Antagonists of the antidiuretic and/or vasopressor action of...

C - Chemistry – Metallurgy – 07 – K

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530/7.06

C07K 7/16 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1185235

INVENTORS: Maurice Manning Wilbur H. Sawyer TITLE: Novel Antagonists of the Antidiuretic and/or Vasopressor Action of Arginine Vasopressin ABSTRACT Compounds acting as antagonists of the antidiuretic activity of arginine vasopressin are of the formula Image 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 antivaso- pressor activity against arginine vasopressin.

397464

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