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Preparative and analytical separation of the zopiclone enantiomers and determination of their affinity to the benzodiazepine receptor binding site

✍ Scribed by Dr. Gottfried Blaschke; Georg Hempel; Walter E. Müller

Publisher: John Wiley and Sons
Year: 1993
Tongue: English
Weight: 276 KB
Volume: 5
Category: Article
ISSN: 0899-0042
DOI: 10.1002/chir.530050605

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✦ Synopsis

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 nmolfliter, respectively, indicating a more than 50 times higher affinity of the (+)-enantiomer toward the receptor.

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