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Abstract：
Voltage-gated sodium channel blockers are one of the vital targets for the management of several central nervous system diseases, including epilepsy, chronic pain, psychiatric disorders, and spasticity. The voltage-gated sodium channels play a key role in controlling cellular excitability. This reduction in excitotoxicity is also applied to improve the symptoms of epileptic conditions. The effectiveness of antiepileptic drugs as sodium channel depends upon the reversible blocking of the spontaneous discharge without blocking its propagation. There are number of antiepileptic drug(s) which are in pipeline to flour the market to conquer abnormal neuronal excitability. They inhibit the seizures through the inhibition of complex voltage- and frequency-dependent ionic currents through sodium channels. Over the past decade, the sodium channel is one of the most explored targets to control or treat the seizure, but there has not been any game-changing discovery yet. Although there are large numbers of drugs approved for the treatment of epilepsy, however they are associated with several acute to chronic side effects. Many research groups have tirelessly worked for better therapeutic medication on this popular target to treat epileptic seizures. The review quotes briefly the developments of the approved examples of sodium channel blockers as anticonvulsant drugs. Medicinal chemists have tried the design and development of some more potent anticonvulsant drugs to minimize the toxicity that are discussed here, and an emphasis is given for their possible mechanism and the structure-activity relationship (SAR).
摘要：
电压门控钠通道阻滞剂是治疗多种中枢神经系统疾病的重要靶点之一。包括癫痫,慢性疼痛,精神疾病,和痉挛。电压门控钠通道在控制细胞兴奋性中起关键作用。这种兴奋性毒性的降低也可用于改善癫痫病症的症状。抗癫痫药作为钠通道的有效性取决于自发放电的可逆阻断而不阻断其传播。有许多抗癫痫药物正在进入市场以征服异常的神经元兴奋性。它们通过抑制通过钠通道的复合电压和频率依赖性离子电流来抑制癫痫发作。在过去的十年里，钠通道是控制或治疗癫痫发作的探索最多的目标之一，但是还没有任何改变游戏规则的发现。虽然有大量的药物被批准用于治疗癫痫，然而，它们与一些急性到慢性副作用有关。许多研究小组已经不知疲倦地致力于更好的治疗药物治疗这一流行的目标，以治疗癫痫发作。该评论简要引用了钠通道阻滞剂作为抗惊厥药物的批准实例的发展。药物化学家已经尝试设计和开发一些更有效的抗惊厥药物，以尽量减少这里讨论的毒性，并重点介绍了它们的可能机制和结构-活动关系(SAR)。
