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吗啡和阿片类药物的受体。

Receptors for morphine and opioids.

作者信息

Sánchez E, Tampier L, Mardones J

出版信息

Gen Pharmacol. 1976 Aug;7(2-3):107-10. doi: 10.1016/0306-3623(76)90044-6.

Abstract

Two points concerning enzymatic systems acting on disposal of morphine are discussed, namely the multiplicity of glucuronyltransferase and the effect of nalorphine on N-demethylation of morphine. Evidences of the presence of at least two different glucuronyltransferases in microsomes of rat liver, kidney and intestine are presented. These evidences are given by the different distribution of the glucuronizing activity for morphine and rho-nitrophenol in microsomal preparations of these organs; by the different glucuronidation activity for both substrates induced by phenobarbital and 3-methylcholantrene; and finally by the chromatographic separation of fractions with enzymatic glucuronidating activity only for rho-nitrophenol or only for morphine. Nalorphine in concentrations of 1.3 X 10(-3) M and 1.3 X 10(-4) M inhibited in vitro de-N-demethylation of morphine 1.3 X 10(-3) M by the supernatant of rat liver homogenates, while in concentration of 1.3 X 10(-5) M it enhanced this reaction.

摘要

本文讨论了与吗啡代谢相关的两个酶系统问题,即葡萄糖醛酸转移酶的多样性以及烯丙吗啡对吗啡N - 去甲基化的影响。文中给出了大鼠肝脏、肾脏和肠道微粒体中至少存在两种不同葡萄糖醛酸转移酶的证据。这些证据包括:这些器官微粒体制剂中吗啡和对硝基苯酚葡萄糖醛酸化活性的不同分布;苯巴比妥和3 - 甲基胆蒽诱导的两种底物的不同葡萄糖醛酸化活性;最后是仅对对硝基苯酚或仅对吗啡具有酶促葡萄糖醛酸化活性的组分的色谱分离。浓度为1.3×10(-3) M和1.3×10(-4) M的烯丙吗啡抑制了大鼠肝脏匀浆上清液对1.3×10(-3) M吗啡的体外去N - 去甲基化反应,而浓度为1.3×10(-5) M时则增强了该反应。

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