四乙铵对交感神经元烟碱受体的非竞争性拮抗  

Non competitive blocking effects of tetraethylammonium on nicotinic acetylcholine receptors in sympathetic neurons

作　　者：郑建全[1] 何湘平[1] 刘传缋[1] 

机构地区：[1]军事医学科学院毒物药物研究所

出　　处：《军事医学科学院院刊》1996年第1期1-4,共4页Bulletin of the Academy of Military Medical Sciences

摘　　要：以培养的新生大鼠颈上交感节神经元为标本，探讨了四乙铵（ｔｅｔｒａｅｔｈｙｌａｍｍｏｎｉｕｍ，ＴＥＡ）对神经元烟碱受体的作用机制。结果表明：（１）烟碱激活交感神经元烟碱受体的ＫＤ值为２５．２９μｍｏｌ／Ｌ；（２）１００μｍｏｌ／ＬＴＥＡ对神经元烟碱受体的作用，主要表现为非竞争性拮抗，对不同浓度（１０～１６０μｍｏｌ／Ｌ）烟碱诱发电流的抑制率为３０％～３９％；（３）ＴＥＡ对烟碱受体的阻断作用具有明显的电压依赖性。推测ＴＥＡ对神经元烟碱受体的非竞争性拮抗作用的结合位点。The cultured neurons of rat superior cervical ganglia were used to investigate the blocking effects of tetraethylammonium (TEA) on neuronal nicotinic acetylcholine receptors (nAChRs).The results show that:(1)nicotine can elicit an inward current with a K D value of 25.29 μmol/L;(2)TEA can block neuronal nAChRs in a noncompetitive way and the inhibitory rate of 100 μmol/L TEA to the currents induced by different concentrations of nicotine (10 160 μmol/L) was about 30% 39%;(3)The blocking effect of TEA on neuronal nAChRs is voltagedependent.It is suggested that the binding site of TEA might be located near the outer ring of the channel.

关 键 词：交感神经 神经元 烟碱受体 四乙铵 阻断作用 

分 类 号：R966[医药卫生—药理学]