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
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...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
- 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
-
Echocardiographic Hemodynamic Monitoring in the Critically Ill Patient
Current Cardiology Reviews The Renin-Angiotensin System and the Neurodegenerative Diseases: A Brief Review
Protein & Peptide Letters Histone Post-translational Modifications in Huntington’s and Parkinson’s Diseases
Current Pharmaceutical Design Connecting Parkinsons Disease and Drug Addiction: Common Players Reveal Unexpected Disease Connections and Novel Therapeutic Approaches
Current Pharmaceutical Design Scientific Basis for the Use of Indian Ayurvedic Medicinal Plants in the Treatment of Neurodegenerative Disorders: 1. Ashwagandha
Central Nervous System Agents in Medicinal Chemistry Motor Complications in Parkinson’s Disease: A Comprehensive Review of Emergent Management Strategies
CNS & Neurological Disorders - Drug Targets Therapeutic Strategies in Parkinsons Disease
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Recent Patents Review on Intranasal Administration for CNS Drug Delivery
Recent Patents on Drug Delivery & Formulation Computer-aided Drug Design Applied to Parkinson Targets
Current Neuropharmacology Adenosine in the Central Nervous System: Effects on Neurotransmission and Neuroprotection
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Past, Present and Future Therapeutics for Cerebellar Ataxias
Current Neuropharmacology Improving Adherence to Antipsychotic Pharmacotherapy
Current Clinical Pharmacology A Systems Medicine Clinical Platform for Understanding and Managing Non- Communicable Diseases
Current Pharmaceutical Design Structural Properties of the NMDA Receptor and the Design of Neuroprotective Therapies
Mini-Reviews in Medicinal Chemistry Scope of Lipid Nanoparticles in Neuroscience: Impact on the Treatment of Neurodegenerative Diseases
Current Pharmaceutical Design Organometallic Complexes: New Tools for Chemotherapy
Current Medicinal Chemistry Peripheral and Central Glutamate Dyshomeostasis in Neurodegenerative Disorders
Current Neuropharmacology Pharmacogenetics of Cytochrome P450 (CYP) 1A2 and Variability in Psychotropic Drug Response
Current Psychiatry Reviews Serotonin 5-HT<sub>1A</sub> Receptors and Antipsychotics - An Update in Light of New Concepts and Drugs
Current Pharmaceutical Design A2A Receptor Ligands: Past, Present and Future Trends
Current Topics in Medicinal Chemistry