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芬替酸的代谢

Metabolism of fentiazac.

作者信息

Fumero S, Mondino A, Silvestri S, Zanolo G, De Marchi G, Pedrazzini S

出版信息

Arzneimittelforschung. 1980;30(8):1253-6.

PMID:7192138
Abstract

The main metabolite of 2-phenyl-4-p-chlorophenylthiazol-5-ylacetic acid (fentiazac) is represented by a p-hydroxylated compound which is formed rapidly and that, still 72 later, can be detected in the general circulation. The p-hydroxylated metabolite is much less toxic than the original molecule from which it derives, being still active from an anti-inflammatory standpoint (its activity being equal to 70--75% of that of fentiazac). The metabolite, which possesses a therapeutic index much higher than that of fentiazac, represents quite an important step in the detoxication processes of the drug and enhances the therapeutic activity of the drug itself.

摘要

2-苯基-4-对氯苯基噻唑-5-基乙酸(芬替扎ac)的主要代谢产物是一种对羟基化化合物,它形成迅速,并且在72小时后仍可在全身循环中检测到。该对羟基化代谢产物的毒性远低于其衍生的原始分子,从抗炎角度来看仍具有活性(其活性相当于芬替扎ac的70%-75%)。该代谢产物的治疗指数远高于芬替扎ac,在药物解毒过程中是相当重要的一步,并增强了药物本身的治疗活性。

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