Abstract
As T-type calcium channels open near resting membrane potential and markedly influence neuronal excitability their activity needs to be tightly regulated. Few neuronal T-current regulations have been described so far, but interestingly some of them involve unusual mechanisms like G protein-independent but receptor-coupled modulation, while the use of recombinant channels has established both a direct action of Gβγ subunits, anandamide, arachidonic acid and a phophorylation process by CaMKII. Nearly all reported types of modulation involve Cav3.2 channels while no regulation of Cav3.1 has been reported, a difference that may originate from diversities in the intracellular loop connecting the II and III domains of the two isotypes. The search for T-current regulators requires taking into account their peculiar activation properties, since a close link may exist between the channel conformation and its modulation. Indeed, in thalamocortical neurons a phosphorylationmediated regulation of the amplitude of the T-current has been shown to be highly dependent upon the state of the channel and only to become apparent when the channels are in the voltage range close to neuronal resting membrane potential.
Keywords: Cav3.1, Cav3.2, Cav3.3, regulation, kinases, second messenger, thalamocortical neurons, dorsal root ganglion
CNS & Neurological Disorders - Drug Targets
Title: Modulation of Neuronal T-Type Calcium Channels
Volume: 5 Issue: 6
Author(s): R. C. Lambert, T. Bessaih and N. Leresche
Affiliation:
Keywords: Cav3.1, Cav3.2, Cav3.3, regulation, kinases, second messenger, thalamocortical neurons, dorsal root ganglion
Abstract: As T-type calcium channels open near resting membrane potential and markedly influence neuronal excitability their activity needs to be tightly regulated. Few neuronal T-current regulations have been described so far, but interestingly some of them involve unusual mechanisms like G protein-independent but receptor-coupled modulation, while the use of recombinant channels has established both a direct action of Gβγ subunits, anandamide, arachidonic acid and a phophorylation process by CaMKII. Nearly all reported types of modulation involve Cav3.2 channels while no regulation of Cav3.1 has been reported, a difference that may originate from diversities in the intracellular loop connecting the II and III domains of the two isotypes. The search for T-current regulators requires taking into account their peculiar activation properties, since a close link may exist between the channel conformation and its modulation. Indeed, in thalamocortical neurons a phosphorylationmediated regulation of the amplitude of the T-current has been shown to be highly dependent upon the state of the channel and only to become apparent when the channels are in the voltage range close to neuronal resting membrane potential.
Export Options
About this article
Cite this article as:
Lambert C. R., Bessaih T. and Leresche N., Modulation of Neuronal T-Type Calcium Channels, CNS & Neurological Disorders - Drug Targets 2006; 5 (6) . https://dx.doi.org/10.2174/187152706779025544
DOI https://dx.doi.org/10.2174/187152706779025544 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
Call for Papers in Thematic Issues
Diagnosis and treatment of central nervous system infectious diseases
Infectious diseases of the central nervous system (CNS) can be divided into bacterial, tuberculous, viral, fungal, parasitic infections, etc. Early etiological treatment is often the most crucial means to reduce the mortality rate of patients with central nervous system infections, reduce complications and sequelae, and improve prognosis. The initial clinical ...read more
Techniques of Drug Repurposing: Delivering a new life to Herbs & Drugs
Of late, with the adaptation of innovative approaches and integration of advancements made towards medical sciences as well as the availability of a wide range of tools; several therapeutic challenges are being translated into viable clinical solutions, with a high degree of efficacy, safety, and selectivity. With a better understanding ...read more
Trends and perspectives in the rational management of CNS disorders
Central nervous system (CNS) diseases enforce a significant global health burden, driving ongoing efforts to improve our understanding and effectiveness of therapy. This issue investigates current advances in the discipline, focusing on the understanding as well as therapeutic handling of various CNS diseases. The issue covers a variety of diseases, ...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
-
The Use of SIFT-MS to Investigate Headspace Aldehydes as Markers of Lipid Peroxidation
Current Analytical Chemistry Nanowired Drug Delivery Across the Blood-Brain Barrier in Central Nervous System Injury and Repair
CNS & Neurological Disorders - Drug Targets Hepatic Effects of Duloxetine-I: Non-Clinical and Clinical Trial Data
Current Drug Safety Kinases as Targets for Parkinson's Disease: From Genetics to Therapy
CNS & Neurological Disorders - Drug Targets Start Small and Stay Small: Minimizing Attrition in the Clinic with a Focus on CNS Therapeutics
Current Topics in Medicinal Chemistry CypD: The Key to the Death Door
CNS & Neurological Disorders - Drug Targets Pharmacogenomics in Alzheimers Disease
Mini-Reviews in Medicinal Chemistry Towards a Reconceptualization of Striatal Interactions Between Glutamatergic and Dopaminergic Neurotransmission and Their Contribution to the Production of Movements
Current Neuropharmacology Castor Oil Based Multifunctional Greener Additives for Lubricating Oil
Current Environmental Engineering Diffuse Intrinsic Pontine Glioma: New Pathophysiological Insights and Emerging Therapeutic Targets
Current Neuropharmacology Review of Antibiotic and Non-Antibiotic Properties of Beta-lactam Molecules
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry New Insights in Mast Cell Modulation by Palmitoylethanolamide
CNS & Neurological Disorders - Drug Targets A Novel Work on Analyzing STRESS and Depression level of Indian Population During COVID-19
Recent Advances in Computer Science and Communications Estrogen Regulation of MicroRNA Expression
Current Genomics Neuroimmune Crosstalk in CNS Disorders: The Histamine Connection
Current Pharmaceutical Design Hydrogen Sulfide in Physiological and Pathological Mechanisms in Brain
CNS & Neurological Disorders - Drug Targets Ion Selective Electrodes for Potentiometric Determination of Tizanidine in Its Pharmaceutical Dosage Form
Current Pharmaceutical Analysis Amelioration of Myocardial Ischemic Reperfusion Injury with Calendula Officinalis
Current Pharmaceutical Biotechnology Ionotropic Glutamate Receptors & CNS Disorders
CNS & Neurological Disorders - Drug Targets Piper sarmentosum Roxb. Root Extracts Confer Neuroprotection by Attenuating Beta Amyloid-Induced Pro-Inflammatory Cytokines Released from Microglial Cells
Current Alzheimer Research