2-Benzodioxinylaminoethanols: a new class of beta-adrenergic blocking and antihypertensive agents.
Various 2-benzodioxinylaminoethanol derivatives were synthetized and investigated for beta-adrenergic blocking activity. Most compounds demonstrated a beta-blocking activity of a competitive type when evaluated in guinea pig atrial and tracheal preparations. Three compounds were more potent than practolol and propranolol. All compounds demonstrated antihypertensive properties in spontaneously hypertensive rats. The most active compound was 1-(1,4-benzodioxin-2-yl)-2-[N4-(2-methoxyphenyl)piperazino]ethanol (11), which at 2.5 mg/kg iv lowered blood pressure by 41%.
D000319:Adrenergic beta-Antagonists; D000818:Animals; D000959:Antihypertensive Agents; D004147:Dioxins / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006973:Hypertension / Q000188:drug therapy / Q000235:genetics; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000502:physiology; D009200:Myocardial Contraction / Q000187:drug effects; D051381:Rats; D011922:Rats, Mutant Strains; D014132:Trachea / Q000502:physiology
D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D004147:Dioxins