生命个体传递神经冲动时扩布的电位变化过程以动作电位发放形式为特质表征.电压门控钠离子通道（voltagegated sodium channels,VGSCs）是形成动作电位的核心蛋白构件，在细胞的电兴奋产生和律动中起主角作用.VGSCs决定神经元细胞的兴奋性以及从突触输入到轴突输出的信号传导过程.VGSCs也是众多外源性天然或人工合成化学产物作用的靶器.大多数临床抗癫药和局麻药、杀虫剂、天然生物神经毒素等均以阻断或调制靶通道对离子的通透性，以及通道的门控动力学性质的方式异化通道结构与功能的平衡，导致临床病理事件的产生或生理机能的缓解与恢复.从内源和外源两个方向略览VGSCs，即赋予生命乐章主音符涵义的生理与病理功能地位及其靶向药理学与毒理学身价.

Action potential is a form of electric signaling responsible for conducting neural firing in organisms. Voltagegated sodium channels (VGSCs) are key molecules contributing to the initiation of action potential, playing an indispensable role in electric excitation and firing neurons. Briefly, the overall excitory activities and signalling input/output process of synaptic transmission in neurons mostly depends on VGSCs. Meanwhile, VGSCs are targets of numerous natural neurotoxns or synthesize compounds. By blocking or modulating the ion permeable selectivity and shifting the structurefunction balance of channel gating, clinical pathology or relief from severe syndromes result. This article gives a general overview of endogenous regulation and exogenous modulation of VGSCs, which may highlight the physiological/pathological status and targetted phamacolgical/toxicological values of VGSCs.