六甲溴铵阻断交感神经元烟碱受体的机理  

Blocking mechanism of hexamethonium bromide on nicotinic acetylcholine receptors in cultured rat superior cervical ganglion neurons

作　　者：郑建全[1] 何湘平[1] 杨爱珍[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：《中国药理学与毒理学杂志》1997年第4期257-259,共3页Chinese Journal of Pharmacology and Toxicology

摘　　要：使用膜片钳全细胞记录技术，观察了六甲溴铵（Ｃ６）对培养新生大鼠颈上交感节（ＳＣＧ）神经元烟碱受体的阻断作用，并对其作用机理进行了研究．本实验发现Ｃ６对神经元烟碱受体的抑制作用具有明显的浓度依赖性和电压依赖性，可明显加速烟碱受体的失敏，提示Ｃ６主要以阻断受体开放离子通道的方式拮抗烟碱受体．The blocking effect of hexamethonium bromide (C 6) on neuronal nicotinic acetylcholine receptors (nAChRs) in cultured rat superior cervical ganglion was studied with the technique of whole cell recording. It was found that: 1) C 6 blocked ganglionic nAChRs with a concentration and voltage dependent manner. As the membrane potential was hyperpolarized from -30 mV to -90 mV, the inhibitory rates induced by 10 μmol·L 1 C 6 on 50 μmol·L 1 DMPP evoked currents were significantly raised from 22±16% to 72±13%. 2) C 6 could accelerate the desensitization of neuronal nAChRs. When the application time was prolonged to 15 s, C 6 not only depressed the amplitudes of DMPP induced current, but also shortened the decay time constants of the currents remarkably. 3) When the mixture of DMPP and C 6 was applied for 6 times continuously with an interval time of 10 s, no significant differences were found among the inhibitory rates induced by 10 μmol·L 1 C 6 every time. The results suggest that C 6 may depress the ganglionic nAChRs by blocking the open channels, as well as accelerating the desensitization of nAChRs.

关 键 词：交甲溴铵 交感神经元 烟碱 电生理学 药理学 

分 类 号：R971[医药卫生—药品]