutically acceptable salts can be formed by taking about I equivalent of a compound of the invention and contacting it with about I equivalent or 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. 5 103291 The compounds of this invention can be administered by oral, parenteral (e.g., intramuscular, intraperitoneal, intravenous or subcutaneous injection, or implant), 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 10 features pharmaceutical compositions comprising, as an active ingredient, at least one compound of the invention in association with a pharmaceutically acceptable carrier. 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 15 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 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 20 acceptable emulsions, solutions, suspensions, syrups, the elixirs containing inert diluents commonly used in the art, such as water. Besides such inert diluents, 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 25 sterile aqueous or non-aqueous solutions, suspensions, or emulsions. Examples of non aqueous solvents or vehicles are propylene glycol, polyethylene glycol, vegetable oils, 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 30 bacteria-retaining filter, by incorporating sterilizing agents into the compositions, by irradiating the compositions, or by heating the compositions. They can also be H-\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 88 manufactured in the form of sterile solid compositions which can be dissolved in sterile water, or some other sterile injectable medium immediately before use. [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 5 a suppository wax. [0334] Compositions for nasal or sublingual administration are also prepared with standard excipients well known in the art. 10335] 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 10 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 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. 15 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 multiple doses. Somatostatin Receptor Specificity and Selectivity Assay 20 [03371 Specificity and selectivity of the somatostatin analogues used to synthesize the somatostatin-dopamine chimers was determined by a radioligand binding assay on 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 25 (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 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 30 artisan. Clonal cell lines stably expressing SSTR's 1-5 were obtained by transfection into CHO-Kl cells (ATCC, Manassas, Va, USA) using the calcium phosphate co precipitation method (Davis L, et al., 1994 In: Basic methods in Molecular Biology, 2nd H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 89 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 1640 media containing 0.5 mg/ml of G418 (Life Technologies, Milano, Italy), ring cloned, and expanded into culture. 5 [03381 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 Tris-HCl 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. [03391 For the SSTR 1, 3, 4, and 5 assays, aliquots of the membrane preparations 10 were incubated 90 minutes at 25 0 C with 0.05 nM [1 2 1I-Tyrl l]SS-14 in 50 mM HEPES (pH 7.4) containing 10 mg/ml bovine serum albumin (BSA), 5 mM MgCl 2 , 200 KIU/ml 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 [mI]MK-678 was employed as the 15 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 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 20 1000 nM SS-14 for SSTR 1, 3, 4, and 5, or 1000 nM MK-678 for SSTR2. Dopamine Receptor Specificity and Selectivity Assay [0341] Specificity and selectivity for the dopamine-2 receptor of the dopamine analogues used to synthesize the somatostatin-dopamine chimers may be determined by 25 a radioligand binding assay as follows. [03421 Crude membranes were prepared by homogenization of frozen rat corpus 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 30 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 H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 90 for 10 min, diluted, and centrifuged as before. The final pellet was resuspended in buffer and held on ice for the receptor binding assay. 103431 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, 5 New England Nuclear, Boston, MA) in 50 mM Tris HCl, 120 mM NaCl, 5 mM KCl, 2 mM CaCl 2 , 1 mM MgCl2. The final assay volume was 1.0 ml. The incubations were 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 10 bound in the presence of 1000 nM (+) butaclamol. Inhibition of cAMP Intracellular Production [0344] The agonist activity of a somatostatin test compound is determined by the following assay. 15 103451 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 serum (FCS). [03461 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 20 ("IBMX"), and the cells are incubated for 30 minutes at 37*C. Cyclic AMP production is stimulated by the addition of 10 pM forskolin ("FSK") (Sigma Chemical Co., St. Louis, MO) for 30 minutes at 37*C. [03471 The agonist effect of a compound is measured by the addition of the test compound (10-0 M to 10~6 M) for five minutes prior to the addition of FSK (10 ptM). 25 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 measured using radioimmunoassay kit (Perkin-Elmer, Boston, MA). Other Embodiments 30 [03481 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 scope and spirit of the invention. Although the invention has been described in H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 91 connection with specific desired embodiments, it should be understood that the invention as claimed should not be unduly limited to such specific embodiments. 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, 5 endocrinology, or related fields are intended to be within the scope of the invention. [03491 All publications mentioned in this specification, including PCT/USO2/17859, 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 10 invention, except where the context requires otherwise due to express language or necessary implication, the word "comprise" or variations such as "comprises" or "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. 15 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 documents forms part of the common general knowledge in the art in Australia or in any other country. H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08
Claims (13)
1. A method of eliciting a dopamine receptor agonist effect in a subject in need thereof, wherein said method comprises administering to said subject an 5 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) as set forth herein; or a pharmaceutically acceptable salt thereof; wherein the compound is selected from: 10 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Ac)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Ac)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 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 , Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopi 0-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop 11-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 2-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopi 3-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 , 30 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 , 1156528_1 (GHMatters) 7/06/10 - 93 Dop 1 0-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop 1l-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I 2-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 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-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Dopl 0-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I I-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1 2-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1 3-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-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-NH2, 20 Dop 1l-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 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-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 I l-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 30 Dop 1 2-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 13-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop5-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, H-\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 94 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-oI, 5 Dop 1 -cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, Dopl 1-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, DoplI2-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop I 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]-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 I O-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 15 Dopl 11-DPhe-cycloI[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH2, DoplI2-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , DoplI3-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-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]-2Na-NH 2 , Dop8-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop9-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop I -cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop 1-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 25 Dopl12-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop13 -cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dopl1-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dopl1-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 30 Dop2-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop3 -Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop4-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-di-SPEC.doc 7/02/08 - 95 Dop3-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop6-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 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 , Dop 1 O-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I1 -DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop I 2-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 13-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop6-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop7-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 0-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop 1l-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop12-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop13-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop2-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 25 Dop3-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop4-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop] -Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop2-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop3-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 30 Dop4-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop5 -Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop6-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 96 Dop7-Caeg-cyclo [DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop8 -Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , Dop9-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop I O-Caeg-cyclo [DCys-3 PalI-DTrp-Lys- DCys] -Thr(Bzl)-Tyr-NH 2 , 5 Dop 11 -Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bz)-Tyr-NH 2 , DoplI 2-Caeg-cyclo [DCys-3 PaI-DTrp- Lys- DCys] -Thr(BzI)-Tyr-NH 2 , DopI 13-Caeg-cyclo[DCys-3 PaI-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , Dopl1 -Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , 10 Dop3 -Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop4-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , Dopl1 -Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop2-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop3 -Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , 15 Dop4-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop5-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , Dop6-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCysI-Ser(Bzl)-Tyr-NH 2 , Dop7-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop8-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , 20 Dop9-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop 1 O-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop I11 -Caeg-cyclo[~DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop I 2-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dopl 13-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -SerBzl)-Tyr-NH 2 , 25 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 , 30 Dop 1 