摘要
4-氨基丁酸是一种控制哺乳动物中枢神经系统神经活性的神经递质抑制剂。大量的直接或间接证据表明γ-氨基丁酸介导的抑制性突触活性受损也许是实验中和临床中一些惊厥性疾病的重要病因。该综述集中于通过影响γ-氨基丁酸受体,质膜γ-氨基丁酸转运蛋白(GATs)及分解酶γ-氨基丁酸转氨酶(GABAT)来改变γ-氨基丁酸神经递质的单体化合物的近期发展。初步展开对这些化合物与癫痫症相关的研究,但是我们也发现γ-氨基丁酸神经递质的减少表明其参与一些神经系统疾病的发病病因,如失眠症、痉挛、神经性疼痛、焦虑及其他精神疾病。
关键词: γ-氨基丁酸,GABA摄取抑制剂,GABAA受体配体,GABAB受体配体,GABAC 受体配体,GABA转氨酶抑制剂。
Current Medicinal Chemistry
Title:GABA System as a Target for New Drugs
Volume: 21 Issue: 28
Author(s): P. Kowalczyk and K. Kulig
Affiliation:
关键词: γ-氨基丁酸,GABA摄取抑制剂,GABAA受体配体,GABAB受体配体,GABAC 受体配体,GABA转氨酶抑制剂。
摘要: 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.
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Cite this article as:
Kowalczyk P. and Kulig K., GABA System as a Target for New Drugs, Current Medicinal Chemistry 2014; 21 (28) . https://dx.doi.org/10.2174/0929867321666140601202158
DOI https://dx.doi.org/10.2174/0929867321666140601202158 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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