Epilepsy is a disorder characterized by seizures and convulsions. The basis of epilepsy is an increase in neuronal excitability that, in some cases, may be caused by functional defects in neuronal voltage gated sodium channels (NaVs). The C121W mutation of the β1 subunit, in particular, gives rise to the thermosensitive generalized epilepsy with febrile seizures plus (GEFS+) phenotype. Lacosamide is used to treat epileptic seizures and is distinct from other anti-seizure drugs by targeting NaV slow-inactivation. We studied the effects of a physiologically relevant concentration of lacosamide on the biophysical properties of NaV1.2 channels associated with either WT-β1 or the mutant C121W-β1 subunit. Biophysical parameters were measured at both normal (22°C) and elevated (34°C) temperatures to elicit the differential temperature-sensitivity of C121W. Lacosamide was more effective in NaV1.2 associated with the WT-β1 than with C121W-β1 at either temperature. There is also a more potent effect by lacosamide on slow inactivation at elevated temperatures. Our data suggest a modulatory role is imparted by the β1 subunit in the interaction between the drug and the channel.

译文

癫痫是一种以癫痫发作和抽搐为特征的疾病。癫痫的基础是神经元兴奋性的增加,在某些情况下,可能是由神经元电压门控钠通道 (NaVs) 的功能缺陷引起的。特别是 β1亚基的C121W突变会引起具有高热惊厥加 (GEFS) 表型的热敏性全身性癫痫。Lacosamide用于治疗癫痫发作,并通过靶向NaV慢灭活与其他抗癫痫药物不同。我们研究了生理相关浓度的lacosamide对与WT-β1或突变C121W-β1亚基相关的NaV1.2通道的生物物理特性的影响。在正常 (22 °C) 和高 (34 °C) 温度下均测量了生物物理参数,以引起C121W的不同温度敏感性。在任一温度下,Lacosamide在与WT-β1相关的NaV1.2中比与C121W-β1更有效。lacosamide在高温下对缓慢失活也有更有效的作用。我们的数据表明,β1亚基在药物与通道之间的相互作用中具有调节作用。

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