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Characterisation of furoxancarbonitriles as a new class of vasodilators.

作者信息

Gasco A M, Boschi D, Di Stilo A, Medana C, Gasco A, Martorana P A, Schönafinger K

机构信息

Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Italy.

出版信息

Arzneimittelforschung. 1998 Mar;48(3):212-8.

PMID:9553676
Abstract

The synthesis, structural characterization, NO-donor properties, and in vitro vasodilating activities of a series of furoxancarbonitriles 2, 17-22a, b are reported. Some derivatives (2b, 2a, 18b, 21b, 22b) are more potent vasodilating agents than sodium nitroprusside (SNP), the reference compound, some others display similar potency (17b, 19b, 20b). Log EC50 values fit well on the linear correlation log EC50 versus log C0.1(1 min) (namely the logarithm of the concentration able to release 2.6 mumol l-1 min-1 of NO) found in a previous work. The haemodynamic profile in anaesthetised pigs for some selected derivatives (2a, b, 19a, b) is also presented. These profiles are consistent with that known for another furoxan NO-donor (4-hydroxymethyl-3-furoxancarboxamide, CAS 1609) and suggest similar characteristic of in vivo NO-release.

摘要

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