0-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop 11I -cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop I 2-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-CysI -NH 2 , Hi:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 97 Dopl 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 , Dop 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-NH2, Dop 1 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-NH2, 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 , Dop 1 0-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , DopI 1 -cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop I 2-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, 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(Dop 1)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop I)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop 1)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 98 Dop 1 -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop 1 -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I -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 I -DLys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dop 1)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop I -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop I -Lys(Dop 1)-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 I -Lys(Dop 1)-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 , 15 Dop 1 -Lys(Dop 1)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop I -Lys(Dop 1)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 1 -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal NH 2 , Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 20 Dop I -Lys(Dop 1)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 -Lys(Dop 1)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 -Lys(Dop 1)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop I -Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, 25 Dop 1 -Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop 1 -Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop I -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 , 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\P64461-div-SPEC.doc 7/02/08 - 99 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-NH 2 , 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-NH 2 , 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-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 100 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-NH 2 , Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 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-NH 2 , 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\P64461-div-SPEC.doc 7/02/08 - 101 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-NH2, 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-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 20 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, 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-NH2, 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\P64461-div-SPEC.doc 7/02/08 - 102 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-NH 2 , 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\P64461-div-SPEC.doc 7/02/08 - 103 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-NH2, 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-NH2, 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-NH2, 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-NH2, 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 , 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\P64461-div-SPEC.dOC 7/02/08 - 104 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-NH2, 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 DopI0-Lys(Dop10)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop1O-Lys(Dop1O)-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\P64461-div-SPEC.dC 7/02/08 - 105 Dop I 0-DLys(Dop1 0)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop1 0-Lys(Dop1 0)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1 0-Lys(Dop1 0)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop 10-Lys(Dopl 0)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop I 0-Lys(Dop1 0)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop O-Lys(Dop1 0)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 10-Lys(Dop1 0)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 1 O-Lys(Dop1 0)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 10 Dop10-Lys(Dopl0)- 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 , Dop 11-Lys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11-DLys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11-DLys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop 11-Lys(Dop 11)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1-Lys(Dopl 1)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I-Lys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dopl1 -Lys(Dop1 1)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 20 Dop 1 -Lys(Dop ll)-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 Il-Lys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop 11-Lys(Dop 11)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 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(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 2-Lys(Dop1 2)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1 2-Lys(Dop1 2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop 1 2-Lys(Dop1 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 1 2-Lys(Dop1 2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop1 2-Lys(Dop1 2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 106 DopI 2-Lys(Dop1 2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, DopI 2-Lys(Dop1 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dopl2-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 , 5 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(DopI3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl3-Lys(Dop13)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Dop13-Lys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopl 3-Lys(Dopl 3)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 13-Lys(Dop1 3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 13-Lys(Dopl 3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 15 Dop 13-Lys(Dop1 3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , DopI3-Lys(Dop13)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , DopI -Lys(Dop1)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop I-Lys(Dopl )-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop I -DLys(Dop 1 )-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr 20 NH 2 , Dop I -DLys(Dop 1)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop I -Lys(Dop I)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop I -Lys(Dop 1)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr 25 NH 2 , Dop I-DLys(Dop1)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop I -DLys(Dop 1)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 30 Dop 1 -Lys(Dop I)-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 107 Dop 1 -Lys(Dop 1 )-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop 1 -DLys(Dop 1 )-Aepa-Caeg-cyc lo [DCys-3 Pal- DTrp- Lys-DCys] -Thr(BzI) Tyr-NH 2 , 5 DoplI -DLys(Dop I )-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]l-Ser(BzI) Tyr-NH 2 , Dop 1 -Lys(Dop I )-Lys-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop I -Lys(Dop 1 )-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) 10 Tyr-NH 2 , Dop 1 -DLys(Dop I )-Lys-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCys] Thr(Bzl)-Tyr-NH 2 , Dop 1 -DLys(Dop 1 )-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] Ser(Bzl)-Tyr-NH 2 , 15 Dop2-Lys(Dop2)-Caeg-cyclo [DCys-3 Pal-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-3 Pal- DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop2-DLys(Dop2)-Caeg-cyclo [DCys-Phe-DTrp- Lys- DCys] -Ser(BzI)-Tyr-N H 2 , 20 Dop2- Lys(Dop2)-Lys-Caeg-cycl o [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bz)-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(Bz)-Tyr 25 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 NH 2 , 30 Dop2-Lys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 108 Dop2-DLys(Dop2)-Aepa-Caeg-cyclolDCys-3 Pal-DTrp-Lys-DCys]-Thr(BzI) Tyr-NH 2 , Dop2- DLys(Dop2)-Aepa-Caeg-cyc lo [DCys-Phe-DTrp- Lys- DC ys] -Ser(BzI) 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(BzI) Tyr-NH 2 , Dop2-DLys(Dop2)-Lys-Aepa-Caeg-cyclo[DCys-3 PaI-DTrp-Lys-DCys] 10 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-cyc lo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , Dop3 -Lys(Dop3)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , 15 Dop3 -Lys(Dop3)-Lys-Caeg-cyclo [DCys-3 PalI-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-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-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 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH- 2 , 25 Dop3-DLys(Dop3 )-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 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(Bzl)-Tyr NH- 2 , 30 Dop3 -DLys(Dop3)-Aepa-Caeg-cycl o[DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 109 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 , Dop4-Lys(Dop4)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , 5 Dop4- Lys(Dop4)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH- 2 Dop4-Lys(Dop4)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -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-cyclolDCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl) 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-cyclo [DCys-3 Pal-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(Bzl)-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 PaI-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-D Lys(Dop4)- Lys-Aepa-Caeg-cyc lo [DCys-3 Pal -DTrp- Lys-DCys] Thr(Bzl)-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-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2, H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 110 Dop5-Lys(Dop5)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, Dop5 -DLys(Dop5)-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop5 -DLys(Dop5)-Caeg-cyclo [DCys-Phe-DTrp- Lys- DCys] -Ser(Bz)-Tyr-NH 2 , 5 Dop5-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 PalI-DTrp-Lys-DCys] -Thr(BzI)-Tyr 10 NH 2 , Dop5 -DLys(Dop5)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop6-Lys(Dop6)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop6-Lys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(3z1)-Tyr-N H 2 , 15 Dop6-DLys(Dop6)-Caeg-cyclollDCys-3Pal-DTrp-Lys-DCys]-Thr(Bz)-Tyr NH 2 , Dop6-DLys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop6-Lys(Dop6)-Lys-Caeg-cyclo [DCys-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-cyc lo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop6-DLys(Dop6)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr 25 NH 2 , Dop7-Lys(Dop7)-Caeg-cyclo [DCys-3 Pal-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-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 30 Dop7-Lys(Dop7)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr NH 2 , Dop8-Lys(Dop8)-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys] -Thir(Bzl)-Tyr-NH 2 , H \maraR\Keep\SpeCi\P64461-div-SPEC.doc 7/02/08 - ill Dop8-Lys(Dop8)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, 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(Bz)-Tyr 5 NH 2 , Dop9-Lys(Dop9)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop9-Lys(Dop9)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]l-Ser(Bzl)-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(Bzl)-Tyr NH 2 , DopI O-Lys(Dopl IO)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , Dop 1 O-Lys(Dop 1 O)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr 15 NH 2 , Dop 1 O-Lys(Dop 1 O)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bz) Tyr-NH 2 , Dop 1 O-Lys(Dopl I )-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH- 2 , 20 Dop I11 -Lys(Dopl 11)-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DC ys] -Thr(BzI)-Tyr NH- 2 , DopI I -Lys(Dopl 1 )-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , DopI I -Lys(Dopl 1)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bz) 25 Tyr-NH 2 , DopI 1 -Lys(DoplI 1)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH- 2 , Dop I 2-Lys(Dop I 2)-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 30 DoplI2-Lys(DoplI2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 112 -I DopI 2-Lys(DoplI 2)-Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop 