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.
Export Options
About this article
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Potential Therapeutic Targets for Neurodegenerative Diseases: Lessons Learned from Calorie Restriction
Current Drug Targets Obstructive Sleep Apnea Syndrome: From Phenotype to Genetic Basis
Current Genomics Minimizing AED Adverse Effects: Improving Quality of Life in the Interictal State in Epilepsy Care
Current Neuropharmacology Adult Neurogenesis in the Hypothalamus: Evidence, Functions and Implications
CNS & Neurological Disorders - Drug Targets p75NTR as a Therapeutic Target for Neuropsychiatric Diseases
Current Molecular Pharmacology Subject Index to Volume 4
Current Topics in Medicinal Chemistry Effect of Hemodialysis on Pharmacokinetics of Ezogabine/Retigabine and its N-Acetyl Metabolite in Patients with End Stage Renal Disease
Current Clinical Pharmacology Non-Pharmacological Treatments for ADHD in Youth
Adolescent Psychiatry Epilepsy, Comorbidities and Treatments
Current Pharmaceutical Design Metabolic and Functional Brain Mapping, Connectivity and Plasticity Applied to the Surgery of Cerebral Tumors
Current Medical Imaging Cardioembolic Stroke: Clinical Features, Specific Cardiac Disorders and Prognosis
Current Cardiology Reviews Potential Use of Nanomedicine for Drug Delivery Across the Blood-Brain Barrier in Healthy and Diseased Brain
CNS & Neurological Disorders - Drug Targets Neuronal and Extraneuronal Nicotinic Acetylcholine Receptors
Current Neuropharmacology Recent Patents and Discovery of Anti-inflammatory Agents from Marine Source
Recent Patents on Inflammation & Allergy Drug Discovery Recent Developments on the Use of Nanomaterials for the Treatment of Epilepsy
Mini-Reviews in Medicinal Chemistry Synthesis and Some Reactions of 1-aryl-4-acetyl-5-methyl-1,2,3-triazole Derivatives with Anticonvulsant Activity
Mini-Reviews in Medicinal Chemistry Vascular and Parenchymal Mechanisms in Multiple Drug Resistance: a Lesson from Human Epilepsy
Current Drug Targets Understanding Genotypes and Phenotypes of the Mutations in Voltage- Gated Sodium Channel α Subunits in Epilepsy
CNS & Neurological Disorders - Drug Targets Subject Index To Volume 12
Current Pharmaceutical Design Barbiturates: A Review of Synthesis and Antimicrobial Research Progress
Current Organic Synthesis