Novel antagonists of the antidiuretic and/or vasopressor action of arginine vasopressin

Compounds acting as antagonists of the antidiuretic activity of arginine vasopressin are those of the formula ##STR1## wherein X is methyl, ethyl, n-propyl, isopropyl or butyl; Tyr is D- or L-; W is Pro or ?3 -Pro; and Z is L- or D- Arg. 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. Compounds wherein D-Tyr is unetherified (X is H), W- is Pro and Z- is D- or L-Arg also act as antagonists of the antidiuretic activity of arginine vasopressin.
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Abstract/Description: Compounds acting as antagonists of the antidiuretic activity of arginine vasopressin are those of the formula ##STR1## wherein X is methyl, ethyl, n-propyl, isopropyl or butyl; Tyr is D- or L-; W is Pro or ?3 -Pro; and Z is L- or D- Arg. 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. Compounds wherein D-Tyr is unetherified (X is H), W- is Pro and Z- is D- or L-Arg also act as antagonists of the antidiuretic activity of arginine vasopressin.
Subject(s): 514/10.9
514/15.4
514/21.1
514/21.7
514/807
530/315
930/21
930/150
930/260
Date Issued: 1983-01-04