US2022339239A1PendingUtilityA1
Use of melanocortins to treat insulin sensitivity
Est. expiryNov 5, 2027(~1.3 yrs left)· nominal 20-yr term from priority
A61K 38/33A61P 3/10A61K 38/04A61K 38/12A61P 3/00A61P 3/04A61P 43/00C07K 7/64A61P 5/50
78
PatentIndex Score
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Claims
Abstract
The present invention relates to peptide ligands of the melanocortin receptors, in particular the melancortin-4 receptor, and as such, are useful in the treatment of disorders responsive to the activation of this receptor, such as insulin resistance.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A method of treating insulin resistance in a subject in need thereof, comprising peripheral administration of an effective amount of a melanocortin receptor 4 agonist to treat said insulin resistance in said subject in need thereof.
2 . The method according to claim 1 , where in said melanocortin receptor 4 agonist useful to treat insulin resistance is selected from the group consisting of:
SEQ ID NO: 1
Ac-Nle-c(Asp-His-D-Phe-Arg-Trpβ-Ala-Lys)-NH 2 ;
SEQ ID NO: 1
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-A6c-Lys)-NH 2 ;
SEQ ID NO: 2
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-NH 2 ;
SEQ ID NO: 3
D-Phe-c(Cys-His-D-Phe-Arg-Trp-Ala-D-Cys)-Thr-NH 2 ;
SEQ ID NO: 3
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-NH 2 ;
SEQ ID NO: 3
D-Phe-c(Cys-His-D-Phe-Arg-Trp-Gaba-D-Cys)-Thr-NH 2 ;
SEQ ID NO: 2
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-NH 2 ;
SEQ ID NO: 4
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Apn-Lys)-NH 2 ;
SEQ ID NO: 5
Ac-A6c-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 6
Ac-D-2-Nal-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 6
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 6
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 7
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 7
Ac-Nle-c(Cys-β-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 7
Ac-Nle-c(Cys-Gaba-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 7
Ac-Nle-c(Cys-Aib-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 7
Ac-Nle-c(Cys-Gly-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 8
Ac-Nle-c(D-Cys-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 8
Ac-Nle-c(D-Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 8
Ac-Nle-c(D-Cys-β-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 8
Ac-Nle-c(D-Cys-Gaba-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 8
Ac-Nle-c(D-Cys-Aib-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 8
Ac-Nle-c(D-Cys-Gly-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 9
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 9
Ac-Nle-c(Cys-β-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 9
Ac-Nle-c(Cys-Gaba-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 9
Ac-Nle-c(Cys-Aib-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 9
Ac-Nle-c(Cys-Gly-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 10
Ac-Nle-c(D-Cys-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 10
Ac-Nle-c(D-Cys-D-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 10
Ac-Nle-c(D-Cys-β-Ala-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 10
Ac-Nle-c(D-Cys-Gaba-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 10
Ac-Nle-c(D-Cys-Aib-His-D-Phe-Arg-Trp-D-Cys)-NH 2 ;
SEQ ID NO: 11
Ac-Oic-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-D-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-Nip-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-hPro-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-hLeu-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-Phe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-D-Phe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 12
n-butanoyl-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-β-hMet-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 11
Ac-Gaba-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 13
Ac-Cha-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;
SEQ ID NO: 13
Ac-hCha-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;
SEQ ID NO: 13
Ac-Leu-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;
SEQ ID NO: 13
Ac-hLeu-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;
SEQ ID NO: 13
Ac-Phe-c(Asp-His-D-Phe-Arg-D-Trp-Ala-Lys)-NH 2 ;
SEQ ID NO: 14
Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-D-Ala-Lys)-NH 2 ;
SEQ ID NO: 14
Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-β-Ala-Lys)-NH 2 ;
SEQ ID NO: 14
Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 14
Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-Aha-Lys)-NH 2 ;
SEQ ID NO: 14
Ac-Nle-c(Asp-His-D-Phe-Arg-D-Trp-Apn-Lys)-NH 2 ;
SEQ ID NO: 15
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-NH 2 ;
SEQ ID NO: 15
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 15
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-NH 2 ;
SEQ ID NO: 15
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-NH 2 ;
SEQ ID NO: 15
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-D-Ala-Cys)-NH 2 ;
SEQ ID NO: 16
Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 16
Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-2-Nal-Cys)-NH 2 ;
SEQ ID NO: 16
Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-1-Nal-Cys)-NH 2 ;
SEQ ID NO: 17
n-butanoyl-Nle-c(Cys-D-Ala-His-D-Phe-Arg-2-Nal-Cys)-NH 2 ;
SEQ ID NO: 17
n-butanoyl-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 18
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-2-Nal-Cys)-NH 2 ;
SEQ ID NO: 18
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-1-Nal-Cys)-NH 2 ;
SEQ ID NO: 18
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Bal-Cys)-NH 2 ;
SEQ ID NO: 59
Ac-Nle-c(Cys-D-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 19
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-D-Ala-Lys)-NH 2 ;
SEQ ID NO: 20
Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-Bal-Cys)-NH 2 ;
SEQ ID NO: 21
Ac-Nle-c(Pen-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 22
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;
SEQ ID NO: 22
Ac-Nle-c(Pen-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;
SEQ ID NO: 23
D-Phe-c(Cys-His-D-Phe-hArg-Trp-β-Ala-D-Cys)-Thr-NH 2 ;
SEQ ID NO: 24
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Thr-NH 2 ;
SEQ ID NO: 25
D-Phe-c(Cys-His-D-Phe-Arg-Bip-β-Ala-D-Cys)-Thr-NH 2 ;
SEQ ID NO: 24
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-NH 2 ;
SEQ ID NO: 26
D-Phe-c(Cys-His-D-Phe-hArg-Bip-β-Ala-D-Cys)-Thr-NH 2 ;
SEQ ID NO: 26
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-NH 2 ;
SEQ ID NO: 27
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-NH 2 ;
SEQ ID NO: 28
Ac-Nle-c(Asp-D-Ala-His-D-Phe-Arg-Trp-Lys)-NH 2 ;
SEQ ID NO: 28
Ac-Nle-c(Asp-D-Ala-His-D-Phe-Arg-Bal-Lys)-NH 2 ;
SEQ ID NO: 29
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-OH;
SEQ ID NO: 30
Ac-Nle-c(Cys-D-Abu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 30
Ac-Nle-c(Cys-D-Val-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 30
Ac-Nle-c(Cys-D-Ile-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 30
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 30
