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Preparative and analytical separation of the zopiclone enantiomers and determination of their affinity to the benzodiazepine receptor binding site
Author(s) -
Blaschke Gottfried,
Hempel Georg,
Müller Walter E.
Publication year - 1993
Publication title -
chirality
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.43
H-Index - 77
eISSN - 1520-636X
pISSN - 0899-0042
DOI - 10.1002/chir.530050605
Subject(s) - chemistry , enantiomer , zopiclone , chromatography , benzodiazepine , chiral column chromatography , high performance liquid chromatography , receptor , stereochemistry , pharmacology , hypnotic , biochemistry , medicine
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. © 1993 Wiley‐Liss, Inc.