PREPARATIVE AND ANALYTICAL SEPARATION OF THE ZOPICLONE ENANTIOMERS AND DETERMINATION OF THEIR AFFINITY TO THE BENZODIAZEPINE RECEPTOR-BINDING SITE

被引：47

作者：

BLASCHKE, G ^{[1
]}

HEMPEL, G ^{[1
]}

MULLER, WE ^{[1
]}

机构：

[1] CENT INST MENTAL HLTH,DEPT PSYCHOPHARMACOL,MANNHEIM,GERMANY

来源：

CHIRALITY | 1993年 / 5卷 / 06期

关键词：

ZOPICLONE; CHIRAL LIQUID CHROMATOGRAPHY; ENANTIOSEPARATION; FRACTIONAL CRYSTALLIZATION; CYCLOPYRROLONE; BENZODIAZEPINE RECEPTOR BINDING;

D O I：

10.1002/chir.530050605

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the preparative separation of rac-zopiclone using malic acid as the resolving agent. Furthermore, two different methods for the analytical determination of zopiclone enantiomers by HPLC on chiral stationary phases are described. The benzodiazepine receptor binding of the isolated enantiomers was investigated. Half-maximal inhibitory concentrations of (+)- and (-)-zopiclone were 21 or 1, 130 nmol/liter, respectively, indicating a more than 50 times higher affinity of the (+)-enantiomer toward the receptor. (C) 1993 Wiley-Liss, Inc.

引用

页码：419 / 421

页数：3

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