Horváth K, Andrási F, Botka P, Hámori T
Institute for Drug Research, Budapest, Hungary.
Acta Physiol Hung. 1992;79(2):153-61.
The anxiolytic action of two 2,3-benzodiazepines: girisopam: GYKI 51,189 (EGIS 5810): (1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5H-2,3-benzodiazepine), and GYKI 52,322 (EGIS 6775): (1-(4-aminophenyl)-4-methyl-7,8-dimethoxy-5H-2,3-benzodiazepine) was investigated in comparison to chlordiazepoxide and buspirone using three different animal models of anxiety: the lick conflict, the elevated plus maze and the open field methods in rats. Both 2,3-benzodiazepines exerted anxiolytic effect in all three tests used, however their pharmacological profile differs considerably from that of either chlordiazepoxide or buspirone. Using the animal models mentioned above the order of potency was GYKI 52,322 (EGIS 6775) > chlordiazepoxide > girisopam > buspirone.
两种2,3-苯二氮䓬类药物(吉立索泮:GYKI 51,189(EGIS 5810):(1-(3-氯苯基)-4-甲基-7,8-二甲氧基-5H-2,3-苯二氮䓬)和GYKI 52,322(EGIS 6775):(1-(4-氨基苯基)-4-甲基-7,8-二甲氧基-5H-2,3-苯二氮䓬))的抗焦虑作用,与氯氮卓和丁螺环酮相比,采用三种不同的大鼠焦虑动物模型进行了研究:舔舐冲突试验、高架十字迷宫试验和旷场试验。两种2,3-苯二氮䓬类药物在所有三种试验中均发挥了抗焦虑作用,然而它们的药理学特征与氯氮卓或丁螺环酮有很大不同。使用上述动物模型,效力顺序为GYKI 52,322(EGIS 6775)>氯氮卓>吉立索泮>丁螺环酮。