1 2-Lys(Dop 1 2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , 5 Dop 1 3-Lys(Dop 1 3)-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DC ys] -Thr(BzI)-Tyr NH 2 , DopI 3-Lys(DoplI 3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop I 3-Lys(Dopl 3)-Lys-Caeg-cyc lo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(BzI) 10 Tyr-NH 2 , Dop I 3-Lys(DoplI 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 , Dop 1 -Lys(Dop 1 )-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop I -DLys(Dop 1 )-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop I -DLys(Dop I )-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -Lys(DoplI)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , DoplI-DLys(Dopl )-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 , 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-NH 2 , 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(Dop5)-DPhe-cyclojlCys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.dOC 7/02/08 - 113 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 , 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]-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]-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 , 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 O-Lys(Dop 1 0)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop1 O-Lys(Dop 1 0)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop 11-Lys(Dop 11)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dopl1 -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 , Dopl2-Lys(Dop12)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopi3-Lys(Dopl3)-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 , Dop1-DPhe-cyclo[Cys-3ITyr(Dop1)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop1)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1-DLys(Dop1)-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 , Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 114 Dop 1 -Lys(Dopl)-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 , Dop 1 -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop l)-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop1 -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop 1 -DLys(Dop l)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -DLys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , 10 Dop 1 -DLys(Dop l)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dop l)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop 1 -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop 1 -Lys(Dop l)-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 , Dop 1 -DLys(Dop l)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I -Lys(Dop l)-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr 20 NH 2 , Dop 1 -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 , 25 Dopl -DLys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-31Tyr-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-NH2, 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\P64461-div-SPEC.doc 7/02/08 - 115 Dop I -Lys(Dop l )-Lys-DTyr-DTyr-cyclo [Cys-31ITyr-DTrp-Lys-Val-Cys] -Thr NH 2 , Dop I -DLys(Dop 1l)-DTyr-DTyr-cyclo [Cys-31ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop I -DLys(DoplI)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr 5 NH 2 , Dop2-DPhe-cyclo [Cys-3ITyr(Dop2)-DTrp-Lys-Va-Cys]-Thr-NH2, Dop2-Lys(Dop2)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH2, 10 Dop2-Lys(Dop2)-Aepa-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Tin NH 2 , Dop2-Lys(Dop2)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 15 Dop2-DLys(Dop2)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH2, Dop2-DLys(Dop2)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cysl-Thr-NH2, Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH2 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , 20 Dop2-DLys(Dop2)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Tin-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 NH 2 , 25 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Dop2)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Tin-NH 2 , 30 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop2-Lys(Dop2)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Tin-NH 2 , Dop2-DLys(Dop2)-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Tin-NH 2 , H:\maraR\Keep\speci\P64461-div.SPECdOC 7/02/08 - 116 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-3ITyr-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-3ITyr-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-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 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 , 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-3 ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 117 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 , Dop5-DLys(Dop5)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 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 , DopS-DLys(Dop5)-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 10 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 ITyr-DTrp-Lys-Abu-Cys] -Thr 15 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-Val-Cys] -Thr-NH 2 , Dop5-Lys(Dop5).-DPhe-cyclo [Cys-3 ITyr.-DTrp-Lys-Val-Cys] -Thr-NH 2 , 20 Dop5-DLys(Dop5)-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-cyclo[Cys-3 ITyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop5 -DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , 25 Dop5 -DLys(Dop5)-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-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 , Dop8-Lys(Dop8)-cyclolCys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 30 Dop9-Lys(Dop9)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I O-Lys(Dop 1 0)-cyclo [Cys-31ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dopl 11-Lys(Dopl 11)-cyclo [Cys-31ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-divSPEC.doc 1/02/08 - 118 Dop 1 2-Lys(Dop I 2)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I 3-Lys(Dop 13)-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 , 5 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 I O-Lys(Dop 1 0)-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-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or 10 DopI 3-Lys(Dop1 3)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]- Thr-NH 2 ; or a pharmaceutically acceptable salt thereof; and wherein said effective amount is the amount effective to elicit a dopamine receptor agonist effect in said subject. 15 2. The method of claim 1, wherein said chimeric analogue comprises a compound according to the formula of: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DPhe-Doc-DPhe-cyclo[Cys-3lTyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 25 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 , 30 Dop2-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 119 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 5 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof.
3. The method of claim 2, wherein said chimeric analogue comprises a compound according to the formula of: 10 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 Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 15 4. The method of claim 3, wherein said chimeric analogue 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 5. The method of claim 3, wherein said 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. 25 6. The method of claim 3, wherein said chimeric analogue comprises a compound according to the formula of: Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 30 7. The method of claim 1, wherein said chimeric analogue comprises a compound according to the formula of: Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 120 Dop2-DTyr-DTyr-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-Dcys] -Thr(Bzl)-Tyr-NH 2 ; or a pharmaceutically acceptable salt thereof. 5 8. 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 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) as set forth 10 herein; or a pharmaceutically acceptable salt thereof; wherein the compound is selected from: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop2-Lys(Ac)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Ac)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop4-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 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 , 25 Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , DopI O-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I I-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop1 2-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 13-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 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 , 1156528_1 (GHMatters) 7/06/10 - 121 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 11-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop12-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 13 -cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , 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 , 10 Dop8-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop9-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 O-D2Nal-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dopl I -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 , 15 Dop 13 -D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , 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 , 20 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 1 I-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 2-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 13-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 25 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, 30 Dop I O-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 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, H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 122 Dop 13-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 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, 5 Dop8-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop9-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 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, 10 Dop I 3-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 , Dop7-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop8-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 15 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 , Dop 11-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopl2-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop13-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 20 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 , Dop9-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 25 Dop10-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 11-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 , Dop1-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 123 Dop3 -Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop3 -DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 5 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 , 10 Dop I O-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , DopI 11-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , DoplI2-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , DopI 13-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop3 -cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 15 Dop4-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 , Dop8-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 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 , Dopl 1-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl12-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop13 -cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 25 Dopl1-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2, Dop2-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop3-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop4-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , DoplI-Aepa-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 30 Dop2-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCys] -Thr(Bzl)-Tyr-N H 2 , Dop3 -Aepa-Caeg-cyc lo [ DCys-3 PalI-DTrp- Lys-D Cys] -Thr(B zl)-Tyr-NH 2 , Dop4-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCysI -Thr(Bzl)-Tyr-N H 2 , H:\maraR\Keep\Speci\P64461-div-SPECdoC 7/02/08 - 124 Dop5-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop6-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop7-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop8-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 5 