title: Antihypertensive aminotetralins related to labetalol and medroxalol.
abstract: A series of compounds was prepared in which the 1-methyl-3-phenylpropylamino moieties of the antihypertensive agents labetalol and medroxalol were replaced by 2-aminotetralins. Compounds containing a 6-methoxy and 6,7-methylenedioxy group in the aminotetralin were at least as active as labetalol in lowering the blood pressure of the spontaneously hypertensive rat (SHR). As determined by ligand binding, these compounds were comparable to labetalol as alpha 1-antagonists but were substantially weaker beta 1-antagonists.
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D002540:Cerebral Cortex / Q000378:metabolism; D055598:Chemical Phenomena; D002621:Chemistry; D004983:Ethanolamines / Q000494:pharmacology; D007741:Labetalol / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D009281:Naphthalenes / Q000138:chemical synthesis*; D051381:Rats; D011918:Rats, Inbred SHR; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000959:Antihypertensive Agents; D004983:Ethanolamines; D009281:Naphthalenes; D011942:Receptors, Adrenergic, alpha; D013764:Tetrahydronaphthalenes; C024892:medroxalol; D007741:Labetalol