Abstract
There is increasing evidence of the potential therapeutic utility of glutamate receptor antagonists in the treatment of several neurodegenerative disorders, including stroke and epilepsy. In the last few years noncompetitive AMPA receptor antagonists have received considerable attention due to their therapeutic potentiality. The discovery of GYKI 52466, the prototype of noncompetitive AMPA receptor antagonists endowed with anticonvulsant and neuroprotective properties, induced growing interest on 2,3-benzodiazepine derivatives. This review covers the chemistry and pharmacology of this important class of AMPA receptor antagonists.
Keywords: 2,3-Benzodiazepines, AMPA Receptor, glutamate receptor antagonists, neurodegenerative disorders, Stroke, Epilepsy, Anticonvulsant, Neuroprotective
Mini-Reviews in Medicinal Chemistry
Title: synthesis and Structure-Activity Relationships of 2,3-Benzodiazepines as AMPA Receptor Antagonists
Volume: 1 Issue: 3
Author(s): M. Zappala, S. Grasso, N. Micale, S. Polimeni and C. De Micheli
Affiliation:
Keywords: 2,3-Benzodiazepines, AMPA Receptor, glutamate receptor antagonists, neurodegenerative disorders, Stroke, Epilepsy, Anticonvulsant, Neuroprotective
Abstract: There is increasing evidence of the potential therapeutic utility of glutamate receptor antagonists in the treatment of several neurodegenerative disorders, including stroke and epilepsy. In the last few years noncompetitive AMPA receptor antagonists have received considerable attention due to their therapeutic potentiality. The discovery of GYKI 52466, the prototype of noncompetitive AMPA receptor antagonists endowed with anticonvulsant and neuroprotective properties, induced growing interest on 2,3-benzodiazepine derivatives. This review covers the chemistry and pharmacology of this important class of AMPA receptor antagonists.
Export Options
About this article
Cite this article as:
Zappala M., Grasso S., Micale N., Polimeni S. and De Micheli C., synthesis and Structure-Activity Relationships of 2,3-Benzodiazepines as AMPA Receptor Antagonists, Mini-Reviews in Medicinal Chemistry 2001; 1 (3) . https://dx.doi.org/10.2174/1389557013406783
DOI https://dx.doi.org/10.2174/1389557013406783 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...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
Related Articles
-
Pharmacology of Ultrasonic Vocalizations in adult Rats: Significance, Call Classification and Neural Substrate
Current Neuropharmacology Adverse Drug Reactions of Anti-Epileptic Drugs in Children with Epilepsy: A Cross-Sectional Study
Current Drug Safety Potential Phytotherapeutic Approaches for the Treatment of Alzheimer’s Disease: An Overview
Current Traditional Medicine Longitudinal Functional MRI of Motor and Cognitive Recovery Following Stroke: A Review
Current Medical Imaging Genetic Variation of Chromosome 1q42: Etiologic Mechanism of Congenital Disorders of Neuronal Migration and Synaptogenesis
Current Psychiatry Reviews Fibromyalgia: Mechanisms, Current Treatment and Animal Models
Current Pharmaceutical Biotechnology Disorders of Consciousness and Electrophysiological Treatment Strategies: A Review of the Literature and New Perspectives
Current Pharmaceutical Design Advances in Pediatric Epilepsy Surgery
Current Pediatric Reviews GABAergic Modulation in Diabetic Encephalopathy-Related Depression
Current Pharmaceutical Design New Proposals for Testing Drugs with IKr-Blocking Activity to Determine Their Teratogenic Potential
Current Pharmaceutical Design Relevance of Follow-Up in Patients with Core Clinical Criteria for Alzheimer Disease and Normal CSF Biomarkers
Current Alzheimer Research Somatic Genome Variations in Health and Disease
Current Genomics Transcranial Direct Current Stimulation - An Adjuvant Tool for the Treatment of Neuropsychiatric Diseases?
Current Psychiatry Reviews Nicotinic Receptor Mutant Mice in the Study of Autonomic Function
Current Drug Targets - CNS & Neurological Disorders IBD Modern Concepts, Nano Drug Delivery and Patents: An Update
Recent Patents on Nanomedicine Neurological Disorders in Mice Lacking Glycogenes that are Mainly Expressed in Brain
CNS & Neurological Disorders - Drug Targets Volumetric Analysis of the Hypothalamus, Amygdala and Hippocampus in Non-Suicidal and Suicidal Mood Disorder Patients – A Post-Mortem Study
CNS & Neurological Disorders - Drug Targets Clinical Uses of Melatonin in Neurological Diseases and Mental and Behavioural Disorders
Current Medicinal Chemistry Decreased Expression of Sox-1 in Cerebellum of Rat with Generalized Seizures Induced by Kindling Model
CNS & Neurological Disorders - Drug Targets Synaptic Potentiation and Sleep Need: Clues from Molecular and Electrophysiological Studies
Current Topics in Medicinal Chemistry