Dop9-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop I O-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop 11 -Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop I2-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bz)-Tyr-NH2, Dop 13 -Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 10 Dop I -Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop3-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop4-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop 1 -Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 15 Dop2-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop3-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop4-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, 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, 20 Dop7-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop8-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop9-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop 1 O-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop 11-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, 25 Dop12-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop 13-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 , 30 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 125 Dop 1-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dopl12-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 , 5 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 , Dop I O-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 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-N H 2 , Dop 13 -DPhe-cyc lo [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 , 15 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 , 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-N H 2 , Dopl 1-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 Dop 1 2-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop 13 3-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-NH2, 25 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 30 NH 2 , Dop2-DLys(Dop2)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop 1 )-DPhe-cyc lo [Cys-Tyr-DTrp- Lys-Abu-Cys] -Thr-N H 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 126 Dop I -Lys(Dop l)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dopl)-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 , 5 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I -DLys(Dopl)-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 , Dop 1 -DLys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I -DLys(Dop 1 )-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr 10 NH 2 , Dop 1 -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 , Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr 15 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-NH2, 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 20 NH 2 , 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, Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 25 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 , DopI-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop1 -Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , 30 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 127 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 NH 2 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-N H 2 , 5 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 , Dop2-DLys(Dop2)-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-N H 2 , 10 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]-Th7-NH2, Dop2-DLys(Dop2)-Aepa-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 15 Dop2-Lys(Dop2)-D2Na1-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, Dop2-Lys(Dop2)-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys]l-Thr-NH2, 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-Va-Cys] -Thr-NH 2 , 20 Dop2-Lys(Dop2)-DPhe-cyclollCys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop2-Lys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, 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 , 25 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop2-Lys(Dop2)-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, 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-CysI -Trp-NH 2 , 30 Dop2-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-VaI-Cys] -Trp-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-VaI-Cys]-Trp NH 2 , H:\MaraR\Keep\Speei\P64461-diV-SPECdoC 7/02/OR - 128 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 , Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 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-NH2, 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 , 10 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 , 15 Dop3-Lys(Dop3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, 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-NH2, 20 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-NH2, Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 25 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 , 30 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 129 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-NH2, 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 5 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-NH2, 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-NH 2 , Dop4-Lys(Dop4)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 15 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, 20 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, 25 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, 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 30 NH 2 , Dop4-Lys(Dop4)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 130 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 5 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 , 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 10 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 , 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 15 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 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal 20 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, 25 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, 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 , 30 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 131 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 , 5 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-NH2, Dop6-Lys(Dop6)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 10 Dop6-Lys(Dop6)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, 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-NH2, 15 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-ol, 20 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 , 25 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 , 30 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 132 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, 5 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 , 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, 10 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, 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 , 15 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-NH2, 20 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 , 25 Dop9-Lys(Dop9)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2, 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 , 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, 30 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 , Dop1O-Lys(Dop10)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 133 Dop 1 0-Lys(Dop1 0)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop1 O-DLys(Dop 1 0)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 0-DLys(Dop 1 0)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop 1 O-Lys(Dop1 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 , Dop O-Lys(Dop1 0)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 10-Lys(Dop1 0)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop O-Lys(Dop1 0)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 10 Dop 1 0-Lys(Dop1 0)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 10-Lys(Dop1 0)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop 10-Lys(Dop10)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop 11-Lys(Dopl1 )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11-Lys(Dop 11)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 Dop 11-DLys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11-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-NH2, Dop 11-Lys(Dopl1 )-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 20 Dop 11-Lys(Dop 11)-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, Dop 11-Lys(Dop 11)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 11-Lys(Dopl1 )-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, 25 Dop 1-Lys(Dopl 1)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop12-Lys(Dopl2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, 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 , 30 Dop12-Lys(Dop12)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , DopI2-Lys(Dop12)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, H.\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 134 Dop I 2-Lys(Dop1 2)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop I 2-Lys(Dop 1 2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop1 2-Lys(Dop 1 2)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop1 2-Lys(Dop1 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , 5 Dop12-Lys(Dop12)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dop13-Lys(Dop13)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl3-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 , Dopl3-DLys(Dop13)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop13-Lys(Dop13)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 13 -Lys(Dop I 3)-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Thr-NH 2 , Dop 13 -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-NH 2 , 15 Dop 13 -Lys(Dop 1 3)-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, Dop 13 -Lys(Dop 1 3)-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Val-Cys] -Trp-NH 2 , Dopl 3-Lys(Dop13)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dopl-Lys(Dopl)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 20 DopI-Lys(Dop1)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop I -DLys(Dop 1)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dopl-DLys(Dop1)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dopl-Lys(Dop1)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr 25 NH 2 , Dopl-Lys(Dopl)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dopi -DLys(Dopl)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , 30 Dopl-DLys(Dopl)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 135 Dop I -Lys(Dop 1 )-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop 1 -Lys(Dop I )-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , 5 Dop I -DLys(Dop 1 )-Aepa-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop 1 -DLys(Dop 1 )-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]l-Ser(Bzl) Tyr-NH 2 , Dop I -Lys(Dopl )-Lys-Aepa-Caeg-cyclo[DCys-3PaI-DTrp-Lys-DCys]-Thr(Bzl) 10 Tyr-NH 2 , DoplI -Lys(Dop 1 )-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI) Tyr-NH 2 , DoplI-DLys(Dopl )-Lys-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys] Thr(Bzl)-Tyr-NH 2 , 15 Dop I -DLys(Dop 1 )-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] 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-cyclollDCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop2-DLys(Dop2)-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-Tyr 20 NH 2 , Dop2-DLys(Dop2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, Dop2-Lys(Dop2)- Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DC ys] -Thr(BzI)-Tyr NH 2 , Dop2-Lys(Dop2)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 25 NH 2 , Dop2-DLys(Dop2)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop2-DLys(Dop2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , 30 Dop2 -Lys(Dop2)-Aepa-Caeg-cyc lo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH 2 , HA\MarR\Kecp\spci\P64461-di--SPEC.doC 7/02/08 - 136 Dop2-Lys(Dop2)-Aepa-Caeg-cycloI[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz1)-Tyr NH 2 , Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , 5 Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl) Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclolDCys-3 Pal-DTrp-Lys-DCys]-Thr(BzI) Tyr-NH 2 , Dop2-Lys(Dop2)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Sr(BzI) 10 Tyr-NH 