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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。

相似文献

1
[Oxidation of phenazepam in isolated hepatocytes from white rats].[苯二氮䓬类药物在大白鼠离体肝细胞中的氧化作用]
Vopr Med Khim. 1983 May-Jun;29(3):49-53.
2
[Catalytic properties of the monooxygenases that oxidize 14C-phenazepam].
Vopr Med Khim. 1980 Sep-Oct;26(5):637-40.
3
[Hydroxylation of the aromatic nuclei and heterocyclic ring of the fenazepam molecule in the endoplasmic reticulum of white rats and mice].
Biull Eksp Biol Med. 1980 Jun;89(6):700-2.
4
[Spectral changes in the liver microsomal cytochrome P-450 of rats during interaction with phenazepam and its 3-hydroxy metabolite].[大鼠肝脏微粒体细胞色素P-450与非那西泮及其3-羟基代谢物相互作用过程中的光谱变化]
Biull Eksp Biol Med. 1984 Aug;98(8):196-8.
5
[Mechanisms of the phenazepam oxidation reactions in cell membranes].
Farmakol Toksikol. 1984 May-Jun;47(3):97-101.
6
[2-14C-phenazepam metabolism in vitro].[2-¹⁴C-非那西泮的体外代谢]
Farmakol Toksikol. 1979 Nov-Dec;42(6):597-600.
7
[Metabolic pathways of 3H-5-bromo-2'-chloro-2-aminobenzophenone in the body of rats and mice (a model of the aromatic hydroxylation of phenazepam)].[3H-5-溴-2'-氯-2-氨基二苯甲酮在大鼠和小鼠体内的代谢途径(非那西泮芳香羟基化模型)]
Izv Akad Nauk SSSR Biol. 1983 Sep-Oct(5):770-7.
8
[Distribution of 14C-phenazepam and its metabolites in the liver, brain and blood plasma in single and prolonged administration to white rats].[14C-非那西泮及其代谢产物在对白鼠单次和长期给药后的肝脏、大脑和血浆中的分布]
Farmakol Toksikol. 1980 Mar-Apr;43(2):144-8.
9
[The role of changes in the antioxidative activity and phospholipid composition of the rat liver in the mechanism of phenazepam action on the liver and the protective effect of talamonal].
Vopr Med Khim. 1985 May-Jun;31(3):17-21.
10
[Biotransformation of the 14C-hydrogenated analog of phenazepam in inbred mice].
Biull Eksp Biol Med. 1987 May;103(5):581-3.