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大鼠和家兔中苯二氮䓬受体亚型激活后脑电活动的改变

Modifications of brain electrical activity after activation of the benzodiazepine receptor types in rats and rabbits.

作者信息

Longo V G, Massotti M, DeMedici D, Valerio A

机构信息

Laboratorio di Farmacologia, Istituto Superiore di Sanità, Roma, Italy.

出版信息

Pharmacol Biochem Behav. 1988 Apr;29(4):785-90. doi: 10.1016/0091-3057(88)90207-9.

Abstract

The present study reports a comparative electroencephalographic (EEG) study of drugs belonging to different chemical classes which share the property to bind at benzodiazepine (BDZ) recognition sites. The EEG patterns are recorded from the neocortex of rats and rabbits as well as from dorsal hippocampus and red nucleus in rabbits after intravenous administration of diazepam (0.1-10 mg/kg), clonazepam (0.02-2.5 mg/kg), zopiclone (0.3-3 mg/kg), flunitrazepam (0.03-2.5 mg/kg), CGS 9896 (0.1-3 mg/kg), zolpidem (0.1-3 mg/kg) and Cl 218,872 (0.1-10 mg/kg). The most relevant differences are observed at the level of the neocortex. All drugs induced appearance of 7-12 Hz spindle bursts. On the contrary, the presence of 15-30 Hz waves (defined beta-like activity) mainly occurs after diazepam, clonazepam and zopiclone. Scarce beta-like activity is present after CGS 9896, zolpidem and Cl 218,872. According to the selectivity of these drugs for the various types of BDZ receptor, one can speculate that activation of BDZ2 is relevant for the appearance of the beta-like activity. Flunitrazepam, diazepam, and zolpidem increase the amplitude of the red nucleus waves. Such an effect is less marked after zopiclone and CGS 9896, whereas is almost absent after clonazepam and Cl 218,872. A reduction of the frequency is observed after flunitrazepam, diazepam, clonazepam, CGS 9896 and zolpidem, whereas it is almost absent after zopiclone and Cl 218,872. Finally, all drugs induce a reduction of the amplitude of the hippocampal theta rhythms, whereas after diazepam, flunitrazepam, zolpidem and CGS 9896 a slowing of the record also occurs.

摘要

本研究报告了一项针对不同化学类别的药物进行的比较性脑电图(EEG)研究,这些药物具有在苯二氮䓬(BDZ)识别位点结合的特性。在静脉注射地西泮(0.1 - 10 mg/kg)、氯硝西泮(0.02 - 2.5 mg/kg)、佐匹克隆(0.3 - 3 mg/kg)、氟硝西泮(0.03 - 2.5 mg/kg)、CGS 9896(0.1 - 3 mg/kg)、唑吡坦(0.1 - 3 mg/kg)和Cl 218,872(0.1 - 10 mg/kg)后,从大鼠和兔子的新皮质以及兔子的背侧海马体和红核记录EEG模式。在新皮质水平观察到最显著的差异。所有药物均诱导出现7 - 12 Hz的纺锤波爆发。相反,15 - 30 Hz波(定义为类β活动)的出现主要发生在地西泮、氯硝西泮和佐匹克隆给药后。CGS 9896、唑吡坦和Cl 218,872给药后出现的类β活动较少。根据这些药物对各种类型BDZ受体的选择性,可以推测BDZ2的激活与类β活动的出现有关。氟硝西泮、地西泮和唑吡坦会增加红核波的振幅。佐匹克隆和CGS 9896给药后的这种效应不太明显,而氯硝西泮和Cl 218,872给药后几乎没有这种效应。氟硝西泮、地西泮、氯硝西泮、CGS 9896和唑吡坦给药后观察到频率降低,而佐匹克隆和Cl 218,872给药后几乎没有这种情况。最后,所有药物均导致海马体θ节律的振幅降低,而地西泮、氟硝西泮、唑吡坦和CGS 9896给药后记录还会出现减慢。

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