2 , 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 , 15 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(Bzl)-Tyr-NH 2 , 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-DCys] -Ser(Bzl)-Tyr 20 NH 2 , 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(BzI)-Tyr NH 2 , 25 Dop3 -DLys(Dop3)-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop3-DLys(Dop3 )-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , Dop3 -DLys(Dop3 )- Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , 30 Dop3-DLys(Dop3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 137 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 , 5 Dop4-Lys(Dop4)-Caeg-cyc lo [DCys-3 Pal-.DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop4-Lys(Dop4)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-N H 2 , Dop4-Lys(Dop4)-Lys-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 Dop4-Lys(Dop4)-Lys-Caeg.cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr 10 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(BzI)-Tyr NH 2 15 Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]I-Ser(Bz1) Tyr-NH 2 , Dop4-DLys(Dop4)-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr 20 NH 2 , 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(BzI)-Tyr NH 2 , Dop4-DLys(Dop4)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr 25 NH 2 , Dop4-DLys(Dop4)-Aepa-Caeg-cyc lo [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 , 30 Dop4-DLys(Dop4)-Lys-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys] Thr(Bzl)-Tyr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 138 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 Pal-DTrp- Lys-DCys] -Thr(Bz)-Tyr-N H2, Dop5-Lys(Dop5)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , 5 Dop5-DLys(Dop5)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(BzI)-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-3 PaI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 10 Dop5-Lys(Dop5)-Lys-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr NH- 2 , Dop5 -DLys(Dop5)-Lys-Caeg-cyclo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop5-DLys(Dop5)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr 15 NH 2 , Dop6-Lys(Dop6)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , Dop6-Lys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , 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(BzI)-Tyr NH 2 , Dop6-Lys(Dop6)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , 25 Dop6-DLys(Dop6)- Lys-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DC ys] -Thr(BzI)-Tyr NH 2 , Dop6-DLys(Dop6)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(13z1)-Tyr NH 2 , Dop7-Lys(Dop7)-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 30 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(BzI)-Tyr NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPECdoc 7/02/08 - 139 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(Bzl)-Tyr-NH2, Dop8-Lys(Dop8)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, 5 Dop8-Lys(Dop8)-Lys-Caeg-cyclo [DCys-3 PaI-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-cyclolDCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , 10 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 , Dop9-Lys(Dop9)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , 15 Dop 1 O-Lys(Dopl I )-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop I O-Lys(Dop 1 O)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , Dop 1 O-Lys(Dop I 0)-Lys-Caeg-cyc lo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI) 20 Tyr-NH 2 , Dop 1 O-Lys(Dop 1 O)-Lys-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop I 1 -Lys(Dopl I1)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bz)-Tyr NH 2 , 25 DopI 11-Lys(Dopl 11)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , DopI I-Lys(Dopl 11)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , DopI 1 -Lys(Dopl 1)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr 30 NH 2 , Dop I 2-Lys(DoplI 2)-Caeg-cyc lo [DCys-3 PalI-DTrp- Lys-DCys] -Thr(Bzl)-Tyr NH 2 , H:\maraR\Keep\speci\P64461-div-SPECdoc 7/02/08 - 140 Dop I 2-Lys(Dop I 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 Pal-DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , 5 Dop I 2-Lys(Dop 1 2)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dopi 3-Lys(Dopl 3)-Caeg-cyclo[DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop 1 3-Lys(Dopl 3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 10 NH 2 , Dopi 3-Lys(Dopl 3)- Lys-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , Dop 1 3-Lys(Dop 1 3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , 15 Dop 1 -Lys(DoplI)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop 1 -Lys(Dopl1)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-N H 2 , Dop I -DLys(Dopl1)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop I -DLys(DoplI)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 -Lys(DoplI)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 Dop I -DLys(DoplI)-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 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 , 25 Dop2-Lys(Dop2)-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop2-DLys(Dop2)-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, 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-Cys1-Thr-NH2, 30 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-NH 2 , H:\MarR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 141 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 , 5 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]-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]-NH 2 , 10 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 , Dop7-Lys(Dop7)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 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 , 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-NH2, 20 Dop O-Lys(Dop 1 0)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop1 O-Lys(Dop 1 0)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopi 1 -Lys(Dopl 1)-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-NH 2 , Dop1 2-Lys(Dop 1 2)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , 25 Dop1 2-Lys(Dop 1 2)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 13-Lys(Dop 1 3)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop 13-Lys(Dopl 3)-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 -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 , 30 Dop1 -DLys(Dop1)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1 -DLys(Dop1)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 142 Dop 1 -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop I -DLys(Dop 1)-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 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 , Dop 1 -DLys(Dop 1)-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dop 1 -DLys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop I -DLys(Dop I)-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -DLys(Dop l)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys)-Thr NH 2 , 15 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I -DLys(Dop 1)-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dop I -Lys(Dop 1)-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys)-Thr-NH 2 , Dop I -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , Dop 1 -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 25 Dop 1 -DLys(Dop 1 )-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , Dop 1 -DLys(Dop I)-DPhe-cyclo[Cys-3 ITyr-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 , Dop 1 -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 30 Dop 1 -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop 1)-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 143 Dopl -DLys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dop l)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dop 1)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , 5 Dop 1 -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-NH2, 10 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 , Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 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-NH2, 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 20 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 , 25 Dop2-DLys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr 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 , 30 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 144 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 , 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 5 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 , 10 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-NH 2 , 15 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-NH2, Dop2-Lys(Dop2)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , 20 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 , 25 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 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop5-Lys(Dop5)-DPhe-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 145 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 5 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 LTyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop5-DLys(Dop5)-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dop5-Lys(Dop5)-cyclo [Cys-3 lTyr-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 LTyr-DTrp-Lys-Abu-Cys]-Thr 15 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-Val-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-VaI-Cys] -Thr-NH 2 , 20 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 25 NH 2 , Dop5-DLys(Dop5 )-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop5-DLys(Dop5 )-Lys-DTyr-DTyr-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr NH 2 , Dop6-Lys(Dop6)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 30 Dop7-Lys(Dop7)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop8-Lys(Dop8)-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop9-Lys(Dop9)-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , H:\maraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 146 DopI O-Lys(Dopl 0)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl 1-Lys(Dopl 1)-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(Dop13)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dop6-Lys(Dop6)-DPhe-cyclo[Cys-3lTyr-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-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop1O-Lys(Dop1O)-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(Dop12)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or Dop13-Lys(Dop 1 3)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]- Thr-NH 2 ; or a pharmaceutically acceptable salt thereof; and wherein said effective amount is the amount effective to elicit a somatostatin 15 receptor agonist effect in said subject.
9. The method of claim 8, wherein said chimeric analogue comprises a compound according to the formula of: Dop2-DPhe-Doc-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 20 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-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 , 30 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 , 1156528_1 (GHMatters) 7/06/10 - 147 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 , 5 Dop2-Lys(Dop2)-DPhe-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , or Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. 10 10. The method of claim 9, wherein said chimeric analogue 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 Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 .or 15 a pharmaceutically acceptable salt thereof.
11. The method of claim 10, wherein said chimeric analogue comprises a compound according to the formula of: Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2; 20 a pharmaceutically acceptable salt thereof.
12. The method of claim 10, wherein said chimeric analogue comprises a compound according to the formula of: Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 ; or 25 a pharmaceutically acceptable salt thereof.
13. The method of claim 10, wherein said chimeric analogue comprises a compound according to the formula of: Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 .or 30 a pharmaceutically acceptable salt thereof.
14. The method of claim 8, wherein said chimeric analogue comprises a compound according to the formula of: H:\MaraR\Keep\Speci\P64461-di-SPEC.doC 7/02/08 - 148 Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or Dop2-DTyr-DTyr-Caeg-cyclo[DCys-3Pal-DTrp-Lys-Dcys]-Thr(Bz)-Tyr-NH 2 ; or 5 a pharmaceutically acceptable salt thereof.
