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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Pharmacokinetic differences of morphine and morphine-glucuronides are reflected in locomotor activity.
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Pharmacokinetic differences of morphine and morphine-glucuronides are reflected in locomotor activity.

机译：吗啡和吗啡-葡糖醛酸苷的药代动力学差异反映在运动活性中。

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The main metabolites of morphine, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G), have been considered to participate in some of the effects of morphine. There is limited knowledge of the pharmacokinetics and dynamics of morphine and the main metabolites in mice, but mice are widely used to study both the analgesic effects and the psychomotor effects of morphine. The present study aimed to explore pharmacokinetic differences between morphine and morphine-glucuronides in mice after different routes of administration, and to investigate how possible differences were reflected in locomotor activity, a measure of psychostimulant properties. Mice were given morphine, M3G or M6G by different routes of administration. Serum concentrations versus time curves, pharmacokinetic parameters and locomotor activity were determined. Intraperitoneal administration of morphine reduced the bioavailability compared to intravenous and subcutaneous administration, but not so for morphine-glucuronides. The two morphine-glucuronides had similar pharmacokinetics, but morphine demonstrated higher volume of distribution and clearance than morphine-glucuronides. The present results demonstrated no locomotor effect of M3G, but a serum concentration effect relationship for morphine and M6G. When serum concentrations and effect changes were followed over time, there was some right hand shifts with respect to locomotor activity, especially during the declining phase of the concentration curve and particularly for M6G.
机译：吗啡的主要代谢物吗啡-3-葡糖醛酸化物（M3G）和吗啡-6-葡糖醛酸化物（M6G）被认为参与了吗啡的某些作用。对吗啡及其主要代谢产物在小鼠体内的药代动力学和动力学知之甚少，但是小鼠被广泛用于研究吗啡的镇痛作用和心理运动作用。本研究旨在探讨不同给药途径后小鼠体内吗啡和吗啡-葡糖醛酸苷之间的药代动力学差异，并探讨运动活动（一种心理刺激特性的量度）如何反映出可能的差异。通过不同的给药途径给予小鼠吗啡，M3G或M6G。测定血清浓度对时间的曲线，药代动力学参数和运动活性。与静脉内和皮下给药相比，吗啡腹膜内给药降低了生物利用度，但吗啡-葡萄糖醛酸苷则没有。两种吗啡-葡糖醛酸苷具有相似的药代动力学，但吗啡比吗啡-葡糖醛酸苷具有更高的分布和清除量。目前的结果表明，没有M3G的运动作用，但是吗啡和M6G的血清浓度影响关系。当跟踪血清浓度和效果随时间的变化时，运动能力会有一些右旋，特别是在浓度曲线下降阶段，尤其是对于M6G。

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