Abstract
Based on the painful effects of exposure to capsaicin, TRPV1 (transient receptor potential vanilloid subfamily member 1) lo-calization is most readily associated with peripheral sensory neurons, however, TRPV1 is now known to be expressed, albeit at lower levels, in the spinal cord, brain and a wide-range of non-neuronal cells. The latter includes epithelial cells (e.g. keratinocytes, urothe-lium, gastric epithelial cells, enterocytes, and pneumocytes) through vascular endothelium and cells of the immune system (e.g. T-cells and mast cells) to smooth muscle, fibroblasts and hepatocytes. Despite extensive research, the physiological function of TRPV1 in the brain and in non-neuronal tissues remains elusive. The preliminary results are exciting, but many are unconfirmed and/or contradictory. As yet, studies with TRPV1 knock-out mice have proven unhelpful in clarifying such biological roles. Now that a range of potent and selective TRPV1 antagonists are available in this rapidly expanding research field , further understanding of the biological roles of TRPV1 throughout the body is within reach. In this article, we will summarize the known roles of peripheral TRPV1 receptors in physi-ology and disease and review the current perspectives for the therapeutic potential of TRPV1 agonists and antagonists in the treatment of a wide range of conditions such as pain, cancer, migraine, chronic cough, asthma, rectal hypersensitivity, inflammatory bowel disease, obesity, overactive bladder and diabetes. New applications of targeting central TRPV1 receptors are reviewed in the accompanying arti-cle by Starowicz et al. (in this issue).
Keywords: chronic Pain, Migraine, carcinoma, synthetic TRPV1 agonists, NOD mice, hyperthermia
Current Pharmaceutical Design
Title: Peripheral TRPV1 Receptors As Targets for Drug Development: New Molecules and Mechanisms
Volume: 14 Issue: 1
Author(s): Arpad Szallasi and Martin J. Gunthorpe
Affiliation:
Keywords: chronic Pain, Migraine, carcinoma, synthetic TRPV1 agonists, NOD mice, hyperthermia
Abstract: Based on the painful effects of exposure to capsaicin, TRPV1 (transient receptor potential vanilloid subfamily member 1) lo-calization is most readily associated with peripheral sensory neurons, however, TRPV1 is now known to be expressed, albeit at lower levels, in the spinal cord, brain and a wide-range of non-neuronal cells. The latter includes epithelial cells (e.g. keratinocytes, urothe-lium, gastric epithelial cells, enterocytes, and pneumocytes) through vascular endothelium and cells of the immune system (e.g. T-cells and mast cells) to smooth muscle, fibroblasts and hepatocytes. Despite extensive research, the physiological function of TRPV1 in the brain and in non-neuronal tissues remains elusive. The preliminary results are exciting, but many are unconfirmed and/or contradictory. As yet, studies with TRPV1 knock-out mice have proven unhelpful in clarifying such biological roles. Now that a range of potent and selective TRPV1 antagonists are available in this rapidly expanding research field , further understanding of the biological roles of TRPV1 throughout the body is within reach. In this article, we will summarize the known roles of peripheral TRPV1 receptors in physi-ology and disease and review the current perspectives for the therapeutic potential of TRPV1 agonists and antagonists in the treatment of a wide range of conditions such as pain, cancer, migraine, chronic cough, asthma, rectal hypersensitivity, inflammatory bowel disease, obesity, overactive bladder and diabetes. New applications of targeting central TRPV1 receptors are reviewed in the accompanying arti-cle by Starowicz et al. (in this issue).
Export Options
About this article
Cite this article as:
Szallasi Arpad and Gunthorpe J. Martin, Peripheral TRPV1 Receptors As Targets for Drug Development: New Molecules and Mechanisms, Current Pharmaceutical Design 2008; 14 (1) . https://dx.doi.org/10.2174/138161208783330754
DOI https://dx.doi.org/10.2174/138161208783330754 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
-
Thyroid Hormone Modulation of Immunity: Its Participation in Chronic Stress-Induced Immune Alterations
Current Immunology Reviews (Discontinued) Is Ecto-nucleoside Triphosphate Diphosphohydrolase (NTPDase)-based Therapy of Central Nervous System Disorders Possible?
Mini-Reviews in Medicinal Chemistry Adenosine Receptor Ligands-Recent Developments Part I. Agonists
Current Medicinal Chemistry Molecular Cloning and the Allergenic Characterization of Tropomyosin from Tyrophagus putrescentiae
Protein & Peptide Letters Inhaled KMUP-1 Prevents Allergic Pulmonary Vascular Inflammation and Remodeling via NO and Suppressed MMP-9 and ICAM-1/VCAM-1
Inflammation & Allergy - Drug Targets (Discontinued) Potent Phosphatidylinositol 3-Kinase Inhibitors and Their Biology
Current Drug Discovery Technologies Determination of Phytochemicals by GC-MS in Two Fractions (17 and 21) of Methanol Extract of Loranthus Micranthus and their Antioxidant and Anti-Inflammatory Activity
The Natural Products Journal Structure and Function of Poly(ADP-ribose) Polymerase-1: Role in Oxidative Stress-Related Pathologies
Current Vascular Pharmacology Identification of Small Molecule as a High Affinity β2 Agonist Promiscuously Targeting Wild and Mutated (Thr164Ile) β 2 Adrenergic Receptor in the Treatment of Bronchial Asthma
Current Pharmaceutical Design Therapeutic Potential of Vanillin and its Main Metabolites to Regulate the Inflammatory Response and Oxidative Stress
Mini-Reviews in Medicinal Chemistry Potential Advantages of Using Synchrotron X-ray Based Techniques in Pediatric Research
Current Medicinal Chemistry Cow’s Milk Allergenicity
Endocrine, Metabolic & Immune Disorders - Drug Targets Mastering the Treatment of Diabetes Mellitus Type 1 in Childhood and Adolescence
Current Pediatric Reviews Pediatric Immune Dysfunction and Health Risks Following Early-Life Immune Insult
Current Pediatric Reviews Efficacy and Safety of Mesenchymal Stromal Cells Therapy for COVID-19 Infection: A Systematic Review and Meta-analysis
Current Stem Cell Research & Therapy Antioxidant Food Supplements and Obesity-Related Inflammation
Current Medicinal Chemistry The Pulmonary Renin-Angiotensin System
Current Pharmaceutical Design Synthesis of 3-Arylindazole-1-acetic Acids and In Vitro Study of Potential Antibacterial Effect
Letters in Drug Design & Discovery Atopic Dermatitis and Cytokines: The Immunoregulatory and Therapeutic Implications of Cytokines in Atopic Dermatitis - Part II: Negative Regulation and Cytokine Therapy in Atopic Dermatitis
Recent Patents on Inflammation & Allergy Drug Discovery New Insights on the Possible Role of Mast Cells in Aspirin-Induced Asthma
Current Molecular Pharmacology