Otsuka M, Tsuchiya T, Kitagawa S
Arzneimittelforschung. 1975 May;25(5):755-60.
Effects of ID-540 (1-methyl-5-(o-fluorophenyl)-7-chloro-1,3-dihydro-2H-1,4-benzodiazepin-2-one) on the central nervous system were evaluated electrophysiologically and behaviorally in cats and rabbits. The reference compound used was diazepam. 1. ID-540 as well as diazepam produced muscle relaxation, grooming, facilitation of appetite and suppression of defensive behaviors. ID-540 made the animals lie on their side during sleep, but diazepam did not. 2. Though more effectively inducing an increase in fast activity and a decrease in frequency of hippocampal theta-waves than diazepam, ID-540 scarcely affected the amplitude of subcortical EEG (hippocampus, amygdala and hypothalamus), which diazepam decreased in cats. 3. ID-540 and diazepam increased the waking phase and decreased the paradoxical sleep phase. 4. ID-540 and diazepam at a dose of 1 mg/kg decreased the duration of amygdala after-discharge for 1 h in cats. Diazepam increased the duration of the after-discharge after it had been decreased, but ID-540 did not. ID-540 did not affect the duration of hippocampal after-discharge whereas diazepam prolonged it. 5. ID-540 depressed more effectively the hippocampal arousal response to stimulation of the ventro-medial hypothalamus than did diazepam in rabbits. 6. ID-540 depressed amygdalo-hippocampal evoked potential in cats. 7. ID-540 did not affect norepinephrine-induced pressor response but reduced hypothalamic pressor response in cats.
在猫和兔子身上,通过电生理学和行为学方法评估了ID-540(1-甲基-5-(邻氟苯基)-7-氯-1,3-二氢-2H-1,4-苯并二氮杂卓-2-酮)对中枢神经系统的影响。所用的对照化合物为地西泮。1. ID-540和地西泮均能产生肌肉松弛、梳理毛发、促进食欲以及抑制防御行为的作用。ID-540能使动物在睡眠时侧卧,而地西泮则不能。2. 尽管ID-540比地西泮更有效地诱导海马θ波快速活动增加和频率降低,但ID-540几乎不影响皮层下脑电图(海马、杏仁核和下丘脑)的振幅,而地西泮会使猫的皮层下脑电图振幅降低。3. ID-540和地西泮增加清醒期并减少异相睡眠期。4. 1mg/kg剂量的ID-540和地西泮可使猫杏仁核放电后持续时间缩短1小时。地西泮在放电后持续时间缩短后会使其延长,但ID-540不会。ID-540不影响海马放电后持续时间,而地西泮会使其延长。5. 在兔子身上,ID-540比地西泮更有效地抑制海马对腹内侧下丘脑刺激的唤醒反应。6. ID-540可抑制猫杏仁核-海马诱发电位。7. ID-540不影响去甲肾上腺素诱导的升压反应,但可降低猫下丘脑升压反应。