Effect of one derivative of 2-aminotetralin on the alpha-adrenergic receptors of isolated vessels.
Experiments were made to test the effects of originally synthesized piperazine derivative of 2-aminotetralin (P11) on the alpha-adrenergic receptors of isolated vessels. Inhibition of the contracting effects of exogenously introduced noradrenaline into isolated rabbit ear artery was found at concentrations of P11 and phentolamine 1 X 10(-8) to 1 X 10(-4) M. IC50 for P11 is 0.68 microM, for phentolamine -- 0,40 microM. There is a certain shift to the right of the concentration effect curves for noradrenaline in isolated strip of rabbit aorta when P11 and phentolamine are applied in concentrations of 1 X 10(-7) to 1 X 10(-5) M. pA2 for P11 is 7.31, for phentolamine -- 8.04. Potentiation of the maximum effect of noradrenaline is observed after P11 1 X 10(-5) M, which decreases upon preliminary administration of cocaine 1 X 10(-5) M and propranolol 1 X 10(-6) M. The tested compound manifests alpha-adrenergic blocking action in the organs studied.
D000818:Animals; D001011:Aorta / Q000294:innervation*; D001158:Arteries / Q000294:innervation; D001696:Biomechanical Phenomena; D003042:Cocaine / Q000494:pharmacology; D004423:Ear / Q000098:blood supply*; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D009281:Naphthalenes / Q000494:pharmacology*; D009638:Norepinephrine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D010646:Phentolamine / Q000494:pharmacology; D011433:Propranolol / Q000494:pharmacology; D011817:Rabbits; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects*; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*
D009281:Naphthalenes; D011942:Receptors, Adrenergic, alpha; D013764:Tetrahydronaphthalenes; C006561:2-aminotetralin; D011433:Propranolol; D003042:Cocaine; D009638:Norepinephrine; D010646:Phentolamine