Abstract

Compounds acting as antagonists of the antidiuretic activity of arginine vasopressin are those of the formula ##STR1## wherein X is (D- or L-)Tyr(R), D-Tyr, D-Phe, D-Val, D-Leu D-Ile, D-Arg, D-Gln, D-Asn, D-NVa, D-Nle, D-Cha, D-Abu, D-Thr or D-Met; R is methyl, ethyl, propyl or butyl and Z is D- or L-Arg. Also acting as antagonists of the antidiuretic action of arginine vasopressin are compounds of the formula ##STR2## wherein X and Z are as above and n is 4 or 5. Other antagonists of the antidiuretic action of arginine vasopressin are of the formula ##STR3## wherein X and n are as above and Z' is (D- or L-)Orn or (D- or L-)Lys. Other antagonists of the antidiuretic action of arginine vasopressin are of the formula ##STR4## wherein X is above, W is D-Pro, Δ3 -Pro or HO-Pro; Z" is (D- or L-)Arg, (D- or L-)Lys or (D- or L-)Orn and n is 4 or 5; provided that when X is (D- or L-)Tyr(R) and n is 5, W is HO-Pro or D-Pro and that when X is D-Gln or D-Asn and n is 5, W is also Pro.

Document Type

Patent

Primary Class

514/10.9

Secondary Class

514/15.4; 530/329; 530/330; 930/20; 930/21; 930/150

Application Number

06/455866

Filing Date

January 1983

Patent Number

US4491577

Assignee(s)

Medical College of Ohio; The Trustees of Columbia University

Publication Date

1-1-1985

Patent Country

US

Language

en_US

Institution

The University of Toledo

Repository

University of Toledo Libraries

Digital Publisher

Digital Initiatives

Rights

These materials are free of copyright restrictions and are in the public domain within the United States only. The USPTO reserves the right to assert copyright protection internationally.

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Rights Statement

No Copyright - United States. URI: http://rightsstatements.org/vocab/NoC-US/1.0/
The organization that has made the Item available believes that the Item is in the Public Domain under the laws of the United States, but a determination was not made as to its copyright status under the copyright laws of other countries. The Item may not be in the Public Domain under the laws of other countries. Please refer to the organization that has made the Item available for more information.