A new beta 2-adrenoceptor agonist with alpha 1-adrenoceptor blocking properties.
The phenylethanolamine D2343 exhibits a dualistic adrenoceptormediated effect, i.e, a beta-agonistic effect combined with an alpha-antagonistic one. Tracheal smooth muscles and heart preparations were used to gauge the agonistic effect of adrenergic beta-receptors. Rabbit aorta and rat vas deferens were used to determine the alpha-adrenoceptor blocking activity. The beta-adrenoceptor activity of D2343 was classified as beta 2-type with about the same efficacy as the beta 2-selective terbutaline on tracheal muscle. The effect on isolated heart preparations was greater than that produced by terbutaline. The alpha-receptor blocking capacity was directed against the alpha 1-receptor type and was of nearly the same potency as for phentolamine.
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000818:Animals; D001011:Aorta / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D009655:Octopamine / Q000031:analogs & derivatives* / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects; D014132:Trachea / Q000187:drug effects; D014649:Vas Deferens / Q000187:drug effects
D000317:Adrenergic alpha-Antagonists; D000318:Adrenergic beta-Agonists; D011942:Receptors, Adrenergic, alpha; D009655:Octopamine; C033651:D 2343