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大鼠肝微粒体对匹那西泮的代谢

Metabolism of pinazepam by rat liver microsomes.

作者信息

Marcucci F, Airoldi L, Zavattini G, Mussini E

出版信息

Eur J Drug Metab Pharmacokinet. 1981;6(2):109-14. doi: 10.1007/BF03189476.

Abstract

The pathways by which pinazepam and diazepam are metabolized by rat microsomes in vitro were studied in detail. Using a gas chromatographic technique to measure either the two parent compounds or their metabolites, it was demonstrated that pinazepam and diazepam were metabolized through the same pathways, but at different rates. Pinazepam was mainly N-dealkylated, while the C3-hydroxylation was a minor metabolic pathway. Diazepam was mostly C3-hydroxylated, with very little being N-demethylated. The different rats for the two metabolic pathways could be of importance in differentiating the action of the two drugs in vivo.

摘要

详细研究了匹那西泮和地西泮在体外被大鼠微粒体代谢的途径。使用气相色谱技术测量两种母体化合物或其代谢产物,结果表明匹那西泮和地西泮通过相同的途径代谢,但速率不同。匹那西泮主要发生N-脱烷基化,而C3-羟基化是次要的代谢途径。地西泮大多发生C3-羟基化,N-去甲基化的很少。这两种代谢途径的差异可能对区分这两种药物在体内的作用具有重要意义。

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