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大鼠体内R-(-)-和S-(+)-普尼拉明的对映体选择性分布

Enantioselective disposition of R-(-)- and S-(+)-prenylamine in the rat.

作者信息

Gietl Y, Spahn H, Mutschler E

机构信息

Department of Pharmacology, Johann Wolfgang Goethe-University, Frankfurt/Main, Fed. Rep. of Germany.

出版信息

Arzneimittelforschung. 1989 Aug;39(8):853-6.

PMID:2818674
Abstract

The disposition of R- and S-prenylamine was investigated in male Wistar rats after i.v. and p.o. dosage of 2 mg/kg racemic prenylamine. Concentrations of the enantiomers were determined in plasma, lung, heart, spleen, liver kidney and muscle tissue within a period of 5 h after dosage. In addition, plasma protein binding was assayed in vitro with racemic drug and found to be similar for the two enantiomers. Except for plasma samples after i.v. administration the concentrations of the S-enantiomer exceeded those of the R-enantiomer.

摘要

在雄性Wistar大鼠静脉注射和口服2mg/kg消旋普尼拉明后,对R-和S-普尼拉明的处置情况进行了研究。给药后5小时内测定了血浆、肺、心脏、脾脏、肝脏、肾脏和肌肉组织中对映体的浓度。此外,用消旋药物在体外测定了血浆蛋白结合率,发现两种对映体相似。除静脉注射后的血浆样本外,S-对映体的浓度超过了R-对映体的浓度。

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