Abstract
Hyperpolarization- and Cyclic Nucleotide-gated (HCN) channels are a family of six transmembrane domain, single pore-loop, hyperpolarization activated, non-selective cation channels. The HCN family consists of four members (HCN1-4). HCN channels represent the molecular correlates of Ih (also known as ‘funny’ If and ‘queer’ Iq), a hyperpolarization- activated current best known for its role in controlling heart rate and in the regulation of neuronal resting membrane potential and excitability. A significant body of molecular and pharmacological evidence is now emerging to support a role for these channels in the function of sensory neurons and pain sensation, particularly pain associated with nerve or tissue injury. As such, HCN channels may represent valid targets for novel analgesic agents. This evidence will be reviewed in this article. We will then summarize our efforts to develop and validate methods for screening for novel HCN channel blockers.
Combinatorial Chemistry & High Throughput Screening
Title: HCN Channels as Targets for Drug Discovery
Volume: 12 Issue: 1
Author(s): Alan D. Wickenden, Sandra R. Chaplan, Adrienne E. Dubin, Hong-Qing Guo, Nyan-Tsz Wu and Michael P. Maher
Affiliation:
Abstract: Hyperpolarization- and Cyclic Nucleotide-gated (HCN) channels are a family of six transmembrane domain, single pore-loop, hyperpolarization activated, non-selective cation channels. The HCN family consists of four members (HCN1-4). HCN channels represent the molecular correlates of Ih (also known as ‘funny’ If and ‘queer’ Iq), a hyperpolarization- activated current best known for its role in controlling heart rate and in the regulation of neuronal resting membrane potential and excitability. A significant body of molecular and pharmacological evidence is now emerging to support a role for these channels in the function of sensory neurons and pain sensation, particularly pain associated with nerve or tissue injury. As such, HCN channels may represent valid targets for novel analgesic agents. This evidence will be reviewed in this article. We will then summarize our efforts to develop and validate methods for screening for novel HCN channel blockers.
Export Options
About this article
Cite this article as:
Wickenden D. Alan, Chaplan R. Sandra, Dubin E. Adrienne, Guo Hong-Qing, Wu Nyan-Tsz and Maher P. Michael, HCN Channels as Targets for Drug Discovery, Combinatorial Chemistry & High Throughput Screening 2009; 12 (1) . https://dx.doi.org/10.2174/138620709787048028
DOI https://dx.doi.org/10.2174/138620709787048028 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...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
Related Articles
-
Role of Immune Cells in the Course of Central Nervous System Injury: Modulation with Natural Products
Current Pharmaceutical Design Therapeutic Potential of Cannabinoids in Trigeminal Neuralgia
Current Drug Targets - CNS & Neurological Disorders Therapeutic Potential of Peptide Toxins that Target Ion Channels
Inflammation & Allergy - Drug Targets (Discontinued) Biological Responses to Hydrogen Molecule and its Preventive Effects on Inflammatory Diseases
Current Pharmaceutical Design Recent Evidence of the Regulatory Role of PPARs in Neural Stem Cells and Their Underlying Mechanisms for Neuroprotective Effects
Current Stem Cell Research & Therapy Ameliorative Potential of Glycyrrhiza glabra Extracts on Memory Impairments in Stress Triggered Rats
Current Traditional Medicine The Atypical Cannabinoid O-1602: Targets, Actions, and the Central Nervous System
Central Nervous System Agents in Medicinal Chemistry Voltage-Gated Sodium Channels as Therapeutic Targets for Treatment of Painful Diabetic Neuropathy
Mini-Reviews in Medicinal Chemistry Tissue Engineering Scaffolds Derived from Chitosan
Current Organic Chemistry Immunotherapeutic Approaches in MS: Update on Pathophysiology and Emerging Agents or Strategies 2006
Endocrine, Metabolic & Immune Disorders - Drug Targets Inhibition of Brain Phospholipase A2 by Antimalarial Drugs: Implications for Neuroprotection in Neurological Disorders
Medicinal Chemistry Reviews - Online (Discontinued) Glucocorticoids: Structure, Signaling and Molecular Mechanisms in the Treatment of Diabetic Retinopathy and Diabetic Macular Edema
Current Molecular Medicine Pharmacological Inhibitors of NAD Biosynthesis as Potential An ticancer Agents
Recent Patents on Anti-Cancer Drug Discovery Pharmacology of Ivabradine and the Effect on Chronic Heart Failure
Current Topics in Medicinal Chemistry Production, Purification, and Biological Activity Analysis of Recombinant Human Persephin Expressed in Insect Cells
Protein & Peptide Letters Extracellular Vesicles as Innovative Tools for Assessing Adverse Effects of Immunosuppressant Drugs
Current Medicinal Chemistry Neuroprotective Strategies for Neurological Disorders by Natural Products: An update
Current Neuropharmacology Aquaporin and Vascular Diseases
Current Neuropharmacology Involvement of the Blood-Brain Barrier in Metabolic Regulation
CNS & Neurological Disorders - Drug Targets Dietary Intakes and Food Habits of Wheelchair Basketball Athletes Compared to Gym Attendees and Individuals who do not Practice Sport Activity
Endocrine, Metabolic & Immune Disorders - Drug Targets