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GABA 系统作为新药的靶标。

GABA system as a target for new drugs.

机构信息

Department of Physicochemical Drug Analysis, Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.

出版信息

Curr Med Chem. 2014;21(28):3294-309. doi: 10.2174/0929867321666140601202158.

Abstract

4-Aminobutyric acid is an inhibitory neurotransmitter involved in the control of neuronal activity in the mammalian central nervous system. There is considerable direct and indirect evidence that impaired activity of GABAmediated inhibitory synapses may be an important causative factor in experimental and clinical seizure disorders. This review is focused on the recent development of compounds which can influence GABA neurotransmission by affecting the GABA receptors, the plasma-membrane GABA transporters (GATs) and catabolic enzyme GABA-transaminase (GABAT). These compounds have been primarily investigated in relation to epilepsy, but it has also been found that a decrease in GABA neurotransmission appears to be involved in the aetiology of several neurological disorders such as insomnia, spasticity, neuropathic pain, anxiety and other mental disorders.

摘要

4-氨基丁酸是一种抑制性神经递质,参与哺乳动物中枢神经系统中神经元活动的控制。有相当多的直接和间接证据表明,GABA 介导的抑制性突触活动的损害可能是实验性和临床癫痫发作障碍的一个重要致病因素。这篇综述主要集中在最近开发的一些化合物,这些化合物可以通过影响 GABA 受体、质膜 GABA 转运体(GATs)和代谢酶 GABA-转氨酶(GABAT)来影响 GABA 神经传递。这些化合物主要是在癫痫方面进行了研究,但也发现 GABA 神经传递的减少似乎与几种神经紊乱有关,如失眠、痉挛、神经性疼痛、焦虑和其他精神障碍。

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