A new series of cardioselective adrenergic beta-receptor blocking compounds. 1-(2-Acyl-4-acylaminophenoxy)-3-isopropylaminopropan-2-ols.
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.
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000813:Anilides / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D001145:Arrhythmias, Cardiac / Q000139:chemically induced; D002415:Cats; D004285:Dogs; D006339:Heart Rate / Q000187:drug effects; D007545:Isoproterenol / Q000037:antagonists & inhibitors; D008968:Molecular Conformation; D009928:Organ Specificity; D010042:Ouabain / Q000037:antagonists & inhibitors; D011412:Propanolamines / Q000138:chemical synthesis* / Q000494:pharmacology; D011941:Receptors, Adrenergic / Q000187:drug effects; D013329:Structure-Activity Relationship
D000319:Adrenergic beta-Antagonists; D000813:Anilides; D011412:Propanolamines; D011941:Receptors, Adrenergic; D010042:Ouabain; D007545:Isoproterenol