Abstract
GABAA receptor channels are ubiquitous in the mammalian central nervous system mediating fast inhibitory neurotransmission by becoming permeant to chloride ions in response to GABA. The emphasis of this review is on the rich chemical diversity of ligands that influence GABAA receptor function. Such diversity provides many avenues for the design and development of new chemical entities acting on GABAA receptors. There is also a significant diversity of GABAA receptor subtypes composed of different protein subunits. The discovery of subtype specific agents is a major challenge in the continuing development of GABAA receptor pharmacology. Leads for the discovery of new chemical entities that influence GABAA receptors come from using recombinant GABAA receptors of known subunit composition as has been elegantly demonstrated by the refining of benzodiazepine actions with a1 subunit preferring agents showing sedative properties but not anxiolytic properties. The most recent advances in the therapeutic use of agents acting on GABAA receptors concern the promotion of sound sleep. Many herbal medicines are used to promote sleep and many of their active ingredients include flavonoids and terpenoids known to modulate GABAA receptor function.
Keywords: inhibitory neurotransmitter, ligand-gated ion channels, second membrane-spanning domain (m), schizophrenia, epilepsies, sleep disorders, anxiolytic, benzodiazepines, spatial memory, ethanol
Current Pharmaceutical Design
Title: GABAA Receptor Channel Pharmacology
Volume: 11 Issue: 15
Author(s): Graham A.R. Johnston
Affiliation:
Keywords: inhibitory neurotransmitter, ligand-gated ion channels, second membrane-spanning domain (m), schizophrenia, epilepsies, sleep disorders, anxiolytic, benzodiazepines, spatial memory, ethanol
Abstract: GABAA receptor channels are ubiquitous in the mammalian central nervous system mediating fast inhibitory neurotransmission by becoming permeant to chloride ions in response to GABA. The emphasis of this review is on the rich chemical diversity of ligands that influence GABAA receptor function. Such diversity provides many avenues for the design and development of new chemical entities acting on GABAA receptors. There is also a significant diversity of GABAA receptor subtypes composed of different protein subunits. The discovery of subtype specific agents is a major challenge in the continuing development of GABAA receptor pharmacology. Leads for the discovery of new chemical entities that influence GABAA receptors come from using recombinant GABAA receptors of known subunit composition as has been elegantly demonstrated by the refining of benzodiazepine actions with a1 subunit preferring agents showing sedative properties but not anxiolytic properties. The most recent advances in the therapeutic use of agents acting on GABAA receptors concern the promotion of sound sleep. Many herbal medicines are used to promote sleep and many of their active ingredients include flavonoids and terpenoids known to modulate GABAA receptor function.
Export Options
About this article
Cite this article as:
Johnston A.R. Graham, GABAA Receptor Channel Pharmacology, Current Pharmaceutical Design 2005; 11 (15) . https://dx.doi.org/10.2174/1381612054021024
DOI https://dx.doi.org/10.2174/1381612054021024 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Clinical Risk Management of Interactions Between Natural Products and Drugs
Current Drug Metabolism Meldrum's Acid in Organic Synthesis, an Outlook to Reaction Media
Current Organic Chemistry Therapeutic Potential of Neuregulin in Cardiovascular System: Can we Ignore the Effects of Neuregulin on Electrophysiology?
Mini-Reviews in Medicinal Chemistry Stem Cell Behavior at Hypothermia: A Review Article
Current Stem Cell Research & Therapy Old Weapons for New Wars: Bioactive Molecules From Cnidarian Internal Defense Systems
Central Nervous System Agents in Medicinal Chemistry Molecular Biotheranostic Approaches of Cancers Using LAT Kit Probes
Current Medical Imaging Potential Therapeutic Strategies of Phytochemicals in Neurodegenerative Disorders
Current Topics in Medicinal Chemistry Engineered Probiotic and Prebiotic Nutraceutical Supplementations in Combating Non-communicable Disorders: A Review
Current Pharmaceutical Biotechnology Blood-brain Barrier Drug Discovery for Central Nervous System Infections
Current Drug Targets - Infectious Disorders Gut Microbiota Regulate Astrocytic Functions in the Brain: Possible Therapeutic Consequences
Current Neuropharmacology Antiepileptic Drugs for Preventing Seizures in Patients with Chronic Subdural Hematoma
Current Pharmaceutical Design MtDNA As a Cancer Marker: A Finally Closed Chapter?
Current Genomics Cancer Nanotechnology: Recent Trends and Developments in Strategies for Targeting Cancer Cells to Improve Cancer Imaging and Treatment
Current Drug Metabolism Past, Present and Future Therapeutics for Cerebellar Ataxias
Current Neuropharmacology Positron Emission Tomography and Brain Monoamine Neurotransmission - Entries for Study of Drug Interactions
Current Pharmaceutical Design The Role of the Urokinase Receptor in Epilepsy, in Disorders of Language, Cognition, Communication and Behavior, and in the Central Nervous System
Current Pharmaceutical Design Antiepileptic Drugs During Pregnancy: Pharmacokinetics and Transplacental Transfer
Current Pharmaceutical Biotechnology Probenecid: An Emerging Tool for Neuroprotection
CNS & Neurological Disorders - Drug Targets ABC Transporters in the CNS – An Inventory
Current Pharmaceutical Biotechnology Amyloid β Oligomers Decrease Hippocampal Spontaneous Network Activity in an Age-Dependent Manner
Current Alzheimer Research