| 摘要 |
This invention is related to novel vasomolol, compounds of this invention have the following formula wherein R1 represents C1-4 alkyl group. vasomolol is an ultra short-acting and vasodilatory selective beta 1-adrenoceptor antagonist, and is devoid of ISA. Vasomolol is an utra short acting and vasodilatory selective beta 1-adrenoceptor antagonist, and is devoid of IA. The ultra short-acting and vsodilatory beta 1-adrenoceptor blocking activities of vasomolol-a guaiacoxypropanolamine derivative of vanillic acid ethyl ester-were studied. Vasomolol (0.5, 1.0, 3.0 mg/kg, I.v.) produced a dose-dependent bradycardia rsponse, and particularly a hypotensive action with an ultra short-acting property in pentobarbital-anesthetized normotensive rats. Vasomolol's steady-state of beta -blockade was attained within 10 min after initiation of an infuson and a rapid recovery from blockade took place after termination of the infusion. In isolated rat aorta, vasomolol (10-6 M-10-5 M) inhibit both henylephrine (10-6 M) and High K+ (75 mM)-induced smooth muscle contractions, concentration-dependently. This inhibitory effect of vasomolol was more sensitive on K+ than on phenylephrine-induced contractions.
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