Ac-Nle-c(Cys-D-Tle-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 30
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 31
Ac-Nle-c(Pen-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 32
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Pen)-NH 2 ;
SEQ ID NO: 32
Ac-Nle-c(Pen-His-D-Phe-Arg-Trp-Gaba-Pen)-NH 2 ;
SEQ ID NO: 33
Ac-Leu-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 33
Ac-Cha-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 33
Ac-Ile-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 33
Ac-Phe-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 33
Ac-Val-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 33
Ac-2-Nal-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 34
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 34
Phe-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 35
Ac-Nle-c(Cys-3-Pal-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 36
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-OH;
SEQ ID NO: 37
Ac-Nle-c(Cys-His-Phe-Arg-D-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 38
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Ala-Lys)-NH 2 ;
SEQ ID NO: 38
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-β-Ala-Lys)-NH 2 ;
SEQ ID NO: 39
Ac-Nle-c(Cys-His-D-2-Nal-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 39
Ac-Nle-c(Cys-His-D-2-Nal-Arg-Trp-Ahx-Cys)-NH 2 ;
SEQ ID NO: 40
Ac-hPhe-c(Asp-His-D-2-Nal-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 40
Ac-Cha-c(Asp-His-D-2-Nal-Arg-Trp-Gaba-Lys)-NH 2 ;
SEQ ID NO: 41
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-OH;
SEQ ID NO: 42
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-OH;
SEQ ID NO: 43
D-Phe-c(Cys-His-D-Phe-Arg-Trp-Ala-D-Cys)-Thr-OH;
SEQ ID NO: 43
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-OH;
SEQ ID NO: 43
D-Phe-c(Cys-His-D-Phe-Arg-Trp-Gaba-D-Cys)-Thr-OH;
SEQ ID NO: 42
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-OH;
SEQ ID NO: 41
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Apn-Lys)-OH;
SEQ ID NO: 44
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;
SEQ ID NO: 44
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;
SEQ ID NO: 44
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;
SEQ ID NO: 44
Ac-D-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;
SEQ ID NO: 44
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;
SEQ ID NO: 44
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;
SEQ ID NO: 44
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-OH;
SEQ ID NO: 45
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Gaba-Cys)-OH;
SEQ ID NO: 45
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-OH;
SEQ ID NO: 45
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-OH;
SEQ ID NO: 45
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-D-Ala-Cys)-OH;
SEQ ID NO: 46
Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-OH;
SEQ ID NO: 46
Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-2-Nal-Cys)-OH;
SEQ ID NO: 46
Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-1-Nal-Cys)-OH;
SEQ ID NO: 46
Ac-Nle-c(Cys-D-Ala-His-D-2-Nal-Arg-Bal-Cys)-OH;
SEQ ID NO: 47
Ac-Nle-c(Pen-D-Ala-His-D-Phe-Arg-Trp-Cys)-OH;
SEQ ID NO: 48
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Pen)-OH;
SEQ ID NO: 49
Ac-Arg-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 50
Ac-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 50
Ac-D-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
SEQ ID NO: 51
Ac-D-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;
SEQ ID NO: 52
Ac-D-Arg-c(Cys-His-D-Phe-Arg-Trp-Gaba-Pen)-NH 2 ;
SEQ ID NO: 52
Ac-Arg-c(Cys-His-D-Phe-Arg-Trp-Gaba-Pen)-NH 2 ;
SEQ ID NO: 51
Ac-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;
SEQ ID NO: 53
Ac-D-Arg-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-NH 2 ;
SEQ ID NO: 53
Ac-Arg-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-NH 2 ;
SEQ ID NO: 35
Ac-Nle-c(Cys-3-Pal-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 54
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-NH 2 ;
SEQ ID NO: 54
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-D-Ala-Cys)-NH 2 ;
SEQ ID NO: 54
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-β-Ala-Cys)-NH 2 ;
SEQ ID NO: 54
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gaba-Cys)-NH 2 ;
SEQ ID NO: 54
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Apn-Cys)-NH 2 ;
SEQ ID NO: 55
Ac-c(Cys-Glu-His-D-Phe-Arg-Trp-Ala-Cys)-NH 2 ;
SEQ ID NO: 55
Ac-c(Cys-Glu-His-D-Phe-Arg-2-Nal-Ala-Cys)-NH 2 ;
SEQ ID NO: 56
Ac-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Ala-Cys)-NH 2 ;
SEQ ID NO: 56
Ac-c(Cys-D-Ala-His-D-Phe-Arg-2-Nal-Ala-Cys)-NH 2 ;
SEQ ID NO: 57
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Ala-Cys)-NH 2 ;
SEQ ID NO: 57
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-β-Ala-Cys)-NH 2 ;
SEQ ID NO: 58
Ac-Nle-c(Asp-D-Ala-His-D-Phe-Arg-Bal-Ala-Lys)-NH 2 ;
(SEQ ID NO: 60)
Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH 2 ;
(SEQ ID NO: 61)
Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -Doc-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH 2 ;
(SEQ ID NO: 62)
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 62)
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-β-Ala-Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 63)
Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc) 2 -Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 64)
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro) 2 -Lys-Asp-Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 65)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro) 2 -Lys-Asp-Tyr-Gly-Arg-(Lys) 2 -
(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 66)
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(β-Ala) 2 -Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 67)
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Pro) 2 -Lys-Asp-Doc-Tyr-Gly-Arg-(Lys) 2 -
(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 68)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys)-(Pro) 2 -Lys-Asp-Doc-Tyr-Gly-Arg-
(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 69)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 69)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-Doc-Tyr-Gly-Arg-
(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 70)
Ac-Nle-c(Asp-His-D-2-Nal-Arg-Trp-Lys)-(Doc) 2 -Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 71)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 72)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 73)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 74)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 75)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
(Lys) 2 -Arg-Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 76)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
(Lys) 2 -Gln-(Arg) 5 -NH 2 ;
(SEQ ID NO: 77)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
Lys-Gln-Lys-(Arg) 5 -NH 2 ;
(SEQ ID NO: 78)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
(Lys) 2 -(Arg) 4 -Gln-Arg-NH 2 ;
(SEQ ID NO: 79)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Aib-Arg-
