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芬氟拉明异构体在大鼠体内的动力学

Kinetics of fenfluramine isomers in the rat.

作者信息

Caccia S, Dagnino G, Garattini S, Guiso G, Madonna R, Zanini M G

出版信息

Eur J Drug Metab Pharmacokinet. 1981;6(4):297-301. doi: 10.1007/BF03189529.

Abstract

The kinetics of fenfluramine isomers were studied in the rat following oral doses of racemic fenfluramine. The data, analyzed using an analogue computer, indicate that the d-fenfluramine is metabolised and excreted at a slower rate than the 1-isomer, resulting in higher plasma and brain concentrations. The kinetic parameters of both isomers were dose-dependent. The rates of disappearance decreased as the dose was raised. The increase in brain area under the curves (AUC) was much greater than the increase of the dose. These findings suggested the rat has a limited capacity for disposition of fenfluramine.

摘要

在大鼠口服消旋芬氟拉明后,对芬氟拉明异构体的动力学进行了研究。使用模拟计算机分析的数据表明,右旋芬氟拉明的代谢和排泄速率比左旋异构体慢,导致血浆和脑内浓度更高。两种异构体的动力学参数均呈剂量依赖性。随着剂量增加,消失速率降低。脑内曲线下面积(AUC)的增加远大于剂量的增加。这些发现表明大鼠对芬氟拉明的处置能力有限。

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