摘要 |
<p>INVENTORS: Maurice Manning Wilbur H. Sawyer TITLE: Novel Antagonists of the Antidiuretic and/or Vasopressor Action of Arginine Vasopressin Compounds acting as antagonists of the antidiuretic activity of arginine vasopressin are of the formula wherein X is Tyr-X'; Tyr- is D- or L-; X' is methyl, ethyl, n-propyl, isopropyl or butyl; W is Pro or .DELTA.3-Pro; and Z is L- or D-Arg. Compounds wherein X is D-Tyr(X') and X' is H or X is D-Phe, D-Val, D-Leu, D-Ile, D-Arg, D-nor-valine, D-norleueine, D-cyclohexylalanine, D-.alpha.-aminobutyric acid, D-threonine or D-methionine; W- is Pro and Z- is D- or L-Arg also act as antagonists of the antidiuretic activity of arginine vasopressin. Related compounds in which X' is H, methyl or ethyl; W is Pro and Val- at the 4-position is replaced by Gln- have antivasopressor activity against arginine vasopressin.</p> |