(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 80)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 80)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 81)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 6 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 82)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 82)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 81)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 6 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 83)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 6 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 84)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 83)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 6 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 85)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
(Lys) 2 -(Arg) 3 -Gln-(Arg) 2 -NH 2 ;
(SEQ ID NO: 86)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
Gln-(Lys) 2 -(Arg) 5 -NH 2 ;
(SEQ ID NO: 87)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
(Lys) 2 -(Arg) 5 -Gln-NH 2 ;
(SEQ ID NO: 71)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 71)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
(Lys) 2 -(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 88)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 2 -Lys-
(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 89)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Arg-Lys-
(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 88)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 2 -Lys-
(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 90)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 2 -
Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 91)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-(Arg) 2 -Lys-
(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 92)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-Arg-Lys-
(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 95)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 2 -
Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 96)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 97)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-(Arg) 2 -Lys-
(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 92)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-Arg-Lys-
(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 98)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 2 -Lys-
(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 99)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Arg-Lys-
(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 101)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-
Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 104)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 2 -Lys-
(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 105)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Arg-Lys-(Arg) 3 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 100)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 2 -
Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 101)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-Arg-Lys-
(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 102)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-(Arg) 2 -Lys-
(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 103)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Gly-Arg-Lys-
(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 113)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 113)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 114)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 114)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 115)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 115)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 116)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 116)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 118)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 118)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 119)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 6 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 120)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 120)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-
(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 121)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 121)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-
(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 122)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 6 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 122)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-
(Arg) 6 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 124)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 6 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 125)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 125)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 126)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 126)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-
(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 127)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 6 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 127)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-
(Arg) 6 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 128)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 128)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-
(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 130)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 130)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 133)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 134)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 134)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-(Arg) 5 -
Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 135)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-β-Ala-Tyr-Gly-(Arg) 6 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 135)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Arg-Asp-β-Ala-Tyr-Gly-(Arg) 6 -
Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 136)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 137)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-(Lys) 2 -Arg-Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 136)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-Arg-(Lys) 2 -(Arg) 2 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 138)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 138)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 139)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 140)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 141)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 2 -Lys-(Arg) 2 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 142)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-Arg-Lys-(Arg) 3 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 141)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-(Arg) 2 -Lys-(Arg) 2 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 142)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Gly-Arg-Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 143)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 2 -Lys-(Arg) 2 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 144)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Arg-Lys-(Arg) 3 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 148)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 148)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 149)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2; ;
