Abstract
In mammals several members of the Transient Receptor Potential channel family (TRPs), expressed mainly in the sensory neurons and skin keratinocytes, are implicated in relevant physiological functions, including thermosensation, nociception and vision. Since the TRPV1-4, TRPA1 and TRPM8 channels from this family play a pivotal role in both the detection and possibly modulation of painful stimuli, they are regarded as a very promising target of novel analgesic drugs. A few agents acting at TRPs, such as capsaicin or menthol, have a long history of their application as analgesics, whereas others (e.g. SB705498, JTS653, JNJ17203212, AP18, A967079, Chembridge-5861528 or PBMC) are currently being evaluated both in animals and in humans. In this review we discuss pain physiology, as well as the pharmacological properties of the TRPs involved in pain detection as potential critical peripheral analgesic targets. We present one of the most relevant strategies in the search for novel analgesic drugs, namely the TRP channels and their ligands, both agonists and antagonists as potential novel therapeutics for inflammatory and neuropathic pain syndromes. The safety profile of these agents, in particular their impact on thermosensation, is also discussed below.
Keywords: Analgesic drugs, hyperthermia, innocuous and noxious cold detection, pain pathways, polymodal nociceptor, transient receptor potential family, vanilloids
Current Medicinal Chemistry
Title:Transient Receptor Potential Channels - Emerging Novel Drug Targets for the Treatment of Pain
Volume: 20 Issue: 11
Author(s): Kinga Salat, Andrzej Moniczewski and Tadeusz Librowski
Affiliation:
Keywords: Analgesic drugs, hyperthermia, innocuous and noxious cold detection, pain pathways, polymodal nociceptor, transient receptor potential family, vanilloids
Abstract: In mammals several members of the Transient Receptor Potential channel family (TRPs), expressed mainly in the sensory neurons and skin keratinocytes, are implicated in relevant physiological functions, including thermosensation, nociception and vision. Since the TRPV1-4, TRPA1 and TRPM8 channels from this family play a pivotal role in both the detection and possibly modulation of painful stimuli, they are regarded as a very promising target of novel analgesic drugs. A few agents acting at TRPs, such as capsaicin or menthol, have a long history of their application as analgesics, whereas others (e.g. SB705498, JTS653, JNJ17203212, AP18, A967079, Chembridge-5861528 or PBMC) are currently being evaluated both in animals and in humans. In this review we discuss pain physiology, as well as the pharmacological properties of the TRPs involved in pain detection as potential critical peripheral analgesic targets. We present one of the most relevant strategies in the search for novel analgesic drugs, namely the TRP channels and their ligands, both agonists and antagonists as potential novel therapeutics for inflammatory and neuropathic pain syndromes. The safety profile of these agents, in particular their impact on thermosensation, is also discussed below.
Export Options
About this article
Cite this article as:
Salat Kinga, Moniczewski Andrzej and Librowski Tadeusz, Transient Receptor Potential Channels - Emerging Novel Drug Targets for the Treatment of Pain, Current Medicinal Chemistry 2013; 20 (11) . https://dx.doi.org/10.2174/09298673113209990107
DOI https://dx.doi.org/10.2174/09298673113209990107 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
-
Beta-blockers in Intensive Care Medicine: Potential Benefit in Acute Brain Injury and Acute Respiratory Distress Syndrome
Recent Patents on Cardiovascular Drug Discovery Potential Treatment of Cardiac Hypertrophy and Heart Failure by Inhibiting the Sarcolemmal Binding of Phospholipase Cβ1b
Current Drug Targets Biological Active Ingredients of Traditional Chinese Herb Astragalus membranaceus on Treatment of Diabetes: A Systematic Review
Mini-Reviews in Medicinal Chemistry Preclinical Development of New Therapy for Glycogen Storage Diseases
Current Gene Therapy Characteristics Other than the Diagnostic Criteria Associated with Metabolic Syndrome: An Overview
Current Vascular Pharmacology Therapeutic Interventions for Advanced Glycation-End Products and its Receptor- Mediated Cardiovascular Disease
Current Pharmaceutical Design The Challenges of Blood Pressure Control in Dialysis Patients
Recent Advances in Cardiovascular Drug Discovery (Discontinued) Beyond the Cardiac Myofilament: Hypertrophic Cardiomyopathy- Associated Mutations in Genes that Encode Calcium-Handling Proteins
Current Molecular Medicine Diabetic Cardiomyopathy and its Prevention by Metallothionein: Experimental Evidence, Possible Mechanisms and Clinical Implications
Current Medicinal Chemistry By Discontinuing Beta-Blockers Before an Exercise Test, We may Precipitate a Rebound Phenomenon
Current Vascular Pharmacology Possible Involvement of TRP Channels in Cardiac Hypertrophy and Arrhythmia
Current Topics in Medicinal Chemistry The Involvement of Lysosomes in Myocardial Aging and Disease
Current Cardiology Reviews Plasma Glucose Concentrations and Cardiac Hypertrophy in Essential Hypertension
Current Hypertension Reviews Adeno-associated Viral Vectors for Correction of Inborn Errors of Metabolism: Progressing Towards Clinical Application
Current Pharmaceutical Design A Systematic Review on Levosimendan in Paediatric Patients
Current Vascular Pharmacology Do Advanced Glycation End Products (AGEs) Contribute to the Comorbidities of Polycystic Ovary Syndrome (PCOS)?
Current Pharmaceutical Design Target Peptide Recognition by S100P Protein and Role of Central Linker Region and Dimer Interface
Protein & Peptide Letters Erythropoietin: New Horizon in Cardiovascular Medicine
Recent Patents on Cardiovascular Drug Discovery Aesthetic Cardiology: Adipose-Derived Stem Cells for Myocardial Repair
Current Stem Cell Research & Therapy FoxO Transcription Factors and Regenerative Pathways in Diabetes Mellitus
Current Neurovascular Research