Abstract
The enhancement of GABA-mediated synaptic transmission underlies the pharmacotherapy of various neurological diseases. GABAA receptors are thus targets for neuroactive drugs, including classical benzodiazepines, mediating their anxiolytic, hypnotic and anticonvulsant effects via the benzodiazepine site (BZS). Based on findings that low intrinsic efficacy and subtype selectivity can greatly improve the specificity of drugs targeting the BZS, recent research has identified possible drug leads with apparently little side effects. In particular, drug leads of natural sources have been identified as promising candidates. This review describes the advances in the design of effective therapeutics targeting the GABAA receptor, focusing on the more recent research on naturally occurring drug leads. This includes discussion on the isolation of neuroactive alkaloids and flavonoids from herbal medicines and their rational development based on structure-activity relationships studies. Interest in the development of effective therapeutics from natural sources is clear and awaits to be seen whether their medicinal potential can be fulfilled.
Keywords: gabaa receptor, benzodiazepine, alkaloids, flavonoids
Current Pharmaceutical Design
Title: Development of Effective Therapeutics Targeting the GABAA Receptor: Naturally Occurring Alternatives
Volume: 10 Issue: 9
Author(s): S. Y. Tsang and H. Xue
Affiliation:
Keywords: gabaa receptor, benzodiazepine, alkaloids, flavonoids
Abstract: The enhancement of GABA-mediated synaptic transmission underlies the pharmacotherapy of various neurological diseases. GABAA receptors are thus targets for neuroactive drugs, including classical benzodiazepines, mediating their anxiolytic, hypnotic and anticonvulsant effects via the benzodiazepine site (BZS). Based on findings that low intrinsic efficacy and subtype selectivity can greatly improve the specificity of drugs targeting the BZS, recent research has identified possible drug leads with apparently little side effects. In particular, drug leads of natural sources have been identified as promising candidates. This review describes the advances in the design of effective therapeutics targeting the GABAA receptor, focusing on the more recent research on naturally occurring drug leads. This includes discussion on the isolation of neuroactive alkaloids and flavonoids from herbal medicines and their rational development based on structure-activity relationships studies. Interest in the development of effective therapeutics from natural sources is clear and awaits to be seen whether their medicinal potential can be fulfilled.
Export Options
About this article
Cite this article as:
Tsang Y. S. and Xue H., Development of Effective Therapeutics Targeting the GABAA Receptor: Naturally Occurring Alternatives, Current Pharmaceutical Design 2004; 10 (9) . https://dx.doi.org/10.2174/1381612043452767
DOI https://dx.doi.org/10.2174/1381612043452767 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
- 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
-
Review of 5-HT4R Ligands: State of Art and Clinical Applications
Current Topics in Medicinal Chemistry Editorial (Hot Topic: Neurodegeneration: The First IBRO-Middle East Neuroscience Conference)
Current Alzheimer Research Insight into the Epigenetics of Alzheimer's Disease: A Computational Study from Human Interactome
Current Alzheimer Research Group I Metabotropic Glutamate Receptor Interacting Proteins: Fine-Tuning Receptor Functions in Health and Disease
Current Neuropharmacology Erratum
Current Alzheimer Research Synthesis and Evaluation of Chalcone and its Derivatives as Potential Anticholinergic Agents
Letters in Drug Design & Discovery Effects of Thyroid Hormones and their Metabolites on Learning and Memory in Normal and Pathological Conditions
Current Drug Metabolism Elucidating the Risk Factors for Progression from Amyloid-Negative Amnestic Mild Cognitive Impairment to Dementia
Current Alzheimer Research Functional Neuroimaging of Sleep Disorders
Current Pharmaceutical Design Striving for a Fuller Characterization of the Cellular Neuropathology of Depression Subtypes
Current Psychiatry Reviews Clinical Implication of Meissner’s Corpuscles
CNS & Neurological Disorders - Drug Targets Migraine and Coronary Artery Disease: An Open Study on the Genetic Polymorphism of the 5, 10 Methylenetetrahydrofolate (MTHFR) and Angiotensin I-Converting Enzyme (ACE) Genes
Central Nervous System Agents in Medicinal Chemistry The Role of Pericytes in Blood-Brain Barrier Function and Stroke
Current Pharmaceutical Design Functional Magnetic Resonance Imaging in Abstinent MDMA Users: A Review
Current Drug Abuse Reviews Diuretic-Associated Electrolyte Disorders in the Elderly: Risk Factors, Impact, Management and Prevention
Current Drug Safety Past, Present and Future Therapeutics for Cerebellar Ataxias
Current Neuropharmacology Oxidative Stress and Mitochondrial Impairment After Treatment with Anti-HIV Drugs: Clinical Implications
Current Pharmaceutical Design Detecting Non-cognitive Features of Prodromal Neurodegenerative Diseases
Current Aging Science Affective Temperaments and Mood Disorders: A Review of Current Knowledge
Current Psychiatry Reviews A Clinical Perspective: Anti Taus Treatment in Alzheimers Disease
Current Alzheimer Research