(SEQ ID NO: 149)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 151)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 150)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 150)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 151)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 152)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 152)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 154)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 153)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 154)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 155)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 155)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 157)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 156)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 156)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 157)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 158)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 158)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 159)
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 160)
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 161)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 162)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Ala-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 164)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 163)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 163)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 164)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 165)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 165)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 166)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 166)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 168)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 167)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 167)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 168)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 170)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 169)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 169)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 170)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 - Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 171)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 171)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 173)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 172)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 172)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 173)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 174)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 174)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Lys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 175)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 176)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-β-Ala-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 177)
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 178)
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Ahx-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 179)
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 180)
D-Phe-c(Cys-His-D-Phe-Arg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 181)
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 182)
Ac-Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 183)
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 184)
Ac-Cha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 183)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 185)
Ac-Nle-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 186)
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 185)
Ac-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 186)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 188)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 187)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 188)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 189)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 190)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 189)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 190)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 191)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 192)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 191)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 192)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 193)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 194)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 193)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 194)
Ac-hCha-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 195)
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 196)
Ac-D-Chg-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 197)
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 198)
Ac-hPhe-c(Asp-His-D-Phe-Arg-Trp-Gaba-Lys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 199)
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 200)
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Apn-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 199)
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 200)
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-Ahx-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 201)
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 202)
Ac-Nle-c(Cys-His-D-Phe-Arg-D-Trp-β-Ala-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 203)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 203)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 205)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 204)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 204)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 205)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 207)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 206)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 206)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 207)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 208)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 208)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 209)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 210)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 209)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 211)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 212)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 213)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 213)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 267)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 214)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 216)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 214)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 217)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 215)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 216)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 215)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc) 2 -Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 217)
