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地苯妥英、利鲁唑和利多卡因:三种具有不同作用机制的钠通道阻滞剂,均可降低海马癫痫样活动。

Diphenytoin, riluzole and lidocaine: three sodium channel blockers, with different mechanisms of action, decrease hippocampal epileptiform activity.

机构信息

University of Colorado Anschutz Medical Campus, Mailstop 8105, PO Box 6511, Aurora, CO 80045, USA.

出版信息

Neuropharmacology. 2013 Oct;73:48-55. doi: 10.1016/j.neuropharm.2013.04.057. Epub 2013 May 21.

Abstract

Epilepsy is a condition affecting 1-2% of the population, characterized by the presence of spontaneous, recurrent seizures. The most common type of acquired epilepsy is temporal lobe epilepsy (TLE). Up to 30% of patients with TLE are refractory to currently available compounds, and there is an urgent need to identify novel targets for therapy. Here, we utilized the in-vitro CA3 burst preparation to examine alterations in network excitability, characterized by changes in interburst interval. Specifically, we show that bath application of three different sodium channel blockers-diphenytoin, riluzole, and lidocaine-slow spontaneous CA3 bursts. This in turn, decreased the epileptiform activity. These compounds work at different sites on voltage-gated sodium channels, but produce a similar network phenotype of decreased excitability. In the case of diphenytoin and riluzole, the change in network activity (i.e., increased interburst intervals) was persistent following drug washout. Lidocaine application, however, only increased the CA3 interburst interval when it was in the bath solution. Thus, its action was not permanent and resulted in returning CA3 bursting to baseline levels. These data demonstrate that the CA3 burst preparation provides a relatively easy and quick platform for identifying compounds that can decrease network excitability, providing the initial screen for further and more complex in-vivo, freely-behaving animal studies.

摘要

癫痫是一种影响 1-2%人群的疾病,其特征是存在自发性、复发性癫痫发作。最常见的获得性癫痫是颞叶癫痫(TLE)。高达 30%的 TLE 患者对现有化合物具有耐药性,因此迫切需要确定新的治疗靶点。在这里,我们利用体外 CA3 爆发制备来检查网络兴奋性的变化,其特征是爆发间隔的变化。具体来说,我们表明,三种不同的钠离子通道阻滞剂——苯妥英、利鲁唑和利多卡因——可减缓自发 CA3 爆发。这反过来又降低了癫痫样活动。这些化合物在电压门控钠离子通道的不同部位起作用,但产生类似的网络表型,即兴奋性降低。在苯妥英和利鲁唑的情况下,药物洗脱后网络活动的变化(即爆发间隔增加)仍然存在。然而,利多卡因仅在其存在于浴液中时才增加 CA3 爆发间隔。因此,其作用不是永久性的,导致 CA3 爆发恢复到基线水平。这些数据表明,CA3 爆发制备为识别可降低网络兴奋性的化合物提供了一个相对简单和快速的平台,为进一步进行更复杂的、自由行为的体内动物研究提供了初步筛选。

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