In vitro studies with (imidazolinyl-2)-2-benzodioxane-1-4 ((+/-)-170 150), a new potent alpha 2-adrenoceptor blocking agent.
In rat vas deferens, (+/-)-170 150 proved to be an alpha 2-adrenoceptor blocking agent with a high alpha 2/alpha 1 selectivity ratio. In rat cerebrocortical membranes, (+/-)-170 150 was seven times more potent than yohimbine for inhibiting specific [3H]clonidine binding. However, (+/-)-170 150 appeared to be 3.5 times less selective for alpha 2-adrenoceptors sites than yohimbine. These results indicate that (+/-)-170 150 is a potent preferential alpha 2-adrenoceptor blocking agent, as had been shown by in vivo experiments.
D000317:Adrenergic alpha-Antagonists / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D003000:Clonidine / Q000378:metabolism; D004147:Dioxins / Q000378:metabolism / Q000494:pharmacology*; D019329:Idazoxan; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D010656:Phenylephrine / Q000494:pharmacology; D011224:Prazosin / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011941:Receptors, Adrenergic / Q000378:metabolism*; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism*; D015016:Yohimbine / Q000494:pharmacology
D000317:Adrenergic alpha-Antagonists; D004147:Dioxins; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; D010656:Phenylephrine; D015016:Yohimbine; D003000:Clonidine; D011224:Prazosin; D019329:Idazoxan