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 |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- 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
-
COVID-19: Our Current Knowledge of Epidemiology, Pathology, Therapeutic Approaches, and Diagnostic Methods
Anti-Cancer Agents in Medicinal Chemistry <i>In Vivo</i> Longitudinal Monitoring of Changes in the Corpus Callosum Integrity During Disease Progression in a Mouse Model of Alzheimer’s Disease
Current Alzheimer Research N-Aryl-5-aminopyrazole: A Versatile Architecture in Medicinal Chemistry
Mini-Reviews in Medicinal Chemistry Molecular Regulation and Pharmacology of Pacemaker Channels
Current Pharmaceutical Design TRPV1 Channel: A Potential Drug Target for Treating Epilepsy
Current Neuropharmacology Update on the Slow Delayed Rectifier Potassium Current (IKs): Role in Modulating Cardiac Function
Current Medicinal Chemistry Natural Products as Leads for Tuberculosis Drug Development
Current Topics in Medicinal Chemistry Focus on the Role of Glutamate in the Pathology of the Peripheral Nervous System
CNS & Neurological Disorders - Drug Targets Synaptic Plasticity, Metaplasticity and Depression
Current Neuropharmacology Protein Kinases and their Modulation in the Central Nervous System
Current Medicinal Chemistry - Central Nervous System Agents New Hopes in Cancer Battle - A Review of New Molecules and Treatment Strategies
Medicinal Chemistry Pediatric Catatonia: Updating An Old Syndrome in Young People
Current Psychiatry Reviews Antiepileptogenic Effect of Retinoic Acid
Current Neuropharmacology Past, Present and Future of Antiepileptic Drug Therapy - Finding a Place for Heterocyclics
Mini-Reviews in Medicinal Chemistry Role of Vitamins in Neurodegenerative Diseases: A Review
CNS & Neurological Disorders - Drug Targets Glutamate Transporter 1: Target for the Treatment of Alcohol Dependence
Current Medicinal Chemistry An Introduction to Hardware and Methods for Biopotential Measurements: A Review
Recent Patents on Biomedical Engineering (Discontinued) Simultaneous Determination of Lamotrigine, Topiramate, Oxcarbazepine, and 10,11-dihydro-10-hydroxycarbazepine in Human Blood Plasma by UHPLC-MS/MS
Current Analytical Chemistry Molecular Mechanism of a Specific NLRP3 Inhibitor to Alleviate Seizure Severity Induced by Pentylenetetrazole
Current Molecular Pharmacology Therapeutic Drug Monitoring of Phenytoin by Simple, Rapid, Accurate, Highly Sensitive and Novel Method and Its Clinical Applications
Current Pharmaceutical Biotechnology