Referenced in: none

Automatically associated channels: Kir2.3

Title: [Racemation of the benzodiazepines camazepam and ketazolam and receptor binding of enantiomers].

Authors: G Blaschke, H Kley, W E Müller

Journal, date & volume: Arzneimittelforschung, 1986 Jun , 36, 893-4

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/2874815

Abstract
The chiral benzodiazepines camazepam (1) and ketazolam (2) were resolved into the enantiomers by chromatography on the optically active adsorbent poly[(S)-N-(1-cyclohexylethyl)-methacrylamide] and fractional crystallisation or repeated chromatography, respectively. The IC50 values of the isomers and of the racemates of both compounds were determined by displacement of radioactively labelled 3H-flunitrazepam and 3H-propyl-beta-carboline-carboxylate from their specific binding sites. (+)-Camazepam exhibits 14fold higher affinity compared to the (-)-enantiomer. In contrast only slight differences in the receptor affinity are observed with the ketazolam enantiomers.