Abstract
Kv7.x channels are a family of six transmembrane domain, single pore-loop, voltage-gated K+ channels. Five members of the family have been identified to date, including the cardiac channel Kv7.1 (formerly known as KvLQT1) and four neuronal Kv7.x channels, Kv7.2 – 5. Heteromeric channels containing Kv7.3 and either Kv7.2 or Kv7.5 are thought to underlie the neuronal M-current, a non-inactivating, slowly deactivating, sub-threshold current that has long been known to exert a powerful stabilizing influence on neuronal excitability. Modulators of these channels have the potential to influence neuronal activity in various tissues and are of much interest as therapeutic drug targets for the treatment of a variety of clinical disorders, such as epilepsy and pain. The purpose of the present article is to review the molecular, functional and behavioral evidence validating Kv7.x as drug targets for the treatment of pain. In addition, an update on pre-clinical Kv7 drug discovery efforts will be presented, along with a summary of on-going clinical trials with Kv7 channel activators.
Keywords: Potassium channels, KCNQ, Kv7, pain, retigabine, flupirtine, ICA-27243
Current Pharmaceutical Design
Title: Kv7 Channels as Targets for the Treatment of Pain
Volume: 15 Issue: 15
Author(s): A. D. Wickenden and G. McNaughton-Smith
Affiliation:
Keywords: Potassium channels, KCNQ, Kv7, pain, retigabine, flupirtine, ICA-27243
Abstract: Kv7.x channels are a family of six transmembrane domain, single pore-loop, voltage-gated K+ channels. Five members of the family have been identified to date, including the cardiac channel Kv7.1 (formerly known as KvLQT1) and four neuronal Kv7.x channels, Kv7.2 – 5. Heteromeric channels containing Kv7.3 and either Kv7.2 or Kv7.5 are thought to underlie the neuronal M-current, a non-inactivating, slowly deactivating, sub-threshold current that has long been known to exert a powerful stabilizing influence on neuronal excitability. Modulators of these channels have the potential to influence neuronal activity in various tissues and are of much interest as therapeutic drug targets for the treatment of a variety of clinical disorders, such as epilepsy and pain. The purpose of the present article is to review the molecular, functional and behavioral evidence validating Kv7.x as drug targets for the treatment of pain. In addition, an update on pre-clinical Kv7 drug discovery efforts will be presented, along with a summary of on-going clinical trials with Kv7 channel activators.
Export Options
About this article
Cite this article as:
Wickenden D. A. and McNaughton-Smith G., Kv7 Channels as Targets for the Treatment of Pain, Current Pharmaceutical Design 2009; 15 (15) . https://dx.doi.org/10.2174/138161209788186326
DOI https://dx.doi.org/10.2174/138161209788186326 |
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
-
Pharmacological Aspects of (-)-Deprenyl
Current Medicinal Chemistry Colloidal Supramolecular Aggregates for Therapeutic Application in Neuromedicine
Current Medicinal Chemistry Novel In Situ Activity Assays for the Quantitative Molecular Analysis of Neurodegenerative Processes in the Retina
Current Medicinal Chemistry Purine Ionotropic (P2X) Receptors
Current Pharmaceutical Design Buprenorphine: A Unique Drug with Complex Pharmacology
Current Neuropharmacology Roles of Glycogen Synthase Kinase 3 in Alzheimer’s Disease
Current Alzheimer Research Beta Caryophyllene and Caryophyllene Oxide, Isolated from Aegle Marmelos, as the Potent Anti-inflammatory Agents against Lymphoma and Neuroblastoma Cells
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Role of Catechol-O-Methyltransferase (COMT)-Dependent Processes in Parkinson’s Disease and L-DOPA Treatment
CNS & Neurological Disorders - Drug Targets <i>Rhizoma Coptidis</i> for Alzheimer’s Disease and Vascular Dementia: A Literature Review
Current Vascular Pharmacology Turning REST/NRSF Dysfunction in Huntingtons Disease into a Pharmaceutical Target
Current Pharmaceutical Design Novel Immunotherapies for Hematological Malignancies
Current Molecular Pharmacology Melatonin-mitochondria Interplay in Health and Disease
Current Topics in Medicinal Chemistry Involvement of Membrane Channels in Autoimmune Disorders
Current Pharmaceutical Design Beta-Amyloid, Oxidative Stress and Down Syndrome
Current Alzheimer Research Fatty Acid Synthase: A Target for the Reversal of Liver Steatosis
Current Enzyme Inhibition Data Visualization and Feature Selection Methods in Gel-based Proteomics
Current Protein & Peptide Science RNAi of cat-2, a Putative Tyrosine Hydroxylase, Increases Alpha Synuclein Aggregation and Associated Effects in Transgenic C. elegans
CNS & Neurological Disorders - Drug Targets Stem Cell-Like Brain Cancer Cells
Current Cancer Therapy Reviews Subject Index to Volume 3
Current Drug Targets - CNS & Neurological Disorders Histone Deacetylase Inhibitors: From Chromatin Remodeling to Experimental Cancer Therapeutics
Current Medicinal Chemistry