D-Phe-c(Cys-His-D-(Et)Tyr-Arg-Trp-β-Ala-D-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 218)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 219)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 218)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 219)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 221)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 220)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 221)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 222)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 223)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 222)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 223)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 224)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 225)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 224)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 225)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Trp-β-Ala-D-Cys)-Thr-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 227)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 226)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-Tyr-Gly-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 228)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 227)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 228)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 229)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 230)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-Tyr-Gly-(Arg) 5 -Gln-
(Arg) 4 -NH 2 ;
(SEQ ID NO: 232)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 231)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-
(Arg) 3 -NH 2 ;
(SEQ ID NO: 232)
D-Phe-c(Cys-His-D-(Et)Tyr-hArg-Bip-β-Ala-D-Cys)-Thr-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 233)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 234)
Ac-Nle-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Gly-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 235)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 236)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 235)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 236)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 237)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 238)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 237)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 238)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 239)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 240)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 239)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 240)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 241)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 242)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 241)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 242)
Nle-c(Cys-His-D-Phe-Arg-Trp-Apn-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 243)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 244)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 243)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 244)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 245)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 246)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 245)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 246)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 247)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 248)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 247)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 248)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 249)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 250)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 249)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 250)
Ac-Nle-c(Cys-D-Leu-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 251)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 252)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 251)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 252)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 253)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 254)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 253)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 254)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 255)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 256)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 255)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 256)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 257)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 258)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 257)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 258)
Ac-Nle-c(Cys-D-Cha-His-D-Phe-Arg-Trp-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 259)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 260)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 259)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 260)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 261)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 262)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-β-Ala-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 261)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 262)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(β-Ala) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 263)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 264)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 263)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 264)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 3 -NH 2 ;
(SEQ ID NO: 265)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 266)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-Doc-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 265)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc) 2 -Tyr-Gly-(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 266)
Nle-c(Cys-His-D-Phe-Arg-Trp-Gaba-Cys)-(Doc) 2 -(Arg) 5 -Gln-(Arg) 4 -NH 2 ;
(SEQ ID NO: 268)
Ac-c(Cys-Glu-His-D-4-Br-Phe-Arg-Trp-Gly-Cys)-(Pro) 2 -Lys-Asp-NH 2;
(SEQ ID NO: 269)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;
(SEQ ID NO: 269)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;
(SEQ ID NO: 269)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-1-Nal-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;
(SEQ ID NO: 210)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-Bal-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;
