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PMID: 1672862 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

DuP 753 is a specific antagonist for the angiotensin receptor.

Hypertension (Dallas, Tex. : 1979) ·Vol. 17 ·No. 4 ·1991-04-00 ·Pages 480-4

Rhaleb NE, Rouissi N, Nantel F, D'Orléans-Juste P, Regoli D

Abstract

2-n-Butyl-4-chloro-5-hydroxy-methyl-1-[(2'-(1H)-tetrazol-5-yl)biph enyl-4- yl)methyl]imidazol potassium salt (DuP 753) is a nonpeptide angiotensin II receptor antagonist that inhibits the contractile effects of angiotensin II competitively and shows pA2 values of 8.27 on the rabbit aorta and jugular vein, 8.66 on the rat portal vein and stomach, 8.19 on the rat urinary bladder, and 8.36 on human colon, ileum, and urinary bladder. This agent (more than 10(-5) M) exhibits no agonistic activity and does not affect the contractile effects of norepinephrine, acetylcholine, bradykinin, desArg9-bradykinin, substance P, neurokinin A, neurokinin B, or bombesin in the various tissues. The present results demonstrate that DuP 753 is a potent nonpeptide antagonist with high affinity, specificity, and selectivity for the angiotensin receptor.

MeSH Terms
Adrenergic alpha-Antagonists/antagonists & inhibitors Adult Angiotensin II/antagonists & inhibitors Angiotensin Receptor Antagonists Animals Blood Vessels/drug effects Digestive System/drug effects Humans Imidazoles/antagonists & inhibitors,pharmacology In Vitro Techniques Kinetics Kinins/pharmacology Losartan Male Muscarinic Antagonists Rabbits Rats Rats, Inbred Strains Tetrazoles/antagonists & inhibitors,pharmacology Urinary Bladder/drug effects
Chemicals
Adrenergic alpha-Antagonists Angiotensin Receptor Antagonists Imidazoles Kinins Muscarinic Antagonists Tetrazoles Angiotensin II Losartan
Authors & Affiliations
5 authors, click to expand affiliations / ORCID
Rhaleb N E
Department of Pharmacology, Medical School University of Sherbrooke, Quebec, Canada.
Rouissi N
Nantel F
D'Orléans-Juste P
Regoli D
Article Info
Journal
Hypertension (Dallas, Tex. : 1979)
Abbr.
Hypertension
ISSN
0194-911X
Published
1991-04-00
Pages
480-4
Language
English
Region
United States
NLM ID
7906255
Subset
IM
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