Hypotensive action of a new benzimidazolinone derivative, threo-1-(2-hydroxy-2-(3,4,5-trimethoxyphenyl)-1-methylethyl)-4-(1,3-dihydro-2H-benzimidazol-2-one-1-yl)piperidine (KF-4942): prazosin-like mode of action.
Among a series of benzimidazolinone derivatives, KF-4942 was examined on its mode of hypotensive action. It was found that KF-4942 was a potent hypotensive agent, and that the hypotension was produced mostly by alpha-adrenergic blockade. Alpha-adrenergic blocking action of KF-4942 was suggested to be selective to the postsynaptic receptor. Thus, KF-4942 was concluded to be an agent with properties similar to prazosin.
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology; D000818:Animals; D000959:Antihypertensive Agents; D001562:Benzimidazoles / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects*; D002339:Carotid Arteries / Q000502:physiology; D004285:Dogs; D005260:Female; D066298:In Vitro Techniques; D007269:Injections, Intra-Arterial; D007275:Injections, Intravenous; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009638:Norepinephrine / Q000494:pharmacology; D010656:Phenylephrine / Q000494:pharmacology; D011187:Posture; D011224:Prazosin / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D012039:Regional Blood Flow / Q000187:drug effects; D014711:Vertebral Artery
D000317:Adrenergic alpha-Antagonists; D000959:Antihypertensive Agents; D001562:Benzimidazoles; D010656:Phenylephrine; C037466:KF 4942; D009638:Norepinephrine; D011224:Prazosin