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氨力农在动物体内的代谢。

Metabolism of amrinone in animals.

作者信息

Baker J F, Chalecki B W, Benziger D P, O'Melia P E, Clemans S D, Edelson J

出版信息

Drug Metab Dispos. 1982 Mar-Apr;10(2):168-72.

PMID:6124404
Abstract

The biotransformation of 14C-amrinone was studied in rats, dogs, and monkeys by automated gradient high-performance liquid chromatography. The major pathways of metabolism elucidated are: A) glucuronidation at the primary amino nitrogen atom and/or the enolized oxygen atom of the pyridone ring; B) addition of glutathione at the pyridone 2-position and ultimate hydrolysis of this compound to the 2-S-cysteinyl metabolite; C) formation of the primary amino N-acetyl derivative and subsequent oxidation of this to the corresponding N-glycolate. In each species studied, urine was the primary route of elimination and unchanged amrinone was the major urinary excretion product, the other known pathways being: rat, A and C; dog, A and B; monkey, A.

摘要

通过自动梯度高效液相色谱法研究了大鼠、狗和猴子体内14C-氨力农的生物转化。所阐明的主要代谢途径如下:A)在吡啶酮环的伯氨基氮原子和/或烯醇化氧原子处进行葡萄糖醛酸化;B)在吡啶酮2位添加谷胱甘肽,并最终将该化合物水解为2-S-半胱氨酰代谢物;C)形成伯氨基N-乙酰衍生物,并随后将其氧化为相应的N-乙醇酸酯。在所研究的每个物种中,尿液是主要的排泄途径,未变化的氨力农是主要的尿排泄产物,其他已知途径为:大鼠,途径A和C;狗,途径A和B;猴子,途径A。

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引用本文的文献

1
Amrinone. A preliminary review of its pharmacological properties and therapeutic use.氨力农。其药理特性与治疗用途的初步综述。
Drugs. 1983 Dec;26(6):468-502. doi: 10.2165/00003495-198326060-00002.
2
The pharmacokinetics and pharmacodynamics of newer inotropic agents.新型正性肌力药物的药代动力学和药效学。
Clin Pharmacokinet. 1987 Aug;13(2):91-109. doi: 10.2165/00003088-198713020-00002.
3
The relationship between the pharmacokinetics of amrinone in the marmoset and platelet effects.氨力农在狨猴体内的药代动力学与血小板效应之间的关系。
Eur J Drug Metab Pharmacokinet. 1988 Apr-Jun;13(2):129-33. doi: 10.1007/BF03191314.