(SEQ ID NO: 270)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-β-Ala-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;
(SEQ ID NO: 270)
Ac-c(Cys-Glu-His-D-2-Nal-Arg-2-Nal-Aib-Cys)-(Pro) 2 -Lys-Asp-NH 2 ;
(SEQ ID NO: 271)
c[Hydantoin(C(O)-(Cys-D-Ala))-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 271)
c[Hydantoin(C(O)-(hCys-D-Ala))-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 272)
c[Hydantoin(C(O)-(Cys-D-Ala))-His-D-2-Nal-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 272)
c[Hydantoin(C(O)-(hCys-D-Ala))-His-D-2-Nal-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 273)
c[Hydantoin(C(O)-(Asp-D-Ala))-His-D-Phe-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 273)
c[Hydantoin(C(O)-(Asp-D-Ala))-His-D-Phe-Arg-Trp-Orn]-NH 2 ;
(SEQ ID NO: 273)
c[Hydantoin(C(O)-(Asp-D-Ala))-His-D-Phe-Arg-Trp-Dab]-NH 2 ;
(SEQ ID NO: 273)
c[Hydantoin(C(O)-(Asp-D-Ala))-His-D-Phe-Arg-Trp-Dap]-NH 2 ;
(SEQ ID NO: 275)
c[Hydantoin(C(O)-(Asp-His))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 274)
c[Hydantoin(C(O)-(Asp-His))-D-Phe-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 274)
c[Hydantoin(C(O)-(Asp-A3c))-D-Phe-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 274)
c[Hydantoin(C(O)-(Asp-A5c))-D-Phe-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 274)
c[Hydantoin(C(O)-(Asp-A6c))-D-Phe-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 275)
c[Hydantoin(C(O)-(Asp-A3c))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 275)
c[Hydantoin(C(O)-(Asp-A5c))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 275)
c[Hydantoin(C(O)-(Asp-A6c))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 275)
c[Hydantoin(C(O)-(Asp-A5c))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 274)
c[Hydantoin(C(O)-(Asp-Aic))-D-Phe-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 274)
c[Hydantoin(C(O)-(Asp-Apc))-D-Phe-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 275)
c[Hydantoin(C(O)-(Asp-Aic))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 275)
c[Hydantoin(C(O)-(Asp-Apc))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 275)
c[Hydantoin-(C(O)-(Asp-Aic))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 275)
c[Hydantoin-(C(O)-(Asp-Apc))-D-2-Nal-Arg-Trp-Lys]-NH 2 ;
(SEQ ID NO: 276)
c[Hydantoin(C(O)-(Glu-D-Ala))-His-D-Phe-Arg-Trp-Orn]-NH 2 ;
(SEQ ID NO: 276)
c[Hydantoin(C(O)-(Glu-D-Ala))-His-D-Phe-Arg-Trp-Dab]-NH 2 ;
(SEQ ID NO: 276)
c[Hydantoin(C(O)-(Glu-D-Ala))-His-D-Phe-Arg-Trp-Dap]-NH 2 ;
(SEQ ID NO: 277)
c[Hydantoin(C(O)-(Glu-His))-D-Phe-Arg-Trp-Dap]-NH 2 ;
(SEQ ID NO: 278)
Hydantoin(C(O)-(Arg-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 278)
Hydantoin(C(O)-(Nle-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 278)
Hydantoin(C(O)-(Gly-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(Nle-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(Gly-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 280)
Hydantoin(C(O)-(Nle-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;
(SEQ ID NO: 280)
Hydantoin(C(O)-(Gly-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Pen)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(Ala-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(D-Ala-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(Aib-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(Val-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(Ile-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(Leu-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 281)
Hydantoin(C(O)-(Gly-Gly))-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 281)
Hydantoin(C(O)-(Nle-Gly))-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 278)
Hydantoin(C(O)-(D-Arg-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(D-Arg-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 279)
Hydantoin(C(O)-(Arg-Gly))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 282)
Hydantoin(C(O)-(D-Arg-Gly))-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 282)
Hydantoin(C(O)-(Arg-Gly))-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 283)
Hydantoin(C(O)-(Ala-Nle))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 283)
Hydantoin(C(O)-(Val-Nle))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 283)
Hydantoin(C(O)-(Gly-Nle))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 284)
Hydantoin(C(O)-(A6c-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 284)
Hydantoin(C(O)-(Gly-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 284)
Hydantoin(C(O)-(Ala-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 284)
Hydantoin(C(O)-(D-Ala-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 284)
Hydantoin(C(O)-(Val-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 284)
Hydantoin(C(O)-(Leu-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 284)
Hydantoin(C(O)-(Cha-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 284)
Hydantoin(C(O)-(Aib-Nle))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 285)
Hydantoin(C(O)-(Gly-Arg))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 285)
Hydantoin(C(O)-(Gly-Arg))-c(Cys-Glu-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 286)
Hydantoin(C(O)-(Gly-Arg))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 286)
Hydantoin(C(O)-(Gly-Arg))-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 287)
Hydantoin(C(O)-(Gly-D-Arg))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 288)
Hydantoin(C(O)-(Gly-D-Arg))-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 288)
Hydantoin(C(O)-(Gly-D-Arg))-c(Cys-D-Ala-His-D-2-Nal-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 289)
Hydantoin(C(O)-(Nle-Ala))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Ala-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ,
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Nle-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(D-Ala-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Aib-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Val-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Abu-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Leu-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Ile-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Cha-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(A6c-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Phe-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 290)
c[Hydantoin(C(O)-(Gly-Cys))-D-Ala-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 291)
c[Hydantoin(C(O)-(Gly-Cys))-Glu-His-D-Phe-Arg-Trp-Cys]-NH 2 ;
(SEQ ID NO: 292)
Ac-Tyr-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 292)
Ac-2-Nal-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 292)
Ac-1-Nal-Arg-c(Cys-D-Ala-His-DPhe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 292)
Ac-Phe-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 292)
Ac-Trp-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 292)
Ac-Pff-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 293)
H-His-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
(SEQ ID NO: 292)
Ac-His-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 ;
or a pharmaceutically acceptable salt thereof.
