Abstract
This article highlights recent advances in the discovery of new positive allosteric modulators of the AMPA receptor, excluding compounds of thiadiazine chemotype, most of which were developed by Servier and the University of Liege. The field of AMPA receptor modulators continues to be a fertile area for the discovery of new potential therapeutic agents, and recent years have seen a marked diversification in the range of chemotypes prepared. An overview is also given of the recent key new biological data.
Keywords: AMPA receptor, AMPA positive modulator, thiadiazine chemotype, glutamatergic neurotransmitter system, neurodegenerative diseases, schizophrenia,Alzheimer's disease, Parkinson's disease, postsynaptic membrane, tetrameric complex, AMPAR complex, synaptic plasticity, glutamate bound dimer, benzothiadiazines, cornichon proteins, deactivation kinetics, cystine-knot AMPAR, cognitive performance, preclinical behavioural testing, chemotypes, trifluoromethylpyrazole, D-amphetamine-stimulated locomotion, Phenethyl Sulfonamide Series, aromatic thiophene linker, cell voltage-clamp electrophysiology, FLIPR-based assays, Cyclopropane Derivatives, FLUO-4, HEK293, indane core structure, Pyrrole/Thiophene Acid Series, Iminothiazole, Trifluoromethylpyrazole Series
Current Medicinal Chemistry
Title: Recent Advances in the Discovery of Selective AMPA Receptor Positive Allosteric Modulators
Volume: 17 Issue: 30
Author(s): Simon E. Ward and Mark Harries
Affiliation:
Keywords: AMPA receptor, AMPA positive modulator, thiadiazine chemotype, glutamatergic neurotransmitter system, neurodegenerative diseases, schizophrenia,Alzheimer's disease, Parkinson's disease, postsynaptic membrane, tetrameric complex, AMPAR complex, synaptic plasticity, glutamate bound dimer, benzothiadiazines, cornichon proteins, deactivation kinetics, cystine-knot AMPAR, cognitive performance, preclinical behavioural testing, chemotypes, trifluoromethylpyrazole, D-amphetamine-stimulated locomotion, Phenethyl Sulfonamide Series, aromatic thiophene linker, cell voltage-clamp electrophysiology, FLIPR-based assays, Cyclopropane Derivatives, FLUO-4, HEK293, indane core structure, Pyrrole/Thiophene Acid Series, Iminothiazole, Trifluoromethylpyrazole Series
Abstract: This article highlights recent advances in the discovery of new positive allosteric modulators of the AMPA receptor, excluding compounds of thiadiazine chemotype, most of which were developed by Servier and the University of Liege. The field of AMPA receptor modulators continues to be a fertile area for the discovery of new potential therapeutic agents, and recent years have seen a marked diversification in the range of chemotypes prepared. An overview is also given of the recent key new biological data.
Export Options
About this article
Cite this article as:
E. Ward Simon and Harries Mark, Recent Advances in the Discovery of Selective AMPA Receptor Positive Allosteric Modulators, Current Medicinal Chemistry 2010; 17 (30) . https://dx.doi.org/10.2174/092986710792927840
DOI https://dx.doi.org/10.2174/092986710792927840 |
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
-
Nongenomic Thyroxine Regulation of Voltage-gated Sodium Current During Embryonic Development
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Conotoxins and Structural Biology: A Prospective Paradigm for Drug Discovery
Current Protein & Peptide Science Neuroprotective effects of the securinine-analogues: identification of Allomargaritarine as a lead compound
CNS & Neurological Disorders - Drug Targets Editorial [Hot Topic:New Approaches for the Treatment of Pain and Inflammation (Guest Editor: Kaustav Biswas)]
Current Topics in Medicinal Chemistry Dysfunction in Brain-Derived Neurotrophic Factor Signaling Pathway and Susceptibility to Schizophrenia, Parkinson’s and Alzheimer’s Diseases
Current Gene Therapy Biophysics of Parkinsons Disease: Structure and Aggregation of α- Synuclein
Current Protein & Peptide Science Recent Advancements in Pathogenesis, Diagnostics and Treatment of Alzheimer’s Disease
Current Neuropharmacology Selective Agents for Serotonin2C (5-HT2C) Receptor
Current Topics in Medicinal Chemistry Nanotech Revolution for the Anti-Cancer Drug Delivery through Blood- Brain-Barrier
Current Cancer Drug Targets The Structure and Main Functions of Aminopeptidase N
Current Medicinal Chemistry n-Butyl-α-D-fructofuranoside Isolated from Ulmus davidiana Enhances Nrf2 Activity Through Activation of JNK
Current Pharmaceutical Biotechnology Metal Complexes of Uracil Derivatives with Cytotoxicity and Superoxide Scavenging Activity
Letters in Drug Design & Discovery Biochemical Micro-Techniques in the Diagnosis and Classification of Amyloidosis
Current Pharmaceutical Analysis Naringenin Scaffold as a Template for Drug Designing
Current Traditional Medicine IL-3 Control Tau Modifications and Protects Cortical Neurons from Neurodegeneration
Current Alzheimer Research The Effects of CCRC on Cognition and Brain Activity in aMCI Patients: A Pilot Placebo Controlled BOLD fMRI Study
Current Alzheimer Research P-glycoprotein Inhibition: The Past, the Present and the Future
Current Drug Metabolism Pharmacoepigenetics and Pharmacoepigenomics: An Overview
Current Drug Discovery Technologies The Cannabinergic System as a Target for Anti-inflammatory Therapies
Current Topics in Medicinal Chemistry Patent Selections
Recent Patents on Engineering