Blaschke G, Kley H, Müller W E
Arzneimittelforschung. 1986 Jun;36(6):893-4.
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.
手性苯二氮䓬类药物卡马西泮（1）和氯氮卓（2）分别通过在光学活性吸附剂聚[(S)-N-(1-环己基乙基)-甲基丙烯酰胺]上进行色谱分离以及分步结晶或反复色谱法拆分为对映体。通过将放射性标记的3H-氟硝西泮和3H-丙基-β-咔啉-羧酸盐从其特异性结合位点置换，测定了这两种化合物的异构体和外消旋体的IC50值。(+)-卡马西泮与(-)-对映体相比，亲和力高14倍。相比之下，氯氮卓对映体的受体亲和力仅观察到细微差异。
