Abstract
Non-selective cationic channels (NSCC) are a heterogeneous family of channels, widely expressed in nonexcitable and excitable cells, that share several functional characteristics but have diverse molecular origin. NSCC can be formed by transient receptor potential (TRP) channels, calcium activated non-selective channels, hyperpolarization activated cation currents, acid-sensitive cationic channels (ASIC), etc. As a result of its wide expression, as well as to the fact that the activation of such currents produce a persistent membrane depolarization, NSCC have been involved in a variety of neuronal processes such as signal transduction, firing pattern (including plateau potentials and bursting mechanisms) as well as synaptic transmission. Due to the relevance of such channels, alterations in their normal function have been associated with the pathophysiology of several nervous system diseases. Over the last years several blockers of such channels have been discovered. Here we review the pharmacology of NSCC blockers including trivalent cations, verapamil derivates, flufenamic acid, the “typical” TRP blockers 2-APB, ACA and SKF 96365 as well as ASIC blockers. This review focuses on the pharmacological properties of such drugs and their potential use for the understanding of the nervous system as well as for the treatment of neurological diseases.
Keywords: Flufenamic acid, Calcium Activated Non-Selective Currents, Hyperpolarization- Activated Cation Currents, Verapamil, Zatebradine
Mini-Reviews in Medicinal Chemistry
Title: Non-Selective Cation Channel Blockers: Potential Use in Nervous System Basic Research and Therapeutics
Volume: 8 Issue: 8
Author(s): Fernando Pena and Benito Ordaz
Affiliation:
Keywords: Flufenamic acid, Calcium Activated Non-Selective Currents, Hyperpolarization- Activated Cation Currents, Verapamil, Zatebradine
Abstract: Non-selective cationic channels (NSCC) are a heterogeneous family of channels, widely expressed in nonexcitable and excitable cells, that share several functional characteristics but have diverse molecular origin. NSCC can be formed by transient receptor potential (TRP) channels, calcium activated non-selective channels, hyperpolarization activated cation currents, acid-sensitive cationic channels (ASIC), etc. As a result of its wide expression, as well as to the fact that the activation of such currents produce a persistent membrane depolarization, NSCC have been involved in a variety of neuronal processes such as signal transduction, firing pattern (including plateau potentials and bursting mechanisms) as well as synaptic transmission. Due to the relevance of such channels, alterations in their normal function have been associated with the pathophysiology of several nervous system diseases. Over the last years several blockers of such channels have been discovered. Here we review the pharmacology of NSCC blockers including trivalent cations, verapamil derivates, flufenamic acid, the “typical” TRP blockers 2-APB, ACA and SKF 96365 as well as ASIC blockers. This review focuses on the pharmacological properties of such drugs and their potential use for the understanding of the nervous system as well as for the treatment of neurological diseases.
Export Options
About this article
Cite this article as:
Pena Fernando and Ordaz Benito, Non-Selective Cation Channel Blockers: Potential Use in Nervous System Basic Research and Therapeutics, Mini-Reviews in Medicinal Chemistry 2008; 8 (8) . https://dx.doi.org/10.2174/138955708784912166
DOI https://dx.doi.org/10.2174/138955708784912166 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from 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
-
Hippocampal Morphology and Autobiographic Memory in Mild Cognitive Impairment and Alzheimer’s Disease
Current Alzheimer Research Neuroprotective Effects of Exercise Treatments After Injury: The Dual Role of Neurotrophic Factors
Current Neuropharmacology Pharmacological Properties and Therapeutic Potential of Naringenin: A Citrus Flavonoid of Pharmaceutical Promise
Current Pharmaceutical Design Subject Index to Volume 3
Current Drug Targets - CNS & Neurological Disorders Editorial [Is Drug Safety Dangerous?]
Current Drug Safety Exosomes: Natural Carriers for siRNA Delivery
Current Pharmaceutical Design A Retrospective Study on the Incidence of Seizures among Neurosurgical Patients Who Treated with Imipenem/Cilastatin or Meropenem
Current Pharmaceutical Biotechnology Molecular Cytogenetics and Cytogenomics of Brain Diseases
Current Genomics From Discovery to the Coming Generation of Histone Deacetylase Inhibitors
Current Medicinal Chemistry Advances in Neuroimaging for HIV-1 Associated Neurological Dysfunction: Clues to the Diagnosis, Pathogenesis and Therapeutic Monitoring
Current HIV Research Use of Bromine-76 and Iodine-123 Radiohalogenated Tracers in the Drug Development Process
Current Pharmaceutical Design Acute Cardioembolic Cerebral Infarction: Answers to Clinical Questions
Current Cardiology Reviews Valproate Induced Acute Pancreatitis - A Unique Case Report
Current Drug Safety Mitochondrial Complex I Deficiency in Humans
Current Genomics The Four Human γ-Aminobutyric Acid (GABA) Transporters: Pharmacological Characterization and Validation of a Highly Efficient Screening Assay
Combinatorial Chemistry & High Throughput Screening Calcium Homeostasis Following Traumatic Neuronal Injury
Current Neurovascular Research Analysis of Adverse Events Related to 720 Cases of Neural Progenitor Cell Transplantation
CNS & Neurological Disorders - Drug Targets Targeting Histone Deacetylases for the Treatment of Immune, Endocrine & Metabolic Disorders
Endocrine, Metabolic & Immune Disorders - Drug Targets Reading and Writing the Blood-Brain Barrier: Relevance to Therapeutics
Recent Patents on CNS Drug Discovery (Discontinued) Protein Synthesis and Assembly in Mitochondrial Disorders
Current Topics in Medicinal Chemistry