3 . The method according to claim 2 , wherein said compound is Ac-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 (SEQ ID NO:50) or a pharmaceutically acceptable salt thereof.
4 . The method according to claim 2 , wherein said compound is Hydantoin(C(O)-(Arg-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 (SEQ ID NO:278) or a pharmaceutically acceptable salt thereof.
5 . The method according to any one of claims 1 - 4 , wherein said subject is obese.
6 . The method according to any one of claims 1 - 4 wherein said subject is overweight.
7 . The method according to any one of claims 1 - 4 , wherein said subject is normal weight.
8 . The method according to any one of claims 1 - 4 , wherein said subject is lean.
9 . The method according to claim 5 , wherein said obese subject suffers from type II diabetes.
10 . The method according to claim 6 , wherein said overweight subject suffers from type II diabetes.
11 . The method according to claim 7 , wherein said normal weight subject suffers from type II diabetes.
12 . The method according to claim 8 , wherein said lean subject suffers from type II diabetes.
13 . The method according to claim 1 , wherein said peripheral administration is oral, subcutaneous, intraperitoneal, intramuscular, intravenous, rectal, transdermal or intranasal.
14 . The method according to claim 13 , wherein said administration is continuous, hourly, four times daily, three time daily, twice daily, once daily, once every other day, twice weekly, once weekly, once every two weeks, once a month, or once every two months.
15 . The method according to claim 14 , wherein said administration is continuous.
16 . The method according to claim 14 , wherein said administration is once daily.
17 . The method according to claim 14 , wherein said administration is once weekly
18 . The method according to claim 14 , wherein said administration is once every two weeks.
19 . The method according to claim 14 , wherein said administration is once a month.
20 . The method according to claim 14 , wherein said administration is once every two months.
21 . The method according to any one of claims 1 - 4 , wherein said peripheral administration of an effective amount of a melanocortin receptor 4 agonist to treat said insulin resistance in a subject need thereof also reduces the body weight of said subject in need thereof.
22 . The method according to claim 21 , wherein said compound is Ac-Arg-c(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 (SEQ ID NO:50) or a pharmaceutically acceptable salt thereof.
23 . The method according to claim 21 , wherein said compound is Hydantoin(C(O)-(Arg-Gly))-c(Cys-Glu-His-D-Phe-Arg-Trp-Cys)-NH 2 (SEQ ID NO:278) or a pharmaceutically acceptable salt thereof.
24 . The method according to any one of claims 21 - 23 , wherein said subject is obese.
25 . The method according to any one of claims 21 - 23 , wherein said subject is overweight.
26 . The method according to claim 24 , wherein said obese subject suffers from type II diabetes.
27 . The method according to claim 25 , wherein said overweight subject suffers from type II diabetes.
28 . The method according to claim 21 , wherein said peripheral administration is oral, subcutaneous, intraperitoneal, intramuscular, intravenous, rectal, transdermal or intranasal.
29 . The method according to claim 28 , wherein said administration is continuous, hourly, four times daily, three time daily, twice daily, once daily, once every other day, twice weekly, once weekly, once every two weeks, once a month, or once every two months.
30 . The method according to claim 29 , wherein said administration is continuous.
31 . The method according to claim 29 , wherein said administration is once daily.
32 . The method according to claim 29 , wherein said administration is once weekly
33 . The method according to claim 29 , wherein said administration is once every two weeks.
34 . The method according to claim 29 , wherein said administration is once a month.
35 . The method according to claim 29 , wherein said administration is once every two months.Cited by (0)
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