PMID: 3647Mar 1, 1976

A new series of cardioselective adrenergic beta-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols

Journal of Medicinal Chemistry
B BasilK R Wooldridge

Abstract

A series of 1-(2-acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols has been synthesized and examined for beta-receptor blocking and antiarrhythmic activity. Several of these compounds are more than 20 times as active in blocking cardiac beta-receptors than vascular beta-receptors when given intravenously to anesthetized cats. The activities have been correlated quantitatively with partition and steric substitution constants. The observed relationships are consistent with a tentative proposal that the vascular receptor is situated in a more lipophilic environment than the cardiac receptor so that there is a differential transport effect between the two types of receptor.

Citations

May 7, 1982·European Journal of Pharmacology·B Basil, R Jordan

Related Concepts

Adrenergic beta-Antagonists
Anilides
Cardiac Arrhythmia
Felis catus
Canis familiaris
Pulse Rate
Novodrin
Tissue Specificity
Ouabain
Propanolamines

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