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[乙胺碘呋酮及其类似物的化学结构与抗心律失常作用之间的关系]

[The relationship between the chemical structure and the antiarrhythmic action of ethacizine and its analogs].

作者信息

Turilova A I, Berdiaev S Iu, Grishchenko A N, Senova Z P

出版信息

Farmakol Toksikol. 1990 Nov-Dec;53(6):20-1.

PMID:2081560
Abstract

The relationship between the chemical structure and the antiarrhythmic activity of phenothiazine derivatives--ethacizine and its analogues--was estimated quantitatively by the value of the antiarrhythmic effect on aconitine model in conscious rats. The lengthening of the side chain of nitrogen atom in position 10 of phenothiazine cycle by one methylene group as well as the substitution of demethylamine radical for diethylamine one increased the antiarrhythmic activity; the toxicity of the compound being also increased. Ethacizine was found to possess the highest antiarrhythmic activity and the greatest antiarrhythmic index.

摘要

通过对清醒大鼠乌头碱模型的抗心律失常作用值,定量评估了吩噻嗪衍生物——乙胺碘呋酮及其类似物的化学结构与抗心律失常活性之间的关系。吩噻嗪环10位氮原子侧链延长一个亚甲基以及用二乙胺基取代去甲胺基,均可增加抗心律失常活性;同时化合物的毒性也会增加。发现乙胺碘呋酮具有最高的抗心律失常活性和最大的抗心律失常指数。

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