Antihypertensive 1-acyl-4-[2-(1,4-benzodioxan-2-yl)-2-hydroxyethylamino]pip eridines.
Several 1-acyl-4-[2-(1,4-benzodioxan-2-yl)-2-hydroxy-ethylamino]piperidine s were prepared and a number of the compounds showed antihypertensive activity in the spontaneously hypertensive rat (SHR). This activity was specific for the (2S, 2R) enantiomers. General pharmacological evaluation and ligand binding data on selected compounds indicated a moderate degree of alpha 1- and beta-antagonistic activity. The alpha 1 antagonism was probably not of sufficient magnitude to explain the blood pressure lowering activity in the SHR.
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D011918:Rats, Inbred SHR; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects; D011943:Receptors, Adrenergic, beta / Q000187:drug effects
D000959:Antihypertensive Agents; D010880:Piperidines; D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta