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 |
- 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
-
Adipose Tissue and Bone Marrow as Sources for Cell-based Therapeutic Angiogenesis in Ischemic Tissues: Biological Foundation and Clinical Prospects for Age-related Vascular Disease
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Hypertension in Type 2 Diabetes Mellitus: Do We Need to Redefine the Role of Sulfonylureas?
Recent Advances in Cardiovascular Drug Discovery (Discontinued) Use of Insulin and Insulin Analogs and Risk of Cancer — Systematic Review and Meta-Analysis of Observational Studies
Current Drug Safety Amiodarone-Induced SIADH: Two Cases Report
Endocrine, Metabolic & Immune Disorders - Drug Targets Pharmacological Targeting of Neuronal Kv7.2/3 Channels: A Focus on Chemotypes and Receptor Sites
Current Medicinal Chemistry Small Molecule Inhibitors of PKCθ as Potential Antiinflammatory Therapeutics
Current Topics in Medicinal Chemistry Editorial (Thematic Issue: Anderson Fabry Disease: A Multiorgan Metabolic Disease Susceptible of Treatment)
Current Pharmaceutical Design Cognitive Impairment and Diabetes
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Update on Cancer Related Issues of Mesenchymal Stem Cell-Based Therapies
Current Stem Cell Research & Therapy An Updated Review for the Diabetic Wound Healing Systems
Current Drug Targets Subject Index to Volume 4
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Role of NFAT5 in Inflammatory Disorders Associated with Osmotic Stress
Current Genomics Chemical Constituents and Biological Activities of Cordia myxa L.: A Review
The Natural Products Journal Stem Cells Derived from Human Exfoliated Deciduous Teeth (SHED) in Neuronal Disorders: A Review
Current Stem Cell Research & Therapy Dynamic Crosstalk between GlcNAcylation and Phosphorylation: Roles in Signaling, Transcription and Human Disease
Current Signal Transduction Therapy Mechanism-Based Treatment in Chronic Neuropathic Pain: The Role of Antidepressants
Current Pharmaceutical Design Human Exfoliated Deciduous Teeth Stem Cells: Features and Therapeutic Effects on Neurogenerative and Hepatobiliary-pancreatic Diseases
Current Stem Cell Research & Therapy Editorial [Hot Topic: Nitric Oxide and Hydrogen Sulfide - Contribution of Gaseous Messengers to the Cardiovascular Control (Guest Editor: Sona Cacanyiova)]
Current Pharmaceutical Biotechnology Risk Profiles in Type 2 Diabetes (Metabolic Syndrome): Integration of IL-10 Polymorphisms and Laboratory Parameters to Identify Vascular Damages Related Complications
Current Pharmaceutical Design Voltage-Gated Sodium Channel Blockers: Synthesis of Mexiletine Analogues and Homologues
Current Medicinal Chemistry