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[苯二氮䓬类药物在大白鼠离体肝细胞中的氧化作用]

[Oxidation of phenazepam in isolated hepatocytes from white rats].

作者信息

Golovenko N Ia, Meteshkin Iu V, Kuznetsova S V

出版信息

Vopr Med Khim. 1983 May-Jun;29(3):49-53.

PMID:6136125
Abstract

In isolated rat hepatocytes aromatic hydroxylation and oxidation of the 14C-phenazepame heterocycle were studied. Both these reactions proceeded with the linear rate in intact hepatocytes and aromatic hydroxylation predominated. After induction of cytochrome P-450 by phenobarbital the rate of the heterocycle oxidation was increased 3.6-fold. Rates of aromatic hydroxylation and the phenazepame heterocycle oxidation did not depend on administration of phenobarbital and 3-methyl cholanthrene into the animals. Effects of the factors studied (concentration of phenazepame, induction of cytochrome P-450 by means of phenobarbital and 3-methyl cholanthrene) on alterations in the rate of oxidation of both aromatic nuclei and the phenazepame heterocycle were estimated using dispersion analysis.

摘要

在离体大鼠肝细胞中,研究了14C-非那西泮杂环的芳香族羟基化和氧化反应。这两种反应在完整肝细胞中均以线性速率进行,且芳香族羟基化占主导。用苯巴比妥诱导细胞色素P-450后,杂环氧化速率提高了3.6倍。芳香族羟基化和非那西泮杂环氧化速率不依赖于给动物注射苯巴比妥和3-甲基胆蒽。使用方差分析评估了所研究因素(非那西泮浓度、用苯巴比妥和3-甲基胆蒽诱导细胞色素P-450)对芳香核和非那西泮杂环氧化速率变化的影响。

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