Johns T G, Piper D C, James G W
Arch Int Pharmacodyn Ther. 1979 Jul;240(1):53-65.
RU 31158, 6-(orthochlorophenyl)-1, 2-dihydro-2 (N-methylpiperazine-1-yl) methylene-8-nitro-IH, 4H-imidazo [1,2-a] [1,4] benzodiazepin-1-one methanesulphonate, demonstrated potent hypnotic activity compared to diazepam when examined in the mouse and rat. RU 31158 potentiated minimal hypnosis in mice induced by both hexobarbital and chlorprothixene with ED50 values of 2.15 (1.53-3.01) and 0.69 (0.46-1.02) mg/kg p.o. respectively; these compared to values for diazepam of 17.00 (11.25-25.67) and 3.60 (2.25-5.76) mg/kg p.o. RU 31158 also potentiated hexobarbital in the rat with an ED50 value of 1.2 (0.7-2.0) mg/kg p.o. as compared to 32.0 (27.5-38.5) mg/kg p.o. for diazepam. Sleep studies in the rat confirmed the hypnotic properties of RU 31158, and also showed that the duration of action at 8.0 and 16.0 mg/kg p.o. was not longer than 9 hours. RU 31158 also showed potent minor tranquilizer, anxiolytic, and anti-convulsant properties in a series of pharmacological tests.
RU 31158，即6-（邻氯苯基）-1,2-二氢-2-（N-甲基哌嗪-1-基）亚甲基-8-硝基-1H，4H-咪唑并[1,2-a][1,4]苯并二氮杂䓬-1-酮甲磺酸盐，在小鼠和大鼠实验中显示出与地西泮相比更强的催眠活性。RU 31158增强了由己巴比妥和氯普噻吨诱导的小鼠最小催眠作用，口服半数有效量（ED50）分别为2.15（1.53 - 3.01）和0.69（0.46 - 1.02）mg/kg；相比之下，地西泮的口服半数有效量分别为17.00（11.25 - 25.67）和3.60（2.25 - 5.76）mg/kg。RU 31158还增强了大鼠体内己巴比妥的作用，口服半数有效量为1.2（0.7 - 2.0）mg/kg，而地西泮为32.0（27.5 - 38.5）mg/kg。大鼠睡眠研究证实了RU 31158的催眠特性，并且还表明口服剂量为8.0和16.0 mg/kg时，其作用持续时间不超过9小时。在一系列药理试验中，RU 31158还表现出强效的弱安定、抗焦虑和抗惊厥特性。
