Abstract
The NMDAR2B subunit is the focus of increasing interest as a therapeutic target in a wide range of CNS pathologies, including acute and chronic pain, stroke and head trauma, drug-induced dyskinesias, and dementias. Due to significant pharmaceutical endeavor, an impressive collection of chemical leads has been developed which target the NR2B subunit, some of which appear to discriminate between closely related subtypes. We now have the benefit of a structural template for the ifenprodil binding site which should further improve future structure activity relationships. A growing appreciation of the likely extrasynaptic localisation of the NR2B receptor subtype and importance of NR2B protein modification, notably tyrosine phosphorylation, may explain its therapeutic importance. The apparent superior preclinical and clinical data for the second and third generation NR2B compounds is likely to reflect subtype selectivity, a unique mode of action and cellular location of the NR2B receptors in the CNS.
Keywords: nmda receptors, cns, neuropathologies, Ifenprodil
Current Medicinal Chemistry
Title: The NMDA Receptor NR2B Subunit: A Valid Therapeutic Target for Multiple CNS Pathologies
Volume: 11 Issue: 3
Author(s): Paul L. Chazot
Affiliation:
Keywords: nmda receptors, cns, neuropathologies, Ifenprodil
Abstract: The NMDAR2B subunit is the focus of increasing interest as a therapeutic target in a wide range of CNS pathologies, including acute and chronic pain, stroke and head trauma, drug-induced dyskinesias, and dementias. Due to significant pharmaceutical endeavor, an impressive collection of chemical leads has been developed which target the NR2B subunit, some of which appear to discriminate between closely related subtypes. We now have the benefit of a structural template for the ifenprodil binding site which should further improve future structure activity relationships. A growing appreciation of the likely extrasynaptic localisation of the NR2B receptor subtype and importance of NR2B protein modification, notably tyrosine phosphorylation, may explain its therapeutic importance. The apparent superior preclinical and clinical data for the second and third generation NR2B compounds is likely to reflect subtype selectivity, a unique mode of action and cellular location of the NR2B receptors in the CNS.
Export Options
About this article
Cite this article as:
Chazot L. Paul, The NMDA Receptor NR2B Subunit: A Valid Therapeutic Target for Multiple CNS Pathologies, Current Medicinal Chemistry 2004; 11 (3) . https://dx.doi.org/10.2174/0929867043456061
DOI https://dx.doi.org/10.2174/0929867043456061 |
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
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
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
Exhaled Breath Biomarkers in Asthmatic Children
Inflammation & Allergy - Drug Targets (Discontinued) Depot Based Drug Delivery System for the Management of Depression
Current Drug Delivery The Beneficial Effect of Rice Bran Extract Against Rotenone-Induced Experimental Parkinson’s Disease in Rats
Current Molecular Pharmacology New Insight into the Therapeutic Role of 5-HT1A Receptors in Central Nervous System Disorders
Central Nervous System Agents in Medicinal Chemistry New Antipsychotics in Treatment of Mood Instability and Cognitive Perceptual Symptoms in Borderline Personality Disorder
Current Psychopharmacology Theories and Treatment of Drug Dependency: A Neurochemical Perspective
Current Molecular Pharmacology Homology Modeling of Adenosine A2A Receptor and Molecular Docking for Exploration of Appropriate Potent Antagonists for Treatment of Parkinsons Disease
Current Aging Science A2A Adenosine Receptor and its Modulators: Overview on a Druggable GPCR and on Structure-Activity Relationship Analysis and Binding Requirements of Agonists and Antagonists
Current Pharmaceutical Design Recent Advances in Progressive Supranuclear Palsy: A Review
Current Alzheimer Research Olanzapine Loaded Cationic Solid Lipid Nanoparticles for Improved Oral Bioavailability
Current Nanoscience Signal Pathways Mediating Antidepressant and Antipsychotic Drugs on Neuronal Cell Survival
Current Medicinal Chemistry - Central Nervous System Agents Innovations to Control the Environment for Persons with Movement Disorders: Support in Home Care
Recent Patents on Biomedical Engineering (Discontinued) Astrocytes: New Targets for the Treatment of Neurodegenerative Diseases
Current Pharmaceutical Design New Ways of Detecting ADRs in Neonates and Children
Current Pharmaceutical Design Are Antipsychotics Useful in the Treatment of Anorexia Nervosa? A Review of the Literature
Current Psychopharmacology Discovery of MAO-B Inhibitors - Present Status and Future Directions Part I: Oxygen Heterocycles and Analogs
Mini-Reviews in Medicinal Chemistry Biochemical, Molecular and Epigenetic Mechanisms of Valproic Acid Neuroprotection
Current Molecular Pharmacology Pharmacotherapy of Schizophrenia: The Past, Present and Future
Current Drug Therapy 9th International Meeting on Metabotropic Gglutamate Receptors (Taormina, Sicily, October 1-6, 2017).
Current Neuropharmacology A Review of the Current Clinical Use of Quetiapine and Extended Release Quetiapine in the Management of Anxiety and Related Disorders
Current Psychopharmacology