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苄硝唑对大鼠肝微粒体混合功能氧化酶系统的影响。

Effect of benznidazole on the mixed function oxygenase system from rat liver microsomes.

作者信息

Masana M, de Toranzo E G, Rubio M, Castro J A

出版信息

Arch Int Pharmacodyn Ther. 1985 Jul;276(1):4-11.

PMID:4051638
Abstract

Previous Benznidazole (Bz) administration to rats (30 mg/kg, i.p.) significantly prolongs their pentobarbital sleeping time. This prolonging effect of Bz administration correlates with the inhibitory action of Bz on the liver aminopyrine or ethylmorphine N-demethylase activities. Inhibition of these enzyme systems by Bz is non-competitive and would not be related to changes in liver microsomal cytochrome P-450 (P-450) content or in cytochrome c-reductase activity or to interactions of Bz with P-450 leading to spectral changes. Covalent interactions of Bz reactive metabolites with microsomal proteins or phospholipids might be involved instead.

摘要

先前给大鼠腹腔注射苯硝唑(Bz,30mg/kg)可显著延长其戊巴比妥睡眠时间。Bz给药的这种延长作用与Bz对肝脏氨基比林或N-脱甲基酶活性的抑制作用相关。Bz对这些酶系统的抑制是非竞争性的,且与肝脏微粒体细胞色素P-450(P-450)含量变化、细胞色素c还原酶活性变化或Bz与P-450相互作用导致光谱变化无关。相反,可能涉及Bz活性代谢产物与微粒体蛋白或磷脂的共价相互作用。

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