Blocking effect of tricyclopinate on nicotinic receptors in cultured sympathetic neurons  

三环哌酯对培养交感神经元烟碱受体的阻断作用<英文>

作　　者：郑建全[1] 何湘平[1] 杨爱珍 刘传缋[1] 

机构地区：[1]北京毒物药物研究所

出　　处：《Acta Pharmacologica Sinica》2000年第11期58-62,共5页中国药理学报（英文版）

基　　金：Project supported by the National Natural Science Foundation of China, No39770850.

摘　　要：AIM: To investigate the mechanism of tricyclopinate, an antagonist of nicotinic receptor, on neuronal nicotinic acetylcholine receptors (nAChR). METHODS: A tight seal whole-cell recording patch-clamp technique was performed to record nicotine-evoked currents in the cultured sympathetic neurons from neonatal rat superior cervical ganglia (SCG). RESULTS: Tricyclopinate inhibited the nicotine-induced currents competitively and the inhibition was voltage-independent. The decay of the nicotine-induced current was accelerated significantly in the presence of tricyclopinate. CONCLUSION: Tricyclopinate inhibits neuronal nAChR by interacting with the allosteric sites rather than the open ionic channels or acetylcholine recognition site of the receptor.目的:观察烟碱受体拮抗剂三环哌酯对烟碱诱发电流的作用.方法:用高阻抗封接膜片箝全细胞记录技术在培养的新生大鼠颈上神经节观察三环哌酯对烟碱诱发电流的作用.结果:三环哌酯竞争性地抑制烟碱诱发电流,其抑制作用没有电压依赖性,但能加速烟碱受体失敏.结论:三环哌酯抑制神经元烟碱受体的作用部位在变构位点而不是在离子通道或乙酰胆碱识别位点.

关 键 词：GANGLIA patch-clamp techniques nicotinic receptors nicotinic antagonists 

分 类 号：R96[医药卫生—药理学]