| 摘要 |
A decapeptide of the formula: N-Ac-A<1>-A<2>-A<3>-Ser-A<4>-A<5>-A<6>-A<7>-A<8>-A<9>, wherein each A<1>, A<2>, and A<3>, independently, is D- beta -Nal, D-p-X-Phe (where X is halogen, H, NH2, NO2, OH, or C1-3 alkyl), D-Trp, D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A<4> is p-X-Phe (where X is halogen, H, NH2, NO2, or C1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A<5> is D-Lys, D-Tyr, D-Arg, D-Phe, D- beta -Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH2, NO2, or C1-3 alkyl), or D-Lys- epsilon -NH-R (where R is H, a branched or straight chain C1-C10 akyl group, or an aryl group); A<6> is Leu, beta -Nal, p-X-Phe (where X is halogen, H, NH2, NO2, OH, C2F5, C1-3 alkyl), or Trp; A<7> is Arg, Lys, or Lys- epsilon -NH-R (where R is H, a branched or straight chain C1-C6 alkyl group, or an aryl group); A<8> is Pro; and A<9> is D-Ala, D-Ala-NH2, Ala-NH2, aminoisobutyric acid amide, or Gly-NH2; provided that at least one of A<2> or A<3> must be D-Phe or D-Tyr, and provided further that when A<4> is Lys or Arg, A<5> must not be D-Arg, D-Lys, D-homo-Arg, D-diethylhomo-Arg, or D-Lys- epsilon -NH-R, or a pharmaceutically acceptable salt thereof, can be used to inhibit the release of sex hormones in the treatment or prophylaxis of various sex hormone-released conditions. They may also be used as female contraceptives.
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