D_1及α_2受体激动剂对卵母细胞表达的GABA_A受体的抑制  

MODULATION OF SKF38393 AND CLONIDINE ON EXPRESSED GABA_A RECEPTORS IN XENOPUS OOCYTES

作　　者：王钦文 王秀清 王凤 李之望[2] 

机构地区：[1]武汉市儿童疾病研究所,湖北武汉430016 [2]同济医科大学实验医学研究中心,湖北武汉430030

出　　处：《中国应用生理学杂志》2001年第4期333-336,共4页Chinese Journal of Applied Physiology

基　　金：国家自然科学基金资助项目 ( 39970 2 40 )

摘　　要：目的 :研究SKF38393及Clonidine对表达的DRG神经元GABAA 受体的调制作用 ,并与新鲜分离细胞相比较。方法 :实验在注射鼠DRG神经元mRNA的卵母细胞上进行 ,以双电极电压钳技术进行研究。结果 :①SKF38393及Clonidine对表达的DRG神经元GABAA 受体有明显的抑制作用 ,其作用呈浓度依赖性。②SKF38393及Clonidine的诱导电流之间有相互抑制作用。③SKF38393及Clonidine对GABAA 受体的抑制作用是非竞争性抑制 ,并且为非电压依赖性。结论 :实验结果提示SKF38393及Clonidine可通过胞内转导 ,由第二信使介导GABAA 受体的磷酸化而抑制GABAAAim and Methods: The present research is performed on Xenopus oocytes injected with rat DRG mRNA. Modulatory effects of SKF38393 and Clonidine on GABAS A receptors expressed in Xenopus oocytes was investigated by two electrodes voltage clamp technique,and it is compared with the neurons fresh isolated. Results: It is found that SKF38393 and Clonidine inhibitate GABA A receptor function obviously by a concentration dependent manner. There is an interaction between SKF38393 and Clonidine induced currents. The inhibition of SKF38393 and Clonidine on GABA A receptors is noncompetitive and voltage independent. Conclusions: The results suggest that the inhibition by SKF38393 and clonidine of GAB A activated current might be a result of phosphorylation of GABA A receptor following action of second messenger and the thereby mediated intracelluar transduction.

关 键 词：SKF38393 可乐定 卵母细胞 背根神经节 GABAA 受体 膜反应 Α2受体激动剂 抑制 D1受体激动剂 

分 类 号：R338.8[医药卫生—人体生理学]