Hashimoto T, Hamada C, Wada T, Fukuda N
Research and Development Division, Takeda Chemical Industries Ltd., Osaka, Japan.
Neuropsychobiology. 1992;26(1-2):89-99. doi: 10.1159/000118901.
Behavioral and EEG effects of 2-(7-chloro-1,8-naphthyridin-2-yl)-3-[(1,4)-dioxa-8-(azas piro-[4.5]dec-8- yl)carbonylmethyl]isoindolin-1-one (DN-2327; 1, 5 and 20 mg/kg p.o.) were compared to those of diazepam (0.2 and 1 mg/kg p.o.) and buspirone (1 and 5 mg/kg p.o.) in freely moving cats. DN-2327 did not affect motor coordination or the relative percentages of the three sleep-wakefulness stages. Diazepam (1 mg/kg) increased wakefulness and non-REM sleep, and buspirone (5 mg/kg) also increased wakefulness and decreased REM sleep. In addition, diazepam (1 mg/kg) caused severe motor disturbance, but buspirone did not. The cortical EEG power density spectra during wakefulness were changed almost dose-dependently by DN-2327 (decreased: 2-7.75 Hz; increased: 20-49.75 Hz), and dose-dependently by diazepam (decreased: 2-7.75 Hz; increased 13-49.75 Hz) and buspirone (decreased: 4-9.75 and 13-19.75 Hz). The effect of DN-2327 on the cortical EEG varied with the sleep-wakefulness stage. The power of the 4- to 7.75-Hz frequency (theta) band of the hippocampal EEG during wakefulness was decreased by diazepam and buspirone but not by DN-2327, while the peak frequency of its spectra was decreased only by diazepam. On the other hand, during non-REM sleep, DN-2327 decreased the power of the theta band as did diazepam. These results indicate that the behavioral and EEG effects of DN-2327 differ completely from those of buspirone and considerably from those of diazepam and that the EEG effect of DN-2327 varies with the sleep-wakefulness stage.
在自由活动的猫身上,比较了2-(7-氯-1,8-萘啶-2-基)-3-[(1,4)-二氧杂-8-(氮杂螺[4.5]癸-8-基)羰基甲基]异吲哚啉-1-酮(DN-2327;1、5和20毫克/千克,口服)与地西泮(0.2和1毫克/千克,口服)和丁螺环酮(1和5毫克/千克,口服)的行为和脑电图效应。DN-2327不影响运动协调性或三个睡眠-觉醒阶段的相对百分比。地西泮(1毫克/千克)增加觉醒和非快速眼动睡眠,丁螺环酮(5毫克/千克)也增加觉醒并减少快速眼动睡眠。此外,地西泮(1毫克/千克)引起严重的运动障碍,但丁螺环酮没有。清醒时,DN-2327几乎呈剂量依赖性地改变皮层脑电图功率密度谱(降低:2-7.75赫兹;增加:20-49.75赫兹),地西泮呈剂量依赖性(降低:2-7.75赫兹;增加13-49.75赫兹),丁螺环酮也呈剂量依赖性(降低:4-9.75和13-19.75赫兹)。DN-2327对皮层脑电图的影响随睡眠-觉醒阶段而变化。清醒时,地西泮和丁螺环酮可降低海马脑电图4至7.75赫兹(θ)频段的功率,但DN-2327不会,而其频谱的峰值频率仅地西泮会降低。另一方面,在非快速眼动睡眠期间,DN-2327与地西泮一样降低了θ频段的功率。这些结果表明,DN-2327的行为和脑电图效应与丁螺环酮完全不同,与地西泮也有很大差异,并且DN-2327的脑电图效应随睡眠-觉醒阶段而变化。