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[氯美扎酮的行为和脑电图效应]

[Behavioral and electroencephalographic effects of lormetazepam].

作者信息

Ueki S, Watanabe S, Fujiwara M, Yamamoto T, Shibata S, Shibata K, Ohta H, Sakurai Y, Iwasaki K, Liou S Y

出版信息

Nihon Yakurigaku Zasshi. 1985 Aug;86(2):145-63. doi: 10.1254/fpj.86.145.

Abstract

Behavioral and electroencephalographic effects of lormetazepam were investigated in rats, mice and rabbits, in comparison with those of diazepam, nitrazepam and flurazepam. Locomotor activity of mice in an open-field situation was decreased with large doses of lormetazepam and diazepam, while it was increased with nitrazepam and flurazepam. The anticonflict effect of lormetazepam in rats was much more potent than those of diazepam, nitrazepam and flurazepam. In suppressing the muricide of olfactory bulbectomized and raphe lesioned rats, lormetazepam was more potent than diazepam, nitrazepam and flurazepam. Lormetazepam, diazepam and flurazepam prevented both maximal electroshock and pentetrazol convulsions in mice, the effects on the latter being much more potent than those on the former. Lormetazepam was more potent than diazepam and flurazepam in potentiating thiopental-, ether- and ethanol anesthesia, impairing rotarod performance and in muscle relaxant activity. In conscious rabbits with chronically implanted electrodes, lormetazepam induced a drowsy EEG pattern and suppressed the EEG arousal responses not only to auditory stimulation but also to electrical stimulation of the midbrain reticular formation or hypothalamus. Lormetazepam also inhibited afterdischarges induced by electrical stimulation of the hippocampus and amygdala. These results indicate that lormetazepam has pharmacological properties characteristic of benzodiazepines and that the activity is more potent than those of diazepam, nitrazepam and flurazepam.

摘要

与地西泮、硝西泮和氟西泮相比,研究了氯美扎酮对大鼠、小鼠和家兔的行为及脑电图影响。大剂量氯美扎酮和地西泮可降低小鼠在旷场环境中的自发活动,而硝西泮和氟西泮则使其增加。氯美扎酮对大鼠的抗冲突作用比地西泮、硝西泮和氟西泮更强。在抑制嗅球切除和中缝损伤大鼠的杀鼠行为方面,氯美扎酮比地西泮、硝西泮和氟西泮更有效。氯美扎酮、地西泮和氟西泮均可预防小鼠的最大电休克和戊四氮惊厥,对后者的作用比对前者更强。氯美扎酮在增强硫喷妥钠、乙醚和乙醇麻醉作用、损害转棒试验性能及肌肉松弛活性方面比地西泮和氟西泮更有效。在长期植入电极的清醒家兔中,氯美扎酮可诱导出困倦的脑电图模式,并不仅抑制对听觉刺激的脑电图觉醒反应,还抑制对中脑网状结构或下丘脑电刺激的反应。氯美扎酮还可抑制海马和杏仁核电刺激诱导的后放电。这些结果表明,氯美扎酮具有苯二氮䓬类药物的药理学特性,且活性比地西泮、硝西泮和氟西泮更强。

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