Abstract
Voltage-gated sodium channels are encoded by a family of ten structurally-related genes that are expressed in spatially and temporally distinct patterns, mainly in excitable tissues. They underlie electrical signalling in nerve and muscle. It has long been known that sodium channel blockers are anaesthetics as well as powerful analgesics when delivered at low concentrations. In addition, cardiac arrhythmias and epileptic activity can be treated with sodium channel blockers. As we have learned more about the sub-types of sodium channels and their distribution, new therapeutic opportunities have suggested themselves. There are indications that sodium channel blockers may also be useful in affective disorders and schizophrenia. The production of tissue-specific and eventually inducible knock out mice as well as genetic studies has proved useful in understanding the specialised role of individual types of sodium channels. The development of sub-type specific blockers has proved slower than anticipated, although the properties of naturally occurring toxin blockers suggest that subtype-specific blockers of sodium channels could be very useful clinically in the treatment of pain.
Current Topics in Medicinal Chemistry
Title: Voltage-Gated Sodium Channel Blockers; Target Validation and Therapeutic Potential
Volume: 5 Issue: 6
Author(s): John N. Wood and James Boorman
Affiliation:
Abstract: Voltage-gated sodium channels are encoded by a family of ten structurally-related genes that are expressed in spatially and temporally distinct patterns, mainly in excitable tissues. They underlie electrical signalling in nerve and muscle. It has long been known that sodium channel blockers are anaesthetics as well as powerful analgesics when delivered at low concentrations. In addition, cardiac arrhythmias and epileptic activity can be treated with sodium channel blockers. As we have learned more about the sub-types of sodium channels and their distribution, new therapeutic opportunities have suggested themselves. There are indications that sodium channel blockers may also be useful in affective disorders and schizophrenia. The production of tissue-specific and eventually inducible knock out mice as well as genetic studies has proved useful in understanding the specialised role of individual types of sodium channels. The development of sub-type specific blockers has proved slower than anticipated, although the properties of naturally occurring toxin blockers suggest that subtype-specific blockers of sodium channels could be very useful clinically in the treatment of pain.
Export Options
About this article
Cite this article as:
John N. Wood and James Boorman , Voltage-Gated Sodium Channel Blockers; Target Validation and Therapeutic Potential, Current Topics in Medicinal Chemistry 2005; 5 (6) . https://dx.doi.org/10.2174/1568026054367584
DOI https://dx.doi.org/10.2174/1568026054367584 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
The Ability of MEAs Containing Cultured Neuroglial Networks to Process Information
Current Bioinformatics Effects of Nucleosides on Glia - Neuron Interactions Open up New Vistas in the Development of More Effective Antiepileptic Drugs
Current Medicinal Chemistry R-Type Voltage-Gated Ca<sup>2+</sup> Channels in Cardiac and Neuronal Rhythmogenesis
Current Molecular Pharmacology GABAB Receptors-Associated Proteins: Potential Drug Targets in Neurological Disorders?
Current Drug Targets Targeting Neuronal Nicotinic Receptors in Cancer: New Ligands and Potential Side-Effects
Recent Patents on Anti-Cancer Drug Discovery Blockers of Voltage-Gated Sodium Channels for the Treatment of Central Nervous System Diseases
Recent Patents on CNS Drug Discovery (Discontinued) The Use of Antibody Engineering to Create Novel Drugs that Target N-methyl-D-Aspartate Receptors
Current Drug Targets Therapeutic Potential of Neurogenesis for Prevention and Recovery from Alzheimers Disease: Allopregnanolone as a Proof of Concept Neurogenic Agent
Current Alzheimer Research Recent Developments in the Treatment of Alcoholic Chronic Pancreatitis
Current Drug Abuse Reviews Challenging Treatment-Resistant Major Depressive Disorder: A Roadmap for Improved Therapeutics
Current Neuropharmacology A Synopsis of Nano-Technological Approaches Toward Anti-Epilepsy Therapy: Present and Future Research Implications
Current Drug Metabolism Sodium Channel Blockers as Therapeutic Target for Treating Epilepsy: Recent Updates
Current Topics in Medicinal Chemistry Computational Models of Neuronal Biophysics and the Characterization of Potential Neuropharmacological Targets
Current Medicinal Chemistry Assessment and Imaging of the Cerebrovascular Glycocalyx
Current Neurovascular Research Neuroinflammation, Diabetes and COVID-19: Perspectives Coming from Ca<sup>2+</sup>/cAMP Signalling
Current Drug Research Reviews Novel Histone Deacetylase Inhibitors for the Treatment of Pediatric Brain Tumors
Central Nervous System Agents in Medicinal Chemistry The Fragile X Family of Disorders: A Model for Autism and Targeted Treatments
Current Pediatric Reviews Viral M2 Ion Channel Protein: A Promising Target for Anti-influenza Drug Discovery
Mini-Reviews in Medicinal Chemistry Psychoemotional Background of Temporomandibular Joint Dysfunction and Possible Drug Therapy
Letters in Drug Design & Discovery Neurogenesis as a New Target for the Development of Antidepressant Drugs
Current Pharmaceutical Design