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哺乳动物的药物代谢。

Mammalian drug metabolism.

作者信息

Nelson S D, Gordon W P

出版信息

J Nat Prod. 1983 Jan;46(1):71-8. doi: 10.1021/np50025a005.

Abstract

Drugs and other chemicals that do not occur in mammalian systems are metabolized by a wide variety of enzymes. Reactions catalyzed by these enzymes have been classified into two general phases. Phase I reactions include oxidations, reductions, and hydrolyses, whereas Phase II reactions are broadly defined as conjugation reactions and include glucuronidation, sulfation, acylation, methylation, and conjugation with glutathione. The mechanisms of these biotransformations are outlined to demonstrate how both non-toxic and toxic metabolites are produced. The mammalian metabolism of acetaminophen, a widely used mild analgesic, and R-(+)-pulegone, the major constituent terpene of pennyroyal oil, will be discussed to illustrate specific features of mammalian drug metabolism.

摘要

在哺乳动物系统中不存在的药物和其他化学物质会被多种酶代谢。这些酶催化的反应大致可分为两个阶段。第一阶段反应包括氧化、还原和水解,而第二阶段反应广义上被定义为结合反应,包括葡萄糖醛酸化、硫酸化、酰化、甲基化以及与谷胱甘肽的结合。概述了这些生物转化的机制,以说明无毒和有毒代谢物是如何产生的。将讨论广泛使用的轻度镇痛药对乙酰氨基酚以及薄荷油主要成分萜烯R-(+)-胡薄荷酮在哺乳动物体内的代谢,以阐明哺乳动物药物代谢的具体特征。

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