| abstract |
There A peptide selected from the group having the formulae: α) X-R?1-R2-R3-R4-R5-R6-Thr-R8-R9-R10-R11-R12¿-Val-Leu-R15-Gln-Leu-Ser-R?19-R20-R21¿-Leu-Leu-Gln-Asp-Ile-R?27-R28-R29¿, wherein X is H, Ac, Aqc, IAc, BrProp, For, Ibu, Nac, 2-Nac, 1- or 2-Npt, 1- or 2-Npr, PhAc, Fpr, or any other aromatic or nonpolar acyl group, R1 is Tyr, His or Phe(Y), in which Y=H, F, Cl, Br, NO¿2?, NH2, CH3 or OCH3, R?2¿ is D-Arg, D-Cit, D-Har, D-Lys,D-Tic or D-Orn, R3 is Asp, D-Asp, Ala, D-Ala or Gly, R4 is Ala, Abu or Gly, R5 is Ile, Ala or Gly, R6 is Phe, Tic, Ala, Pro, Tpi, Nal or Phe(Y), in which Y=H, F, Cl, Br, NO¿2?, NH2, CH3 or OCH3, R?8¿ is Asn, Gln, Ser, Thr, Val, Leu, Ile, Ala, D-Ala, D-Asn, D-Gln, D-Thr, D-Leu, Abu, D-Abu, Nle, or Aib, R9 is Ser, R10 is Tyr or Phe(Y), in which Y=H, F, Cl, Br, NO¿2?, CH3 or OCH3, R?11¿ is Arg, D-Arg, or Cit, R12 is Lys, D-Lys, Cit, D-Cit, Orn, D-Orn, Nle or Ala, R15 is Gly, Ala, Abu or Gln, R19 is Ala or Abu, R20 is Arg, D-Arg or Cit, R21 is Lys, D-Lys, Orn or Cit, R27 is Met, Nle or Abu, R28 is Ser, Asn, Asp, Ala or Abu, R29 is Agm, Arg-NH¿2?, Arg-OH, Cit-NH2, Cit-OH, Har-NH2 or Har-OH, and β) X-A?1-B2-A3-R4-R5-R6-Thr-A8-Ser-R10-R11-B12¿-Val-Leu-R?15-A16-A17-Ser-R19-B20-B21¿-Leu-Leu-Gln-A?25-Ile-R27-R28-B29¿, wherein a lactam bridge is formed between any one of the pairs of positions 1,2; 2,3; 8,12; 16,20; 17-21; 21,25; 25,29 or both 8,12 and 21,25 positions, and X is H, Ac, Aqc, IAc, BrProp, For, Ibu, Nac, 2-Nac, 1- or 2-Npt, 1- or 2-Npr, PhAc, Fpr, or any other aromatic or nonpolar acyl group, A is Glu, D-Glu, Gln, Asp, D-Asp, Asn, Abu, Leu, Tyr, His, Phe(Y), in which Y=H, F, Cl, Br, NO¿2?, NH2, CH3 or OCH3, Ser, Thr, Val, Ile, Ala, D-Ala, D-Asn, D-Gln, D-Thr, D-Leu, Abu, D-Abu, Nle, or Aib, B is Lys, D-Lys, Arg, D-Arg, Orn, D-Orn, or Agm; R?4¿ is Ala, Abu or Gly, R5 is Ile, Ala or Gly, R6 is Phe, Tic, Tpi, Nal or Phe(Y), in which Y=H, F, Cl, Br, NO¿2?, NH2, CH3 or OCH3, R?10¿ is Tyr or Phe(Y), in which Y=H, F, Cl, Br, NO¿2?, NH2, CH3 or OCH3, R?15¿ is Gly, Ala, Abu or Gln, R27 is Met, Nle or Abu, R28 is Ser, Asn, Asp, Ala or Abu, and pharmaceutically acceptable salts thereof. |