Abstract
A large number of therapeutic roles have been proposed for σ1 receptors but the involvement of σ1 receptor in non-acute pain had not been well explored up to now. σ1 receptor knock-out mice became available offering us the possibility to study the role of σ1 receptor in nociception, particularly in models where central sensitization processes play a significant role. Given the attractive therapeutic potential, we have developed a chemical program aimed at the discovery of novel and selective σ1 ligands. Herein we discuss the rational basis of this approach and report preliminary pharmacological results of several chemical series and aspects of their structure-activity relationship on σ1 receptor. Functional data in pain models are presented mainly on one series that provide evidence to consider selective σ1 receptor antagonists an innovative and alternative approach for treating neuropathic pain.
Keywords: Neuropathic pain, analgesia, sigma-1 antagonists, sigma-1 knock-out, central sensitization
Central Nervous System Agents in Medicinal Chemistry
Title: Selective Sigma-1 (σ1) Receptor Antagonists: Emerging Target for the Treatment of Neuropathic Pain
Volume: 9 Issue: 3
Author(s): Jose Luis Diaz, Daniel Zamanillo, Jordi Corbera, Jose Manuel Baeyens, Rafael Maldonado, Miquel Angel Pericàs, Jose Miguel Vela and Antoni Torrens
Affiliation:
Keywords: Neuropathic pain, analgesia, sigma-1 antagonists, sigma-1 knock-out, central sensitization
Abstract: A large number of therapeutic roles have been proposed for σ1 receptors but the involvement of σ1 receptor in non-acute pain had not been well explored up to now. σ1 receptor knock-out mice became available offering us the possibility to study the role of σ1 receptor in nociception, particularly in models where central sensitization processes play a significant role. Given the attractive therapeutic potential, we have developed a chemical program aimed at the discovery of novel and selective σ1 ligands. Herein we discuss the rational basis of this approach and report preliminary pharmacological results of several chemical series and aspects of their structure-activity relationship on σ1 receptor. Functional data in pain models are presented mainly on one series that provide evidence to consider selective σ1 receptor antagonists an innovative and alternative approach for treating neuropathic pain.
Export Options
About this article
Cite this article as:
Diaz Luis Jose, Zamanillo Daniel, Corbera Jordi, Baeyens Manuel Jose, Maldonado Rafael, Pericàs Angel Miquel, Vela Miguel Jose and Torrens Antoni, Selective Sigma-1 (σ1) Receptor Antagonists: Emerging Target for the Treatment of Neuropathic Pain, Central Nervous System Agents in Medicinal Chemistry 2009; 9 (3) . https://dx.doi.org/10.2174/1871524910909030172
DOI https://dx.doi.org/10.2174/1871524910909030172 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
- 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
-
A Survey on the Applications of Implantable Micropump Systems in Drug Delivery
Current Drug Delivery Combination Therapy in Fibromyalgia
Current Pharmaceutical Design Interferon gama induced Tryptophan Degradation Neuropsychiatric and Immunological Consequences
Current Drug Metabolism Autoantibody Reaction to Myelin Basic Protein by Plasma Parvovirus B19 IgG in MS Patients
Protein & Peptide Letters Acknowledgements to Reviewers
Current Medicinal Chemistry The Physio-Pharmacological Role of the NPS/NPSR System in Psychiatric Disorders: A Translational Overview
Current Protein & Peptide Science Medication Assisted Treatment of Drug Abuse and Dependence: Global Availability and Utilization
Recent Patents on Anti-Infective Drug Discovery Pollutants in Organic Chemistry and Medicinal Chemistry Education Laboratory. Experimental and Machine Learning Studies
Current Topics in Medicinal Chemistry Multiple Sclerosis and Neuroinflammation: The Overview of Current and Prospective Therapies
Current Pharmaceutical Design Book Review: Remark the Book of Landmark Papers in Neurology
Current Alzheimer Research 3-Methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol: the Importance of Functional Groups for Antiparkinsonian Activity
Medicinal Chemistry COMT as a Drug Target for Cognitive Functions and Dysfunctions
CNS & Neurological Disorders - Drug Targets Meet Our Editorial Board Member
Current Neuropharmacology Prevention and Treatment of Allergic Asthma in Pregnancy: From Conventional Drugs to New Therapeutical Approaches
Current Pharmaceutical Biotechnology A comprehensive review on the efficacy of S-Adenosyl-L-methionine in Major Depressive Disorder.
CNS & Neurological Disorders - Drug Targets The Role of Psychiatrist in Organ Transplantation: From Gate-keeper to Patient's Advocate
Current Psychiatry Reviews TNF-Related Apoptosis-Inducing Ligand (TRAIL) as a Pro-Apoptotic Signal Transducer with Cancer Therapeutic Potential
Current Pharmaceutical Design Behavioral and Neurochemical Studies in Distinct Animal Models of Ethanols Motivational Effects
Current Drug Abuse Reviews Commentary: Gut Microbiota and Brain Function: A New Target for Brain Diseases?
CNS & Neurological Disorders - Drug Targets Temporal Progression of Kainic Acid Induced Changes in Vascular Laminin Expression in Rat Brain with Neuronal and Glial Correlates
Current Neurovascular Research