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

Abstract

A series of 1-(2-acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols was 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 i.v. to anesthetized cats. The activities were 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 2 types of receptor.