| 摘要 |
The invention provides compounds of the formula: …<CHEM>… in which:… X is D-Phe, D-Val, D-Leu, D-Ile, D-Arg, D-norvaline, D-norleucine, D-cyclohexylalanine, D- alpha -amino-butyric acid, D-threonine, D-methionine, D-Tyr(H), D-or-L-Tyr(X<1>) (in th which X<1> is methyl, ethyl, n-propyl, isopropyl or butyl) or Tyr(X<1><1>) in which X<1><1> is H, methyl or ethyl);… Y is Val, when X is other than Tyr (X<1><1>), or Gln, when X is Tyr (X<1><1>);… W is Pro or, when X is Tyr (X<1>), DELTA <3>-Pro; and… Z is D- or L-Arg. …<??>Compounds of the above formula in which X is Tyr (X<1>) are antagonists of the diuretic action of ADH; compounds of the above formula in which X is other than Tyr (H), Tyr (X<1>) or Tyr (X<1><1>) and antagonists of the ADH activity of arginine vasopression; and compounds of the above formula in which X is Tyr (X<1><1>) are antagonists of the vasodepression activity of ADH. The invention also provides pharmaceutical compositions comprising compounds of the above formula in association with a pharmaceutical carrier or diluent. |