15. A method of eliciting both a dopamine receptor agonist effect and 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 10 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) as set forth herein; or a pharmaceutically acceptable salt thereof; wherein the compound is selected from: 15 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop2-Lys(Ac)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DLys(Ac)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 20 Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop3-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop4-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 25 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 , Dop9-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop10-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop 1 -DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl 2-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopi 3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 1156528_1 (GHMatters) 7/06/10 - 149 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 , 5 Dop9-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 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 , Dop 1 2-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 13-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dop5-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop6-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH2 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 , i5 Dop1 0-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 11 -D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1 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 , 20 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 , Dop1 0-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 25 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-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\P64461-div-SPEC.doC 7/02/08 - 150 Dop I O-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop I1I -DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop I 2-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl 13-DPhe-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-oI, 5 Dop5 -cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, 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 Dopl 1 -cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 11I -cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop I 2-cyclo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-oI, Dop 13 -cyc lo [Cys-Phe-DTrp-Lys-Thr-Cys] -Thr-ol, Dop5 -DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys]-2Na-NH 2 , 15 Dop6-DPhe-cyclo [Cys-Tyr-DTrp-Lys-Thr-Cys] -2NaI-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]-2Na-NH 2 , 20 Dop 11I -DPhe-cyclollCys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop 1 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 1 O-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dop] 1-cycle [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , 30 Dopl12-cycle [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dop13 -cycle [Cys-Tyr-DTrp-Lys-Thr-Cys] -2Nal-NH 2 , Dopl1-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , H:\MaraR\Keep\Speci\P6446l-div-SPEC.doC 7/02/08 - 151 Dop2-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 -Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop2-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop3 -Aepa-DPhe-cyclolCys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 5 Dop4-Aepa-DPhe-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop3-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop4-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 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 , 10 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 , 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-NH2, DopI 11-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 DoplI2-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 , Dop3 -cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop4-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , DopS-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 20 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 0-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 25 Dop 1-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 2-cyclo[Cys-3 ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I 3-cyclo [Cys-3 LTyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 -Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , Dop2-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2, 30 Dop3 -Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , Dop4-Caeg-cyclo [DCys-3 PalI-DTrp-Lys- DCys] -Thr(Bz)-Tyr-NH 2 , Dop 1 -Aepa-Caeg-cycl o [DCys-3 Pal -DTrp- Lys-DCys] -Thr(Bzl)-Tyr-N H 2 , H:\maraR\Keep\speci\P64461-div-SPECdoc 7/02/08 - 152 Dop2-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop3-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop4-Aepa-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop5-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , 5 Dop6-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop7-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop8-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop9-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop1 0-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 10 Dop 11 -Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , DopI 2-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop 13-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , DopI -Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 15 Dop3-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop4-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , DopI -Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop2-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop3-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 20 Dop4-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop5-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH2, Dop6-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-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 , 25 Dop9-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dopl O-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , DopI I -Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , DopI 2-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop 13-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-SerBzl)-Tyr-NH 2 , 30 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 153 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 , Dopl 1-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cysl -NH 2 , 5 Dop 1 2-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop 1 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 , 10 Dop8-DPhe-cyclollCys-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 1 O-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH2, Dop I1I -DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 2-DPhe-cycloIICys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop 1 3-DPhe-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-N H 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-NH2, 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 I11 -cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 2-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I 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]l-Thr-NH2, 30 Dop2-Lys(Dop2)-Lys-DTyr-DTyr-cyclo [Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr NH 2 , H:\MaraR\Keep\Speci\P6446div-SPECdOC 7/02/08 - 154 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 , Dop I -Lys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 5 Dop I -Lys(Dopl)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -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 1 -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 Dopl -DLys(Dop l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I -DLys(Dop l)-Aepa-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 1 -DLys(Dopl)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl -DLys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 15 Dop 1 -DLys(Dopl)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2, Dop 1 -Lys(Dopl)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I -Lys(Dop l)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I -Lys(Dop l)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr NH 2 , 20 Dop 1 -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 Dop 1 -Lys(Dop1)-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, Dopl -Lys(Dopl)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl -Lys(Dopl)-Lys-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 30 Dopl -Lys(Dop2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , DopI-Lys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 155 Dop I -Lys(Dop2)-Lys-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp NH 2 , Dop I -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-NH2, 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-NH 2 , 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-NH2, 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-NH 2 , 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-NH2, 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\P64461-div-SPEC.doc 7/02/08 - 156 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 , 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-NH 2 , 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-NH2, 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-NH2, 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-NH 2 , Dop3-Lys(Dop3)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, 25 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-NH2, 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\P64461-div-SPEC.doc 7/02/08 - 157 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-NH2, 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-NH2, 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\P64461-div-SPEC.doC 7/02/08 - 158 