CARDIOSELECTIVITY OF BETA-ADRENOCEPTOR BLOCKING-AGENTS .1. 1-[(4-HYDROXYPHENETHYL)AMINO]-3-(ARYLOXY)PROPAN-2-OLS

A series of l-[(4-hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols was synthesized together with several 1-[(3, 4-dimethoxyphenethyl)aniino]-3-(aryloxy)propan-2-ols. Their affinity to β1 and β2-adrenoceptors was determined and compared with the affinity of known β-blockers. We were able to confirm the substantial cardioselectivity of l-(3, 4-dimethoxyphenethyl)-3-[(4-substituted aryl)oxy]propan-2-ols when compared to those with a l-(4-hydroxyphenethyl) group. An increase in the size of the 4 substituent of the 3-(aryloxy) moiety to caproamido leads to a substantially higher affinity for the β-adrenoceptor of rat ventricular muscle in the presence of the 3, 4-dimethoxyphenethyl than in the presence of the 4-hydroxyphenethyl or isopropyl group; this combination also gave the highest cardioselectivity. © 1979, American Chemical Society. All rights reserved.