| 摘要 |
A GnRH antagonist peptide, having the formula X-R1R2-R3-SerR5-R6-R7- Arg-Pro-R10, is prepared. In the formula, X is hydrogen, acrylyl or acetyl; R1 is beta-(2-naphthyl)D-Ala, dehydroPro or 4Cl-D-Phe; R2 is 4Cl-D-Phe, 4F-D-Phe or C alphaMe-4Cl-D-Phe; R3 is D-Trp or beta-(2- naphthyl)D-Ala; R5 is Arg or D-Arg; R6 is D-Try, beta-(2-naphthyl)D- Ala or D-Arg; R7 is Leu or N-alpha-methyl-Leu; and R10 is Gly-NH2, NHCH2CH3, D-Ala-NH2, Gly-OCH3, Gly-OCH2CH3, Gly-NHNH2 or Sar-NH2. The peptide is useful as inhibitors of gonadotropin and steroid for contraceptive use.
|