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 , 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-NH 2 , 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-NH2, 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-NH2, Dop5-Lys(Dop5)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 159 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\P64461-div-SPEC.doc 7/02/08 - 160 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 , 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-NH2, 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-NH2, Dop8-Lys(Dop8)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , 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-NH2, 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-NH2, 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\P64461-div-SPEC.doc 7/02/08 - 161 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 DopI0-Lys(Dop10)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , DopIO-Lys(Dop10)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop1O-DLys(Dop1O)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , DopI0-DLys(Dop1O)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 10 DopIO-Lys(Dop10)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , DopI0-Lys(Dop10)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1O-Lys(Dop1O)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop10-Lys(Dop1O)-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , DopI0-Lys(Dop10)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, 15 DopIO-Lys(Dop10)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, DopI0-Lys(Dop10)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, Dop 1 O-Lys(Dop 10)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , Dopl 1-Lys(Dopl l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dopl I-Lys(Dopl l)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 20 Dopl l-DLys(Dopl l)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop 11 -DLys(Dop 11 )-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop I1-Lys(Dopl l)-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 II -Lys(Dop ll)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH2, Dop 11 -Lys(Dop 11 )-cyclo[Cys-Tyr-DTrp-Lys-Thr-Cys]-2Nal-NH 2 , Dopll-Lys(Dopl l)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 11-Lys(Dop1 1)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop I1-Lys(Dop 11)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH2, 30 Dop I-Lys(Dop 11)- cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Trp-NH 2 , DopI2-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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 162 DopI 2-DLys(DopI 2)-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop1 2-DLys(Dop I 2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , DopI 2-Lys(Dop 1 2)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I 2-Lys(Dop 1 2)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop I 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-NH 2 , DopI 2-Lys(Dop1 2)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop1 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(Dop12)- 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(DopI3)-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 , 15 Dop 13-Lys(Dop1 3)-D2Nal-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop I 3-Lys(Dop 1 3)-cyclo[Cys-Tyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 13-Lys(Dop 13)-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 , 20 Dop 13-Lys(Dop 1 3)-DPhe-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 13-Lys(Dop I 3)-cyclo[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-ol, Dop 13-Lys(Dop I 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 , Dop1-Lys(Dop1)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH2, 25 DopI-Lys(Dop1)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 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 , Dopl-Lys(Dop1)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr 30 NH 2 , Dop 1 -Lys(Dop 1)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 163 Dop 1 -DLys(Dop 1 )-Lys-Caeg-cyclo[DCys-3PaI-DTrp-Lys-DCys]-Thr(Bz)-Tyr NH 2 , Dopi -DLys(Dopl )-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr NH 2 , 5 Dop 1 -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 NH 2 , Dop 1 -DLys(Dop 1 )-Aepa-Caeg-cyclollDCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) 10 Tyr-NH 2 , Dop I -DLys(Dop I )-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI) Tyr-NH 2 , Dop 1 -Lys(Dop 1 )-Lys-Aepa-Caeg-cyclo [DCys-3 Pal -DTrp- Lys-DCys] -Thr(BzI) Tyr-NH 2 , 15 Dop 1 -Lys(Dop I )-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(BzI) Tyr-NH 2 , Dop 1 -DLys(Dop I )-Lys-Aepa-Caeg-cyclollDCys-3PaI-DTrp-Lys-DCys] Thr(Bzl)-Tyr-NH 2 , Dop I -DLys(Dop I )-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] 20 Ser(Bzl)-Tyr-N H 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(Bzl)-Tyr-NH 2 , Dop2-DLys(Dop2)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , 25 Dop2-DLys(Dop2)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , Dop2-Lys(Dop2)- Lys-Caeg-cyclo [DCys-3 PalI-DTrp-Lys-DCys] -Thr(BzI)-Tyr NH 2 , Dop2-Lys(Dop2)-.Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , 30 Dop2-DLys(Dop2)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , H:\MaraR\Kep\SPeCi\P64461-diV-SPEC.doc 7/02/08 - 164 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 NH 2 , 5 Dop2-Lys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop2-D Lys(Dop2)-Aepa-Caeg-cyc lo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , Dop2-DLys(Dop2)-Aepa-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl) 10 Tyr-NH 2 , Dop2 -Lys(Dop2)-Lys-Aepa-Caeg-cyc lo [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 PalI-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(Bzl)-Tyr-NH 2 , 20 Dop3-Lys(Dop3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, 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 , 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(Bzl)-Tyr 30 NH 2 , Dop3 -DLys(Dop3 )-Caeg-cycloj[DCys-Phe-DTrp-Lys-DCys1-Ser(Bz1)-Tyr-NH 2 , H;\MaraR\Keep\Speci\P64461-div-SPEC.dOC 7/02/08 - 165 Dop3 -DLys(Dop3 )- Lys-Caeg-cyclo [DC ys-3 PalI-DTrp-Lys-DC ys] -Thr(Bzl)-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(BzI) Tyr-NH 2 , Dop3 -DLys(Dop3 )-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl) Tyr-NH 2 , Dop4-Lys(Dop4)-Caeg-cyclo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(Bz1)-Tyr-NH2, 10 Dop4-Lys(Dop4)-Caeg-cyclolDCys-Phe-DTrp-Lys-DCysI-Ser(Bz)-Tyr-NH2, 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(Bz)-Tyr NH 2 15 Dop4-Lys(Dop4)-Aepa-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(BzI)-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 PalI-DTrp-Lys- DCys] -Thr(Bzl) 20 Tyr-NH 2 , Dop4-Lys(Dop4)-Lys-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl) Tyr-NH 2 , Dop4-DLys(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(Bz1)-Tyr NH 2 , 30 Dop4-D Lys(Dop4)-Aepa-Caeg-cyc lo [DCys-3 Pal -DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPECdOc 7/02/08 - 166 Dop4-DLys(Dop4)-Aepa-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bz) 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-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , Dop5-Lys(Dop5)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH 2 , Dop5-DLys(Dop5)-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr 10 NH 2 , Dop5 -DLys(Dop5)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys]-Ser(Bz)-Tyr-NH2, Dop5 -Lys(Dop5)-Lys-Caeg-cycl o[DCys-3 PalI-DTrp-Lys-DCys] -Thr(Bz)-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-3Pal-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-3 Pal-DTrp-Lys-DCys] -Thr(BzI)-Tyr-NH 2 , Dop6-Lys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(BzI)-Tyr-NH 2 , Dop6-DLys(Dop6)-Caeg-cyclo [DCys-3 Pal- DTrp- Lys-DCys] -Thr(BzI)-Tyr NH- 2 , Dop6-DLys(Dop6)-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr-NH 2 , 25 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-3 Pal-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\P64461div-SPEC.doC 7/02/06 - 167 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-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-3Pal-DTrp-Lys-DCys] -Thr(Bzl)-Tyr-NH 2 , 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 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-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr-NH 2 , Dop9-Lys(Dop9)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr-NH 2 , 15 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(Bzl)-Tyr NH 2 , DopI O-Lys(Dop1 0)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr 20 NH 2 , DopI O-Lys(Dopl 0)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dop O-Lys(Dop 1 0)-Lys-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , 25 Dopl O-Lys(Dop1 0)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , Dopi I-Lys(Dopl 1)-Caeg-cyclo[DCys-3Pal-DTrp-Lys-DCys]-Thr(Bzl)-Tyr NH 2 , DopI1 -Lys(Dopl 1)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 30 NH 2 , Dop 11-Lys(Dop 11)-Lys-Caeg-cyclo[DCys-3 Pal-DTrp-Lys-DCys]-Thr(Bzl) Tyr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 168 Dop I11 -Lys(Dopl 11)-Lys-Caeg-cyclo [DCys-Phe-DTrp-Lys-DCys] -Ser(Bzl)-Tyr NH 2 , Dop 1 2-Lys(Dop 1 2)-Caeg-cyclo [DCys-3 PaI-DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , 5 Dopi 2-Lys(DoplI 2)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , Dop 1 2-Lys(Dop 1 2)-Lys-Caeg-cyclo [DCys-3 Pal-DTrp-Lys-DCys] -Thr(BzI) Tyr-NH 2 , Dop 1 2-Lys(Dop 1 2)-Lys-Caeg-cyclollDCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr 10 NH 2 , Dop I 3-Lys(DoplI 3)-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl)-Tyr NH 2 , Dop I 3-Lys(DoplI 3)-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(Bzl)-Tyr NH 2 , 15 DoplI3-Lys(Dopl 3)-Lys-Caeg-cyclo [DCys-3 Pal- DTrp-Lys-DCys] -Thr(Bzl) Tyr-NH 2 , Dop I 3-Lys(DoplI 3)-Lys-Caeg-cyclo[DCys-Phe-DTrp-Lys-DCys]-Ser(BzI)-Tyr NH 2 , Dop I -Lys(DoplI)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , 