Abstract
This review gives a brief overview of the expression patterns, molecular pharmacology and physiological roles of the vanilloid receptor 1 (VR1). Particular emphasis is given to the therapeutic utility of VR1 modulators. Small molecule agonists of VR1, including capsaicin and RTX, are currently utilized for a number of clinical syndromes, including intractable neuropathic pain, spinal detrusor hyperreflexia, and bladder hypersensitivity; however, antagonists of VR1 have yet to reach the clinic. While the classic VR1 antagonist, capsazepine has proven a useful tool for unraveling the molecular pharmacology of VR1, in vivo studies with this compound have had limited success due to poor pharmacokinetic properties and species selectivity issues. With the cloning of VR1 in 1997, the pharmaceutical community has been provided a molecular target for high throughput screening and small molecule lead discovery and optimization. As a result, resurgence in the interest of VR1 antagonists has given way to many new pharmacological agents that may provide better tools to probe VR1 physiology, and ultimately yield promising therapeutic agents.
Keywords: vr1, capsaicin, resiniferatoxin, antagonist, hyperalgesia, pain, capsazepine, inflammation
Current Medicinal Chemistry
Title: Current Perspectives on the Therapeutic Utility of VR1 Antagonists
Volume: 11 Issue: 24
Author(s): K. J. Valenzano and Q. Sun
Affiliation:
Keywords: vr1, capsaicin, resiniferatoxin, antagonist, hyperalgesia, pain, capsazepine, inflammation
Abstract: This review gives a brief overview of the expression patterns, molecular pharmacology and physiological roles of the vanilloid receptor 1 (VR1). Particular emphasis is given to the therapeutic utility of VR1 modulators. Small molecule agonists of VR1, including capsaicin and RTX, are currently utilized for a number of clinical syndromes, including intractable neuropathic pain, spinal detrusor hyperreflexia, and bladder hypersensitivity; however, antagonists of VR1 have yet to reach the clinic. While the classic VR1 antagonist, capsazepine has proven a useful tool for unraveling the molecular pharmacology of VR1, in vivo studies with this compound have had limited success due to poor pharmacokinetic properties and species selectivity issues. With the cloning of VR1 in 1997, the pharmaceutical community has been provided a molecular target for high throughput screening and small molecule lead discovery and optimization. As a result, resurgence in the interest of VR1 antagonists has given way to many new pharmacological agents that may provide better tools to probe VR1 physiology, and ultimately yield promising therapeutic agents.
Export Options
About this article
Cite this article as:
Valenzano J. K. and Sun Q., Current Perspectives on the Therapeutic Utility of VR1 Antagonists, Current Medicinal Chemistry 2004; 11 (24) . https://dx.doi.org/10.2174/0929867043363686
DOI https://dx.doi.org/10.2174/0929867043363686 |
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
-
Human Hematopoietic Stem Cells in Gene Therapy: Pre-Clinical and Clinical Issues
Current Gene Therapy Effect of Stilbene and Chalcone Scaffolds Incorporation in Clofibric Acid on PPARα Agonistic Activity
Medicinal Chemistry Roles of TRAF6 in Central Nervous System
Current Neuropharmacology Regulation of Mucous Cell Metaplasia in Bronchial Asthma
Current Molecular Medicine Diabetes Mellitus and Male Aging: Pharmacotherapeutics and Clinical Implications
Current Pharmaceutical Design Rational Targeting of Peroxisome Proliferating Activated Receptor Subtypes
Current Medicinal Chemistry Platelets and Platelet Interaction with Progenitor Cells in Vascular Homeostasis and Inflammation
Current Vascular Pharmacology Technological Advances in Antigen Delivery and Synthetic Peptide Vaccine Developmental Strategies
Mini-Reviews in Medicinal Chemistry Ocular Drug Delivery - New Strategies for Targeting Anterior and Posterior Segments of the Eye
Current Pharmaceutical Design Gene Therapy for Immunologic Tolerance: Using Bone Marrow-Derived Cells to Treat Autoimmunity and Hemophilia
Current Stem Cell Research & Therapy Anti-Angiogenic Therapy as a Cancer Treatment Paradigm
Current Medicinal Chemistry - Anti-Cancer Agents Regulatory T Cells in Central Nervous System: in Health and Disease
Central Nervous System Agents in Medicinal Chemistry T Cell Redirecting Therapies for Cancer Treatment
Current Cancer Drug Targets Pertinence of Apoptosis Markers for the Improvement of In Vitro Fertilization (IVF)
Current Medicinal Chemistry Recent Advances in Understanding Hormonal Therapy Resistant Prostate Cancer
Current Cancer Drug Targets Antifolates - Past, Present and Future
Current Medicinal Chemistry - Anti-Cancer Agents Proteoglycans in Inflammation
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Prophylactic and Therapeutic Approaches Against Respiratory Syncytial Virus
Current Medicinal Chemistry - Anti-Infective Agents Tracking the Mesenchymal Stem Cell Fate After Transplantation Into the Infarcted Myocardium
Current Stem Cell Research & Therapy Metaflammation: Tissue-Specific Alterations of the NLRP3 Inflammasome Platform in Metabolic Syndrome
Current Medicinal Chemistry