Abstract
Antiepileptic drugs (AEDs) cover a broad spectrum of pathological conditions ranging from seizures following congenital or acquired brain disorders to behavioural and psychiatric disorders and recently neuropathic pain. The need for novel antiepileptics raises from the expanding field of indications as well as from the fact, that special seizure types are refractory to common AEDs. In addition, many of the conventional antiepileptic drugs exhibit an unfavourable side-effect profile. Since there is growing evidence, that NMDA receptor activation might play a crucial role in epilepsy, NMDA receptor antagonists have become compounds of interest in preventing and treating seizures. This review focuses on NMDA receptor antagonistic compounds, which are already in use for the treatment of epileptic seizures (i. e. MgSO4, felbamate) and compounds in clinical trials (i. e. remacemide, ADCI). Further interest is put on NMDA antagonists in preclinical and biological testing (memantine, dizocilpine, conantokins, Co101244 / PD174494, ifenprodil, arcaine, L-701,324, eliprodil, CGP40116, LY235959, LY233053, MRZ2 / 576, LU73068, 4-Cl-KYN). Some of the latter compounds are predominantely of academic interest (i. e. 4-Cl-KYN), others (i. e. dizocilpine, LY235959, LY233053) might be of therapeutical value when combined with conventional AEDs. In order to reduce adverse effects in antiepileptic medication using NMDA antagonists, special interest will be focused on subtype selective compounds. In this respect, Co 101244, a novel potent and selective NR1 / 2B NMDA receptor antagonist might be a lead for therapeutically promising compounds.
Keywords: antiepilptic drugs, nmda receptor, antiepileptic valproic acid vpa, magentic resonance imaging mri, adci, memantineconantokins, ifenprodil, eliprodil, glutamate site, cgp
Current Medicinal Chemistry
Title: The NMDA Receptor Complex: A Promising Target for Novel Antiepileptic Strategies
Volume: 8 Issue: 11
Author(s): B. K. Kohl and G. Dannhardt
Affiliation:
Keywords: antiepilptic drugs, nmda receptor, antiepileptic valproic acid vpa, magentic resonance imaging mri, adci, memantineconantokins, ifenprodil, eliprodil, glutamate site, cgp
Abstract: Antiepileptic drugs (AEDs) cover a broad spectrum of pathological conditions ranging from seizures following congenital or acquired brain disorders to behavioural and psychiatric disorders and recently neuropathic pain. The need for novel antiepileptics raises from the expanding field of indications as well as from the fact, that special seizure types are refractory to common AEDs. In addition, many of the conventional antiepileptic drugs exhibit an unfavourable side-effect profile. Since there is growing evidence, that NMDA receptor activation might play a crucial role in epilepsy, NMDA receptor antagonists have become compounds of interest in preventing and treating seizures. This review focuses on NMDA receptor antagonistic compounds, which are already in use for the treatment of epileptic seizures (i. e. MgSO4, felbamate) and compounds in clinical trials (i. e. remacemide, ADCI). Further interest is put on NMDA antagonists in preclinical and biological testing (memantine, dizocilpine, conantokins, Co101244 / PD174494, ifenprodil, arcaine, L-701,324, eliprodil, CGP40116, LY235959, LY233053, MRZ2 / 576, LU73068, 4-Cl-KYN). Some of the latter compounds are predominantely of academic interest (i. e. 4-Cl-KYN), others (i. e. dizocilpine, LY235959, LY233053) might be of therapeutical value when combined with conventional AEDs. In order to reduce adverse effects in antiepileptic medication using NMDA antagonists, special interest will be focused on subtype selective compounds. In this respect, Co 101244, a novel potent and selective NR1 / 2B NMDA receptor antagonist might be a lead for therapeutically promising compounds.
Export Options
About this article
Cite this article as:
Kohl K. B. and Dannhardt G., The NMDA Receptor Complex: A Promising Target for Novel Antiepileptic Strategies, Current Medicinal Chemistry 2001; 8 (11) . https://dx.doi.org/10.2174/0929867013372328
DOI https://dx.doi.org/10.2174/0929867013372328 |
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
-
Applications of Nanosystems to Anticancer Drug Therapy (Part II. Dendrimers, Micelles, Lipid-based Nanosystems)
Recent Patents on Anti-Cancer Drug Discovery Targeting the Expression of Anti-Apoptotic Proteins by Antisense Oligonucleotides
Current Drug Targets Phytochemicals: Potential in Management of Climacteric Neurobiology
Current Pharmaceutical Design Elderly Patients with Migraine: An Open-Label Study on Prophylaxis Therapy with Levetiracetam
Central Nervous System Agents in Medicinal Chemistry From A1 to A3 en passant Through A2A Receptors in the Hippocampus: Pharmacological Implications
CNS & Neurological Disorders - Drug Targets Ketogenic Diet and Other Dietary Intervention Strategies in the Treatment of Cancer
Current Medicinal Chemistry Metabolism of Drugs Used in the Therapy of Seizures: An Analytical Point of View. Part 1
Current Drug Metabolism Synthesis and Analysis of Anticonvulsant Activities of New 4-[2-(4- alkoxybenzylamino)ethyl]-2H-1,2,4-triazol-3(4H)-one Derivatives
Letters in Drug Design & Discovery Phosphodiesterase 5 Inhibitors in the Treatment of Erectile Dysfunction
Current Pharmaceutical Design An Introduction to Molecular Modeling of G-Protein Coupled Receptors
Current Computer-Aided Drug Design Classical and New Renin-Angiotensin Signalling in Atherosclerosis
Current Signal Transduction Therapy Neurodegenerative Diseases of the Retina and Potential for Protection and Recovery
Current Neuropharmacology Subtype-Selective Noncompetitive Modulators of Metabotropic Glutamate Receptor Subtype 1 (mGluR1)
Current Topics in Medicinal Chemistry Voltage-Gated Sodium Channels: Mutations, Channelopathies and Targets
Current Medicinal Chemistry Pediatrics for Disability: A Comprehensive Approach to Children with Syndromic Psychomotor Delay
Current Pediatric Reviews Cellular Functions of Vaults and their Involvement in Multidrug Resistance
Current Drug Targets The Therapeutic Aspects of the Endocannabinoid System (ECS) for Cancer and their Development: From Nature to Laboratory
Current Pharmaceutical Design Hypersensitivity to Lamotrigine and Nonaromatic Anticonvulsant Drugs: A Review
Current Pharmaceutical Design Evolution of the Human Ion Channel Set
Combinatorial Chemistry & High Throughput Screening Multiscale Modelling of Relationships between Protein Classes and Drug Behavior Across all Diseases Using the CANDO Platform
Mini-Reviews in Medicinal Chemistry