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  • Title: [Racemation of the benzodiazepines camazepam and ketazolam and receptor binding of enantiomers].
    Author: Blaschke G, Kley H, Müller WE.
    Journal: Arzneimittelforschung; 1986 Jun; 36(6):893-4. PubMed ID: 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.
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