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吗啡代谢产物的药理作用
引用本文:黄宇,苏瑞斌.吗啡代谢产物的药理作用[J].军事医学科学院院刊,2004,28(2):177-179.
作者姓名:黄宇  苏瑞斌
作者单位:军事医学科学院毒物药物研究所,北京,100850
摘    要:吗啡主要在肝脏与葡糖苷酸结合并产生两种代谢产物:吗啡-3-葡糖苷酸(M3G)和吗啡-6-葡糖苷酸(M6G)。M6G能结合阿片受体,动物实验显示其镇痛作用比吗啡强,不良反应较轻微。M3G与阿片受体亲和力较低,没有镇痛作用,且动物实验表明M3G能对抗吗啡和M6G的镇痛作用,可能参与吗啡耐受的形成。本文综述了吗啡的代谢过程及其代谢产物的药理作用。

关 键 词:吗啡  代谢物  镇痛
文章编号:1000-5501(2004)02-0177-03

Pharmacological effect of the metabolites of morphine
HUANG Yu,SU Rui-Bin.Pharmacological effect of the metabolites of morphine[J].Bulletin of the Academy of Military Medical Sciences,2004,28(2):177-179.
Authors:HUANG Yu  SU Rui-Bin
Abstract:The two metabolites of morphine, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G), are mainly formed by morphine glucuronidation in the liver. M6G binds to opioid receptors with high affinity and exhibits stronger analgesia than morphine in animal models. Administration of M6G is accompanied by fewer side effects than after morphine administration. M3G displays very low affinity for opioid receptors and has no analgesic activity. Animal studies show that M3G may antagonize the analgesic effect of morphine and M6G, thus M3G may play a role in the development of morphine tolerance.
Keywords:morphine  metabolite  analgesia
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