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吡唑啉酮衍生物对大鼠的肝毒理学研究。第一部分:氨基比林的研究(作者译)

[Hepatotoxicological studies of pyrazolone derivatives on rats. Part 1: The study of aminophenazone (author's transl)].

作者信息

Bien E, Skorka G, Buntrock P, Neubauer J

出版信息

Pharmazie. 1981;36(7):492-500.

PMID:7280002
Abstract

After oral application of aminophenazone to animals (170 and 340 mg/kg daily, over up to 17 weeks), the authors investigated the effect of this drug on some liver functions and performed also a morphological study. They found that aminophenazone produces an increase of the smooth ER, peripheral fatty degradation and reactive-inflammatory responses of the liver, the intensity of these phenomena being dependent upon the dose and time of application. The increase of the smooth ER is the expression of the inductive effect which persists throughout the whole experimental period and manifests itself by accelerated degradation of hexobarbital, increased N-demethylation, increased ascorbic acid synthesis and increased liver weight. The increase in body weight is reduced in the animals treated. The enzyme activities in the plasma lie within the range observed with control animals; they are no indicator of the slight live changes stated. Reactive metabolites and/or the impairment of other metabolic reactions may be considered to be the cause of the hepatotoxic effect of aminophenazone.

摘要

给动物口服氨基苯乙酮(每日170和340毫克/千克,持续长达17周)后,作者研究了该药物对某些肝功能的影响,并进行了形态学研究。他们发现氨基苯乙酮会导致肝脏滑面内质网增加、外周脂肪降解以及反应性炎症反应,这些现象的强度取决于给药剂量和时间。滑面内质网的增加是诱导作用的表现,这种作用在整个实验期间持续存在,并通过己巴比妥降解加速、N - 去甲基化增加、抗坏血酸合成增加以及肝脏重量增加而体现出来。受试动物的体重增加减少。血浆中的酶活性在对照动物观察到的范围内;它们并非所述轻微肝脏变化的指标。反应性代谢产物和/或其他代谢反应的损害可能被认为是氨基苯乙酮肝毒性作用的原因。

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