Abstract
The involvement of VR1 in the endogenous pain signalling has converted this receptor into a promising therapeutic target for the development of a new family of potent analgesics devoid of the shortcomings of other analgesics commonly used. The desensitisation induced after VR1 activation points to the utility of VR1 agonists for the treatment of various nociceptive disorders including mitigation of neuropathic pain, inhibition of neurogenic inflammation and suppression of urinary bladder hyperreflexia, whereas VR1 antagonists have been described as valuable agents for the treatment of inflammatory hyperalgesia and pain. Structure of the main classes of VR1 ligands developed to date, their molecular mechanisms of action and their promising utility for the management of diverse nociceptive alterations, specially neuropathic pain, are discussed in this review.
Keywords: vanilloid receptor type 1, analgesia, neuropathic pain, structure-affinity relationship studies
Mini-Reviews in Medicinal Chemistry
Title: VR1 Receptor Modulators as Potential Drugs for Neuropathic Pain
Volume: 3 Issue: 7
Author(s): Maria L. Lopez-Rodriguez, Alma Viso and Silvia Ortega-Gutierrez
Affiliation:
Keywords: vanilloid receptor type 1, analgesia, neuropathic pain, structure-affinity relationship studies
Abstract: The involvement of VR1 in the endogenous pain signalling has converted this receptor into a promising therapeutic target for the development of a new family of potent analgesics devoid of the shortcomings of other analgesics commonly used. The desensitisation induced after VR1 activation points to the utility of VR1 agonists for the treatment of various nociceptive disorders including mitigation of neuropathic pain, inhibition of neurogenic inflammation and suppression of urinary bladder hyperreflexia, whereas VR1 antagonists have been described as valuable agents for the treatment of inflammatory hyperalgesia and pain. Structure of the main classes of VR1 ligands developed to date, their molecular mechanisms of action and their promising utility for the management of diverse nociceptive alterations, specially neuropathic pain, are discussed in this review.
Export Options
About this article
Cite this article as:
Lopez-Rodriguez L. Maria, Viso Alma and Ortega-Gutierrez Silvia, VR1 Receptor Modulators as Potential Drugs for Neuropathic Pain, Mini-Reviews in Medicinal Chemistry 2003; 3 (7) . https://dx.doi.org/10.2174/1389557033487845
DOI https://dx.doi.org/10.2174/1389557033487845 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
-
Antioxidative Activity, Polyphenolic Content and Anti-Glycation Effect of Some Thai Medicinal Plants Traditionally Used in Diabetic Patients
Medicinal Chemistry Pharmacotherapy in Systemic Lupus Erythematosus
Current Rheumatology Reviews Nutraceutical: A Drug, Dietary Supplement and Food Ingredient
Current Pharmacogenomics and Personalized Medicine Predictive Factors of follow-up Non-attendance and Mortality Among Adults with Type 2 Diabetes Mellitus- an Analysis of the Malaysian Diabetes Registry 2009
Current Diabetes Reviews Metabolic Control and Diabetic Retinopathy
Current Diabetes Reviews A Systematic Review of Analytical Profiles of SGLT2 Inhibitors and their Combinations for Treatment of Type 2 Diabetes Mellitus
Current Pharmaceutical Analysis Metabolic and Cardiovascular Ageing Indices in Relation to Glycated Haemoglobin in Healthy and Diabetic Subjects
Current Aging Science Advent and Maturation of Regenerative Medicine
Current Stem Cell Research & Therapy Diabetes and the Impairment of Reproductive Function: Possible Role of Mitochondria and Reactive Oxygen Species
Current Diabetes Reviews Conference Report: 9th International Summer School of Neurology
CNS & Neurological Disorders - Drug Targets MG17, A Novel Triazole Derivative Abrogated Neuroinflammation and Related Neurodegenerative Symptoms in Rodents
Current Molecular Pharmacology Etanercept Improves Cognitive Performance and Increases eNOS and BDNF Expression During Experimental Vascular Dementia in Streptozotocin- induced Diabetes
Current Neurovascular Research Control of Neuropathic Pain by Immune Cells and Opioids
CNS & Neurological Disorders - Drug Targets Bio-Inspired Strategies against Diabetes and Associated Complications: A Review
Recent Patents on Drug Delivery & Formulation FoxO Transcription Factors and Regenerative Pathways in Diabetes Mellitus
Current Neurovascular Research RNAi in Clinical Studies
Current Medicinal Chemistry The Impact of Mitochondrial DNA and Nuclear Genes Related to Mitochondrial Functioning on the Risk of Parkinson’s Disease
Current Genomics Endothelin-1 Impairs Retrograde Axonal Transport and Leads to Axonal Injury in Rat Optic Nerve
Current Neurovascular Research Aryl- and Heteroaryl-Thiosemicarbazone Derivatives and Their Metal Complexes: A Pharmacological Template
Recent Patents on Anti-Cancer Drug Discovery Role of Mechanoinsensitive Nociceptors in Painful Diabetic Peripheral Neuropathy
Current Diabetes Reviews