Shabanov P D, Lapina I A, Yaitchnikov I K
Act Nerv Super (Praha). 1984 Jun;26(2):97-102.
Four imidazole- and pyrazoledicarboxylic acid derivatives: 1-ethyl-4,5-di-(N-methylcarbamoyl)-imidazole (aethimizol), 1-allyl-4,5-di(N-methylcarbamoyl)-imidazole (allylnorantifein), 1-ethyl-4,5-di-(N-methylcarbamoyl)-pyrazole (IEM-476), and 1-allyl-4,5-di-(N-methylcarbomyol)-pyrazole (IEM-474) were investigated for their ability to abolish in rats the amnesia of passive avoidance response induced by electroconvulsive shock and to alter the infraslow activity and temperature of the brain in rabbits. IEM-476 10 mg/kg did abolish (P less than 0,05) the amnesia in rats, while the other agents did not. The experiments in rabbits with brain indwelling golden electrodes and thermocouples revealed a shift in the amplitude and frequency of multiminute waves of infraslow activity and a decrease in the temperature of hippocampus, hypothalamus and neocortex after aethimizol (1,5 mg/kg) and IEM-476 (3 mg/kg). Allylnorantifein and IEM-474 (both 3 mg/kg) shifted the amplitude and frequency of multiminute waves of infraslow activity in the reticular formation of the mesencephalon, in the medial group of thalamic nuclei, and the neocortex, i. e. the structures of the nonspecific ascending brain system, and failed to affect the brain temperature. The effects of IEM-476 and IEM-474 were shorter in duration, than those of aethimizol and allylnorantifein.
1-乙基-4,5-二（N-甲基氨基甲酰基）咪唑（乙咪唑）、1-烯丙基-4,5-二（N-甲基氨基甲酰基）咪唑（烯丙基去甲安替芬）、1-乙基-4,5-二（N-甲基氨基甲酰基）吡唑（IEM-476）和1-烯丙基-4,5-二（N-甲基氨基甲酰基）吡唑（IEM-474）消除大鼠电惊厥休克诱导的被动回避反应失忆以及改变家兔大脑超慢活动和温度的能力。IEM-476（10毫克/千克）确实消除了（P<0.05）大鼠的失忆，而其他药物则没有。在家兔中使用脑内植入金电极和热电偶的实验显示，乙咪唑（1.5毫克/千克）和IEM-476（3毫克/千克）给药后，超慢活动的多分钟波的幅度和频率发生变化，海马体、下丘脑和新皮层的温度降低。烯丙基去甲安替芬和IEM-474（均为3毫克/千克）改变了中脑网状结构、丘脑内侧核群和新皮层（即非特异性上行脑系统的结构）中超慢活动的多分钟波的幅度和频率，且未影响脑温。IEM-476和IEM-474的作用持续时间比乙咪唑和烯丙基去甲安替芬短。