20 Dop 1 -Lys(DoplI)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dopi -DLys(Dopl )-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 I -Lys(Dopl1)-cyclo[Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 1 -DLys(Dopl1)-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]-NH 2 , Dop2-Lys(Dop2)-DPhe-cyclollCys-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-NH2, 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\P64461-div-SPEC.dOC 7/02/08 - 169 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-NH 2 , 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-NH2, 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-CysI-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-NH2, 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] -NH 2 , 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-NH 2 , 20 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-CysI-Thr-NH2, 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-NH2, Dop I O-Lys(Dop 1 0)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , 25 Dop I O-Lys(Dopl I )-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 11I -Lys(Dop 11 )-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH2, Dop I11 -Lys(Dop 11 )-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop I 2-Lys(Dop 1 2)-cyclo [Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys] -NH 2 , Dop 1 2-Lys(Dop I 2)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , 30 DoplI3-Lys(Dopl 3)-cyclo[Cys-Phe-Phe-DTrp-Lys-Thr-Phe-Cys]-NH 2 , Dop 1 3-Lys(Dop 1 3)-DPhe-cyclo [Cys-Phe-(N-Me)DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 -DPhe-cyclo [Cys-31ITyr(Dop 1 )-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPECdoC 7/02/08 - 170 Dop 1 -DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop 1)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 -DLys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 Dopl -Lys(Dopl)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop I -Lys(Dop I)-Aepa-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , Dop 1 -DLys(Dop 1 )-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr-NH 2 , 10 Dop 1 -Lys(Dop I)-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 , Dop I -DLys(Dop I )-Lys-DTyr-DTyr-cyclo [Cys-3 ITyr-DTrp-Lys-Thr-Cys] -Thr 15 NH 2 , Dop 1 -DLys(Dop 1)-DPhe-cyclo [Cys-3 ITyr-DTrp-Lys-Abu-Cys] -Thr-NH 2 , Dopl -DLys(Dopl)-Aepa-DPhe-cyclo[Cys-31Tyr-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 , 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 , 25 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 30 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 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 171 Dop I -Lys(Dop l)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop l)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop 1 -Lys(Dop l)-Aepa-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , 5 Dop 1 -DLys(Dop l)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dopl -Lys(Dopl)-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop1 -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, 10 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 , Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 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 , 20 Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH2, Dop2-DLys(Dop2)-Aepa-DPhe-cyclo[Cys-31Tyr-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 25 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 30 NH 2 , Dop2-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.dOC 7/02/08 - 172 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-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 , 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-3ITyr-DTrp-Lys-Abu-Cys]-Thr NH 2 , 15 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-3 ITyr-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-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-3 ITyr-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-3ITyr-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-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 173 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 , 5 Dop5-Lys(Dop5)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-Lys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3lTyr-DTrp-Lys-Thr-Cys]-Thr NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop5-DLys(Dop5)-Lys-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr 10 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 , Dop5-Lys(Dop5)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 15 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 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3lTyr-DTrp-Lys-Abu-Cys]-Thr 20 NH 2 , 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 , 25 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-3ITyr-DTrp-Lys-Val-Cys]-Thr 30 NH 2 , Dop5-DLys(Dop5)-DTyr-DTyr-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 174 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 , Dop7-Lys(Dop7)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 5 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 1 O-Lys(Dop1 0)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop 11-Lys(Dop1 )-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop12-Lys(Dop12)-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 10 Dopl 3-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 , Dop9-Lys(Dop9)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , 15 Dop10-Lys(Dop10)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dopi1 -Lys(Dopl 1)-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 Dop 13-Lys(Dop1 3)-DPhe-cyclo[Cys-31Tyr-DTrp-Lys-Thr-Cys]- Thr-NH 2 ; or a pharmaceutically acceptable salt thereof; and 20 wherein said effective amount is the amount effective to elicit both a dopamine receptor agonist effect and a somatostatin receptor agonist effect in said subject.
16. The method of claim 15, wherein said chimeric analogue comprises a compound according to the formula of: 25 Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Val-Cys]-Thr-NH 2 , Dop2-DPhe-Doc-DPhe-cyclo[Cys-3ITyr(Dop2)-DTrp-Lys-Val-Cys]-Thr-NH 2 , Ac-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Ac-DLys(Dop2)-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , Dop3-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , 30 Dop4-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop5-DPhe-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 , Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 , H:\MaraR\Keep\Speci\P64461-div-SPEC.doC 7/02/08 - 175 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-NH2, 5 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 , 10 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 a pharmaceutically acceptable salt thereof. 15
17. The method of claim 16, wherein said chimeric analogue 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 20 Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 .or a pharmaceutically acceptable salt thereof.
18. The method of claim 17, wherein said chimeric analogue comprises a compound according to the formula of 25 Dop2-Lys(Dop2)-DTyr-DTyr-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH2; a pharmaceutically acceptable salt thereof.
19. The method of claim 17, wherein said chimeric analogue comprises a compound according to the formula of 30 Dop2-DLys(Dop2)-cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 ; or a pharmaceutically acceptable salt thereof. H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08 - 176 20. The method of claim 17, wherein said chimeric analogue comprises a compound according to the formula of Dop2-DPhe-cyclo[Cys-3ITyr-DTrp-Lys-Thr-Cys]-Thr-NH 2 .or a pharmaceutically acceptable salt thereof. 5
21. The method of claim 15, wherein said chimeric analogue comprises a compound according to the formula of: Dop2-Lys(Dop2)-DTyr-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], Dop2-Tyr-cyclo[DDab-Arg-Phe-Phe-DTrp-Lys-Thr-Phe], or 10 Dop2-DTyr-DTyr-Caeg-cyclo[DCys-3Pal-DTrp-Lys-Dcys]-Thr(Bzl)-Tyr-NH2; or a pharmaceutically acceptable salt thereof. H:\MaraR\Keep\Speci\P64461-div-SPEC.doc 7/02/08
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|---|---|---|---|
| AU2008200693A Ceased AU2008200693B2 (en) | 2003-04-11 | 2008-02-14 | Treatment of disease or condition with somatostatin-dopamine chimeric analogs |
| AU2008200694A Ceased AU2008200694B2 (en) | 2003-04-11 | 2008-02-14 | Method of treating acromegaly, hyperprolactinemia, portal hypertension and gastrointestinal bleeding with somatostatin-dopamine chimeric analogs |
| AU2008200692A Ceased AU2008200692B2 (en) | 2003-04-11 | 2008-02-14 | Eliciting a dopamine receptor agonist effect with somatostatin-dopamine chimeric analogs |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2008200693A Ceased AU2008200693B2 (en) | 2003-04-11 | 2008-02-14 | Treatment of disease or condition with somatostatin-dopamine chimeric analogs |
| AU2008200694A Ceased AU2008200694B2 (en) | 2003-04-11 | 2008-02-14 | Method of treating acromegaly, hyperprolactinemia, portal hypertension and gastrointestinal bleeding with somatostatin-dopamine chimeric analogs |
Country Status (1)
| Country | Link |
|---|---|
| AU (3) | AU2008200693B2 (en) |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60231403D1 (en) * | 2001-06-08 | 2009-04-16 | Sod Conseils Rech Applic | CHIMERO SOMATOSTATIN DOPAMINE ANALOGUE |
-
2008
- 2008-02-14 AU AU2008200693A patent/AU2008200693B2/en not_active Ceased
- 2008-02-14 AU AU2008200694A patent/AU2008200694B2/en not_active Ceased
- 2008-02-14 AU AU2008200692A patent/AU2008200692B2/en not_active Ceased
Non-Patent Citations (1)
| Title |
|---|
| Saveanu, A. Journal of Clin. Endocrinol. Metab. (2002) 87(12) 5545-5552 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2008200694A1 (en) | 2008-03-06 |
| AU2008200693B2 (en) | 2010-07-08 |
| AU2008200694B2 (en) | 2011-04-14 |
| AU2008200693A1 (en) | 2008-03-06 |
| AU2008200692A1 (en) | 2008-03-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |