摘要
目的:探讨右奥硝唑中枢抑制效应与脑内γ-氨基丁酸(gamma amino butyric acid,GABA)系统的关系。方法:经不同剂量右/左奥硝唑处理后使用N,N-二甲基二吖啶硝酸盐(1-(Ethoxycarbonylmethyl)-6-methoxyquinolinium bromide,MQAE)荧光探针检测原代培养小鼠皮层神经元氯离子浓度,并通过western blot方法检测GABAA受体亚基的表达。尾静脉注射给予右/左奥硝唑后测定小鼠高架十字迷宫行为。结果:右奥硝唑剂量依赖性激活小鼠皮层神经元的氯离子通道,经右奥硝唑处理后的皮层神经元能增加GABAA受体α1亚基的水平,且右奥硝唑有潜在的抗焦虑活性。结论:右/左奥硝唑中枢作用不同,右奥硝唑较强的中枢抑制作用可能与激活GABA系统有关。
The aim of the study was to investigate the central inhibition effect and mecha-nism of R-ornidazole through the γ-aminobutyric acid （GABA） ergic systems. Methods： The chloride influxwas estimated in primary cultured prefrontal cortical neurons with treatments of R/S-ornidazole or GABA.After treatments of R/S-ornidazole ordiazepam, the GABAAreceptor α1subunits expression in primary cul-tured prefrontal cortical neurons was determined. The anxiolytic effect of R-ornidazole was measured withelevated plus maze test （EPM） in mice. Results： Compared with S-ornidazole, both R-ornidazole and GA-BA increased chloride influx and R-ornidazole significantly increased GABAAreceptor α1subunits expres-sion. In addition, R-ornidazole showed anxiolytic effect in mice in the elevated plus maze test. Conclu-sion： The inhibition mechanism of R-ornidazole on central nervous system in mice may be through themodification of GABA ergic systems.
出处
《药学与临床研究》
2015年第1期9-12,共4页
Pharmaceutical and Clinical Research
基金
国家重大新药创制科技重大专项资助项目(No.2008ZX09101-101)
