Abstract
Transient Receptor Potential Vanilloid 1 (TRPV1) is a Ca2+ permeant non-selective cation channel expressed in a subpopulation of primary afferent neurons. TRPV1 is activated by physical and chemical stimuli. It is critical for the detection of nociceptive and thermal inflammatory pain as revealed by the deletion of the TRPV1 gene. TRPV1 is distributed in the peripheral and central terminals of the sensory neurons and plays a role in initiating action potentials at the nerve terminals and modulating neurotransmitter release at the first sensory synapse, respectively. Distribution of TRPV1 in the nerve terminals innervating blood vessels and in parts of the CNS that are not subjected to temperature range that is required to activate TRPV1 suggests a role beyond a noxious thermal sensor. Presently, TRPV1 is being considered as a target for analgesics through evaluation of different antagonists. Here, we will discuss the distribution and the functions of TRPV1, potential use of its agonists and antagonists as analgesics and highlight the functions that are not related to nociceptive transmission that might lead to adverse effects.
Keywords: TRPV1, nociceptors, protein kinases, inflammatory mediators, pain, nociceptive ion channels
Current Neuropharmacology
Title: TRPV1: A Target for Next Generation Analgesics
Volume: 6 Issue: 2
Author(s): Louis S. Premkumar and Parul Sikand
Affiliation:
Keywords: TRPV1, nociceptors, protein kinases, inflammatory mediators, pain, nociceptive ion channels
Abstract: Transient Receptor Potential Vanilloid 1 (TRPV1) is a Ca2+ permeant non-selective cation channel expressed in a subpopulation of primary afferent neurons. TRPV1 is activated by physical and chemical stimuli. It is critical for the detection of nociceptive and thermal inflammatory pain as revealed by the deletion of the TRPV1 gene. TRPV1 is distributed in the peripheral and central terminals of the sensory neurons and plays a role in initiating action potentials at the nerve terminals and modulating neurotransmitter release at the first sensory synapse, respectively. Distribution of TRPV1 in the nerve terminals innervating blood vessels and in parts of the CNS that are not subjected to temperature range that is required to activate TRPV1 suggests a role beyond a noxious thermal sensor. Presently, TRPV1 is being considered as a target for analgesics through evaluation of different antagonists. Here, we will discuss the distribution and the functions of TRPV1, potential use of its agonists and antagonists as analgesics and highlight the functions that are not related to nociceptive transmission that might lead to adverse effects.
Export Options
About this article
Cite this article as:
Premkumar S. Louis and Sikand Parul, TRPV1: A Target for Next Generation Analgesics, Current Neuropharmacology 2008; 6 (2) . https://dx.doi.org/10.2174/157015908784533888
DOI https://dx.doi.org/10.2174/157015908784533888 |
Print ISSN 1570-159X |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6190 |
- 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
-
Improving Adherence to Combination Antiretroviral Therapy in Children with HIV Infection: Challenges and Possibilities
Current Pediatric Reviews Treatment for Obsessive Compulsive Disorder
Current Psychiatry Reviews Interactions of Cnidarian Toxins with the Immune System
Inflammation & Allergy - Drug Targets (Discontinued) Exome-wide pharmacogenomic analysis of response to thiopurines in inflammatory bowel disease patients
Current Pharmacogenomics and Personalized Medicine Pharmaceutical Care: Past, Present and Future
Current Pharmaceutical Design Possible Involvement of Programmed Cell Death Pathways in the Neuroprotective Action of Polyphenols
Current Alzheimer Research The Role of mGlu Receptors in Hippocampal Plasticity Deficits in Neurological and Psychiatric Disorders: Implications for Allosteric Modulators as Novel Therapeutic Strategies
Current Neuropharmacology Insight into the Physiopathologic Mechanism for the Coexistence of Depression and Osteoporosis
Current Signal Transduction Therapy Maximum Temperature Through a Yttrium Stabilized Zirconia Ceramic After Er,Cr:YSGG Laser Irradiation
Current Dentistry Review of Progress in Predicting Protein Methylation Sites
Current Organic Chemistry Meet Our Editorial Board Member
Infectious Disorders - Drug Targets Cardiovascular Effects of Green Tea Catechins: Progress and Promise
Recent Patents on Cardiovascular Drug Discovery Tactile Angle Discrimination Decreases due to Subjective Cognitive Decline in Alzheimer’s Disease
Current Alzheimer Research Daclizumab: A Potential Asthma Therapy?
Recent Patents on Inflammation & Allergy Drug Discovery Modulating Blood-Brain Barrier Permeability and Treatment-Resistant Psychiatric Illness: Is Pituitary Neuroimaging a New Frontier?
Current Pharmacogenomics and Personalized Medicine Understanding the Structural Basis of ALDH-2 Inhibition by Molecular Docking
Medicinal Chemistry 2-Amino/Azido/Hydrazino-5-alkoxy-5H-[1]benzopyrano[4,3-d]pyrimidines:Synthesis and Pharmacological Evaluation
Medicinal Chemistry The Importance of the Adenosine A2A Receptor-Dopamine D2 Receptor Interaction in Drug Addiction
Current Medicinal Chemistry Cannabis: An Overview of its Adverse Acute and Chronic Effects and its Implications
Current Drug Abuse Reviews Chemo-botanical and Neurological Accounts of Some Ayurvedic Plants Useful in Mental Health
The Natural Products Journal