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首页> 外文期刊>Expert opinion on therapeutic targets >Targeting α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate receptors in epilepsy
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Targeting α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate receptors in epilepsy

机译：靶向癫痫中的α-氨基-3-羟基-5-甲基-4-异恶唑-丙酸酯受体

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Introduction: Despite epilepsies being between the oldest and most studied neurological diseases, new treatment remains an unmet need of scientific research due to the high percentage of refractory patients. Several studies have identified new suitable anti-seizure targets. Glutamate activation of α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate receptors (AMPARs) have long ago been identified as suitable targets for the development of anti seizure drugs. Areas covered: Here, we describe: i) AMPARs' structure and their involvement and role during seizures and in epilepsy and ii) the efficacy of AMPAR antagonists in preclinical models of seizures and epilepsy. Expert opinion: The physiological and pathological role of AMPAR in the CNS and the development of AMPAR antagonists have recently gained attention considering their recent involvement in status epilepticus and the marketing of perampanel. The need for new anti-seizure drugs represents a major challenge in both preclinical and clinical epilepsy. The introduction into the market of perampanel for the treatment of epilepsy will shed new light on the real potential of AMPAR antagonism in clinical settings outside the limited world of clinical trials. While research will go on in this area, fundamental will be the post-marketing evaluation of perampanel efficacy and tolerability and a better definition of the role of this receptor in the epileptic brain.
机译：简介：尽管癫痫介于最古老和研究最多的神经系统疾病之间，但由于难治性患者的比例很高，因此新疗法仍然是科学研究未满足的需求。一些研究已经确定了新的合适的抗癫痫发作靶标。长期以来，谷氨酸激活α-氨基-3-羟基-5-甲基-4-异恶唑-丙酸酯受体（AMPARs）已被确定为开发抗癫痫药物的合适靶标。涵盖的领域：在这里，我们描述：i）AMPAR的结构及其在癫痫发作和癫痫中的作用和作用，以及ii）AMPAR拮抗剂在癫痫和癫痫的临床前模型中的功效。专家意见：考虑到AMPAR在最近的癫痫持续状态和perampanel的销售，它们在中枢神经系统中的生理和病理作用以及AMPAR拮抗剂的开发最近受到关注。对新的抗癫痫药物的需求代表了临床前和临床癫痫中的主要挑战。 Perampanel用于治疗癫痫病的市场将为AMPAR拮抗作用在有限的临床试验领域以外的临床环境中的真正潜力提供新的启示。尽管将在该领域进行研究，但基本的将是上市后对perampanel功效和耐受性的评估，以及对该受体在癫痫脑中作用的更好定义。

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