Vasomolol: an ultra short-acting and vasodilatory vanilloid type .beta..sub. - adrenoceptor antagonist
US5939578A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Jun 21, 1996 |
| Grant date | Aug 17, 1999 |
| Priority date | — |
| Expiry date | Jun 21, 2016 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C213/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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 wa…
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