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苯乙酰胺类似物对血清肌酐及抗惊厥活性影响的构效关系

Structure-activity relationships in the effects of phenacemide analogs on serum creatinine and anticonvulsant activity.

作者信息

Richards R K

出版信息

Arch Int Pharmacodyn Ther. 1980 Mar;244(1):107-12.

PMID:7416882
Abstract

The anticonvulsant phenacemide had been shown to produce a marked rise of serum creatinine in humans and experimental animals without significant impairment of renal function. The mechanisms is not yet fully elucidated. A series of aromatic and aliphatic analogs of phenacemide were tested in rabbits under standardized conditions. A number of chemicals-structural requirements for this effect could be recognized within the limited number of compounds available. None of them exceeded the potency of phenacemide. There was no consistent correlation between the effect of serum creatinine and anticonvulsant potency in mice.

摘要

抗惊厥药苯乙酰胺已被证明可使人类和实验动物的血清肌酐显著升高,而肾功能无明显损害。其机制尚未完全阐明。在标准化条件下,对一系列苯乙酰胺的芳香族和脂肪族类似物在兔子身上进行了测试。在有限数量的可用化合物中,可以识别出产生这种效应的一些化学结构要求。它们的效力均未超过苯乙酰胺。在小鼠中,血清肌酐效应与抗惊厥效力之间没有一致的相关性。

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