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
-
Editorial (Thematic Issue: Mental Diseases in Medicinal Chemistry: From Synthetic and Natural Drugs to their Therapeutic Treatments)
Current Topics in Medicinal Chemistry Can Topiramate Induce Pruritus? A Case Report and Review of Literature
CNS & Neurological Disorders - Drug Targets 5-HT7 Receptors
Current Drug Targets - CNS & Neurological Disorders Dry Age-Related Macular Degeneration: Recent Progress of Therapeutic approaches
Current Molecular Pharmacology Serotonin Control of Dopaminergic Neurotransmission: Focus on 5-HT2 Receptors
Current Neuropharmacology A Longitudinal Study of Alterations of S100B, sRAGE and Fas Ligand in Association to Olanzapine Medication in a Sample of First Episode Patients with Schizophrenia
CNS & Neurological Disorders - Drug Targets Metabolic Reprogramming of Human Cells in Response to Oxidative Stress: Implications in the Pathophysiology and Therapy of Mitochondrial Diseases
Current Pharmaceutical Design Potassium Channels and CNS Diseases
CNS & Neurological Disorders - Drug Targets Targeting γ-Aminobutyric Acid (GABA) Carriers to the Brain: Potential Relevance as Antiepileptic Pro-Drugs
Medicinal Chemistry Transglutaminases - Possible Drug Targets in Human Diseases
Current Drug Targets - CNS & Neurological Disorders Design, Synthesis and Anticonvulsant Activity Evaluation of 7-Substituted –[1,2,4]-Triazolo[4,3-f]Pyrimidine Derivatives
Medicinal Chemistry High Throughput Screening for Bioactive Components from Traditional Chinese Medicine
Combinatorial Chemistry & High Throughput Screening In-person vs. eHealth Mindfulness-based Intervention for Adolescents with Chronic Illnesses: A Pilot Randomized Trial
Adolescent Psychiatry Migraine and Central Sensitization: Clinical Features, Main Comorbidities and Therapeutic Perspectives
Current Rheumatology Reviews Extraction, GC-MS Evaluation and Anti-epileptic Potential of Seeds Ethanolic Extract of Putranjiva roxburghii Wall
Central Nervous System Agents in Medicinal Chemistry Microenvironmental Determinants of Adult Neural Stem Cell Proliferation and Lineage Commitment in the Healthy and Injured Central Nervous System
Current Stem Cell Research & Therapy Golgi Localization of Glycosyltransferases Involved in Ganglioside Biosynthesis
Current Drug Targets Defining Primary and Secondary Progenitor Disorders in the Brain: Proteomic Approaches for Analysis of Neural Progenitor Cells
Current Pharmaceutical Biotechnology Possible Protecting Role of TNF-α in Kainic Acid-induced Neurotoxicity Via Down-Regulation of NFκB Signaling Pathway
Current Alzheimer Research Editorial (Thematic Issue: Current Research on Cannabis Use Disorder)
Current Pharmaceutical Design