Vasomolol: an ultra short-acting and vasodilatory vanilloid type

Details Vasomolol: an ultra short-acting and vasodilatory vanilloid type Vasomolol: an ultra short-acting and vasodilatory vanilloid type

1996-06-21

1999-08-17

Gerstl, Robert

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

502451, C07C21304

Patent

active

059395788

ABSTRACT:
This invention is related to novel vasomolol, compounds of this invention have the following formula wherein R.sub.1 represents C.sub.1-4 alkyl group. ##STR1## vasomolol is an ultra short-acting and vasodilatory selective .beta..sub.1 -adrenoceptor antagonist, and is devoid of ISA.
Vasomolol is an utra short acting and vasodilatory selective .beta..sub.1 -adrenoceptor antagonist, and is devoid of IA. The ultra short-acting and vsodilatory .beta..sub.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.sup.-6 M-10.sup.-5 M) inhibit both henylephrine (10.sup.-6 M) and High K.sup.+ (75 mM)--induced smooth muscle contractions, concentration-dependently. This inhibitory effect of vasomolol was more sensitive on K.sup.+ than on phenylephrine-induced contractions.

REFERENCES:
patent: 3961071 (1976-06-01), Koppe
March, Advanced Organic Chemistry, p. 1196, 1992.

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