Cheung H, Kamp D, Harris E
Department of Biology, Fisons Pharmaceuticals, Rochester, NY 14623.
Epilepsy Res. 1992 Nov;13(2):107-12. doi: 10.1016/0920-1211(92)90065-2.
Lamotrigine (LTG), 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine, is a novel antiepieptic drug structurally unrelated to the major anticonvulsants in current use. Previous studies of LTG in rodents revealed efficacy in maximal electroshock test, pentylenetetrazol test and kindling models of seizures suggesting potential utility in the treatment of partial and generalized (tonic-clonic) seizures. In the present study, LTG was found to block sustained repetitive firing of sodium-dependent action potentials in mouse spinal cord cultured neurons and inhibit [3H]batrachotoxinin A 20-alpha-benzoate binding in rat brain synaptosomes suggesting a direct interaction with voltage-activated sodium channels.
拉莫三嗪(LTG),即6 -(2,3 - 二氯苯基)-1,2,4 - 三嗪 - 3,5 - 二胺,是一种新型抗癫痫药物,其结构与目前使用的主要抗惊厥药无关。先前对啮齿动物进行的拉莫三嗪研究表明,它在最大电休克试验、戊四氮试验及癫痫点燃模型中均有疗效,提示其在治疗部分性和全身性(强直阵挛性)癫痫发作方面具有潜在效用。在本研究中,发现拉莫三嗪可阻断小鼠脊髓培养神经元中钠依赖性动作电位的持续重复发放,并抑制大鼠脑突触体中[3H]蛙毒素A 20-α-苯甲酸酯的结合,这表明它与电压激活钠通道存在直接相互作用。