突触前抗癫痫药物--基本机制及其合理组合的线索。

IF 3.6 3区医学 Q2 PHARMACOLOGY & PHARMACY Pharmacological Reports Pub Date : 2024-08-01 Epub Date: 2024-05-22 DOI:10.1007/s43440-024-00603-7

Ewa K Czapińska-Ciepiela, Jarogniew Łuszczki, Piotr Czapiński, Stanisław J Czuczwar, Władysław Lasoń

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引用次数: 0

摘要

在临床高效抗癫痫药物（ASMs）中，有突触前释放机制的调节剂。其中，左乙拉西坦和溴瓦西坦对突触囊泡蛋白 2 A 型（SV2A）具有高亲和力，而普瑞巴林和加巴喷丁则是电压门控钙通道 α2δ1 亚基的选择性配体。在本文中，我们介绍了在理解突触前释放机制在癫痫和 ASM 的神经化学机制中的重要性方面所取得的最新进展。此外，我们还讨论了对突触前作用 ASM 基本机制的了解是否有助于建立针对耐药性癫痫的合理多药疗法。

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Presynaptic antiseizure medications - basic mechanisms and clues for their rational combinations.

Among clinically highly efficient antiseizure medications (ASMs) there are modifiers of the presynaptic release machinery. Of them, levetiracetam and brivaracetam show a high affinity to the synaptic vesicle protein type 2 A (SV2A), whereas pregabalin and gabapentin are selective ligands for the α2δ1 subunits of the voltage-gated calcium channels. In this paper, we present recent progress in understanding the significance of presynaptic release machinery in the neurochemical mechanisms of epilepsy and ASMs. Furthermore, we discuss whether the knowledge of the basic mechanisms of the presynaptically acting ASMs might help establish a rational polytherapy for drug-resistant epilepsy.

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来源期刊

Pharmacological Reports 医学-药学

CiteScore

8.40

自引率

0.00%

发文量

审稿时长

6 months

期刊介绍： Pharmacological Reports publishes articles concerning all aspects of pharmacology, dealing with the action of drugs at a cellular and molecular level, and papers on the relationship between molecular structure and biological activity as well as reports on compounds with well-defined chemical structures. Pharmacological Reports is an open forum to disseminate recent developments in: pharmacology, behavioural brain research, evidence-based complementary biochemical pharmacology, medicinal chemistry and biochemistry, drug discovery, neuro-psychopharmacology and biological psychiatry, neuroscience and neuropharmacology, cellular and molecular neuroscience, molecular biology, cell biology, toxicology. Studies of plant extracts are not suitable for Pharmacological Reports.