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吗啡在小鼠、大鼠、家兔、豚鼠、猫、狗和猴体内向二氢吗啡酮和去甲吗啡的生物转化。

Biotransformation of morphine to dihydromorphinone and normorphine in the mouse, rat, rabbit, guinea pig, cat, dog, and monkey.

作者信息

Yeh S Y, McQuinn R L, Gorodetzky C W

出版信息

Drug Metab Dispos. 1977 Jul-Aug;5(4):335-42.

PMID:70327
Abstract

Biotransformation of morphine to dihydromorphinone and normorphine was studied in several mammalian species. Free and total dihydromophinone, morphine, and normorphine in the urine were determined, as propionyl derivatives, with a gas-chromatographic technique. Dihydromorphinone was detected as a morphine metabolite in the acid-hydrolyzed urine of all species studied except the dog and morphine-dependent man. Normorphine in both free and conjugated forms was detected in the urine of all species studied. The degree of biotransformation of morphine to dihydromorphinone in the guinea pig did not change during chronic administration of morphine sulfate, 25 mg/kg, daily for 28 days. The small amounts of dihydromorphinone and normorphine produced as metabolites make it unlikely that they play any significant role in the modification of the pharmacologic effects of morphine.

摘要

在几种哺乳动物物种中研究了吗啡向二氢吗啡酮和去甲吗啡的生物转化。采用气相色谱技术,将尿液中的游离和总二氢吗啡酮、吗啡及去甲吗啡作为丙酰衍生物进行测定。除狗和吗啡依赖的人外,在所研究的所有物种的酸水解尿液中均检测到二氢吗啡酮作为吗啡代谢物。在所研究的所有物种的尿液中均检测到游离和结合形式的去甲吗啡。在豚鼠中,每日给予25mg/kg硫酸吗啡,持续28天的慢性给药过程中,吗啡向二氢吗啡酮的生物转化程度未发生变化。作为代谢产物产生的少量二氢吗啡酮和去甲吗啡不太可能在吗啡药理作用的改变中发挥任何重要作用。

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