| 摘要 |
Peptides which inhibit the secretion of gonadotropins by the pituitary gland and inhibit the release of steroids by the gonads. Administration of an effective amount prevents ovulation of female mammalian eggs and/or the release of steroids by the gonads. The peptides have the structure: X-R1-(W)D-Phe-R3-R4-R5-R6-R7-Arg-Pro-R10 wherein X is hydrogen or an acyl group having 7 or less carbon atoms; R1 is dehydro-Pro, D-pGlu, D-Phe, 4Cl-D-Phe, D-Trp, Pro, or beta -D-NAL; W is Cl, F, NO2, C< alpha > Me/4Cl, Cl2 or Br; R3 is D-3PAL, beta -B-NAL or (Y)D-Trp, with Y being H, NO2, NH2, OCH3, F, Cl, Br, CH3, N<in>For or N<in>Ac; R4 is Ser, Orn, AAL or aBu; R5 is Tyr, Arg, (3F)Phe, (2F)Phe, (3I)Tyr, (3CH3)Phe, (2CH3)Phe, (3Cl)Phe or (2Cl)Phe; R4 is a D-isomer of a lipophilic amino acid or is 4-NH2-D-Phe, D-Lys, D-Orn, D-Har, D-His, 4-gua-D-Phe, D-PAL, or D-Arg; R7 is Nle, Leu, NML, Phe, Met, Nva, Tyr, Trp, Cys, PAL or 4F-D-Phe; and R10 is Gly-NH2 D-Ala-NH2 or NH-Y min , with Y min being lower alkyl, cycloalkyl, fluoro lower alkyl or NHCONH-Q, where Q is H or lower alkyl, provided however that when R3 is D-PAL, R5 is Arg and that when R3 is either beta -D-NAL or D-Trp, then R7 is Tyr, PAL, Phe or 4F-D-Phe. |
