Zakusov V V, Voronina T A, Garibova T L, Pálosi E, Sporni L
Farmakol Toksikol. 1983 Nov-Dec;46(6):5-9.
A new daytime tranquilizer uxepam--1-methyl-4-carbamoyl-5-phenyl-7-chloro-1,3,4,5-tetrahydro-2H-1, 4-benzodiazepine-2-on (RGH-3331) administered to animals removes emotional-behavioral abnormalities under conflict situation, reduces aggressiveness induced by electric and painful stimulation, prevents convulsions induced by corasole and electric shock, prolongs the hypnotic effect of hexenal. When applied in high doses the drug suppresses the avoidance reflex, orienting-research behavior and motor activity, disturbs movement coordination. Within wide dosage range uxepam potentiates the summation activity in the central nervous system. As regards anxiolytic activity, the drug does not yield to diazepam and compares very favourably with chlordiazepoxide. The sedative and myorelaxant effects displayed by uxepam are insignificant. The data obtained make it possible to attribute uxepam to daytime tranquilizers.
一种新型日间镇静剂乌西泮——1-甲基-4-氨基甲酰基-5-苯基-7-氯-1,3,4,5-四氢-2H-1,4-苯二氮䓬-2-酮(RGH-3331),给动物服用后可消除冲突情境下的情绪行为异常,减轻电刺激和疼痛刺激诱发的攻击性,预防可拉佐和电击诱发的惊厥,延长己烯醛的催眠作用。高剂量应用时,该药物会抑制回避反射、定向探究行为和运动活动,扰乱运动协调。在宽剂量范围内,乌西泮可增强中枢神经系统的总和活动。就抗焦虑活性而言,该药物不逊色于地西泮,与氯氮䓬相比非常有利。乌西泮表现出的镇静和肌松作用不明显。所获得的数据使我们有可能将乌西泮归类为日间镇静剂。