Abstract
Amongst ionotropic glutamatergic receptors, the AMPA receptor subtype has been recognized as a major contributor to the fast excitatory neurotransmission in the central nervous system and the expression and maintenance of longterm potentiation. This receptor subtype also represents an interesting target to develop innovative therapeutic drugs such as positive allosteric modulators (AMPA receptor potentiators) since the enhancement of AMPA signals is expected to be beneficial in the management of several neurological disorders such as depression, schizophrenia, Parkinsons disease and learning-memory deficits linked to Alzheimers disease. This article is dedicated to the use of (hetero)aromatic ring-fused thiadiazines (i.e. benzo- pyrido- and thienothiadiazines) as core structures for the discovery of new positive allosteric modulators of AMPA receptors. Recent advances exploring other chemotypes in the field of AMPA potentiators is the object of a separate review of the present issue.
Keywords: Positive allosteric modulators, AMPA receptor potentiators, benzothiadiazines, pyridothiadiazines, thienothiadiazines, neurological disorders, ionotropic glutamatergic receptors, Alzheimer's disease, schizophrenia, Parkinson's disease, postsynaptic receptors, modulators, thienothiadiazi-nes, central nervous system, Kainic acid
Current Medicinal Chemistry
Title: Ring-Fused Thiadiazines as Core Structures for the Development of Potent AMPA Receptor Potentiators
Volume: 17 Issue: 30
Author(s): B. Pirotte, P. Francotte, E. Goffin, P. Fraikin, L. Danober, B. Lesur, I. Botez, D.-H. Caignard, P. Lestage and P. de Tullio
Affiliation:
Keywords: Positive allosteric modulators, AMPA receptor potentiators, benzothiadiazines, pyridothiadiazines, thienothiadiazines, neurological disorders, ionotropic glutamatergic receptors, Alzheimer's disease, schizophrenia, Parkinson's disease, postsynaptic receptors, modulators, thienothiadiazi-nes, central nervous system, Kainic acid
Abstract: Amongst ionotropic glutamatergic receptors, the AMPA receptor subtype has been recognized as a major contributor to the fast excitatory neurotransmission in the central nervous system and the expression and maintenance of longterm potentiation. This receptor subtype also represents an interesting target to develop innovative therapeutic drugs such as positive allosteric modulators (AMPA receptor potentiators) since the enhancement of AMPA signals is expected to be beneficial in the management of several neurological disorders such as depression, schizophrenia, Parkinsons disease and learning-memory deficits linked to Alzheimers disease. This article is dedicated to the use of (hetero)aromatic ring-fused thiadiazines (i.e. benzo- pyrido- and thienothiadiazines) as core structures for the discovery of new positive allosteric modulators of AMPA receptors. Recent advances exploring other chemotypes in the field of AMPA potentiators is the object of a separate review of the present issue.
Export Options
About this article
Cite this article as:
Pirotte B., Francotte P., Goffin E., Fraikin P., Danober L., Lesur B., Botez I., Caignard D.-H., Lestage P. and de Tullio P., Ring-Fused Thiadiazines as Core Structures for the Development of Potent AMPA Receptor Potentiators, Current Medicinal Chemistry 2010; 17 (30) . https://dx.doi.org/10.2174/092986710792927859
DOI https://dx.doi.org/10.2174/092986710792927859 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- 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
-
What Do Athletes Know on the Effect of Steroids? An Exploratory Study in Italy
CNS & Neurological Disorders - Drug Targets Genetic Studies in Relation to Kuru: An Overview
Current Molecular Medicine Gastrodia Elata Bl Attenuates Cocaine-Induced Conditioned Place Preference and Convulsion, but not Behavioral Sensitization in Mice: Importance of GABAA Receptors
Current Neuropharmacology Planum Temporale Analysis Via a New Volumetric Method in Autoptic Brains of Demented and Psychotic Patients
Current Alzheimer Research Effects of Cannabis on the Adolescent Brain
Current Pharmaceutical Design The Control of Endoplasmic Reticulum-Initiated Apoptosis by the BCL-2 Family of Proteins
Current Molecular Medicine Preface
Current Neuropharmacology Genetic and Modifying Factors that Determine the Risk of Brain Tumors
Central Nervous System Agents in Medicinal Chemistry Bioactive Compounds in Some Culinary Aromatic Herbs and Their Effects on Human Health
Mini-Reviews in Medicinal Chemistry Neck Circumference and its Correlation to Other Anthropometric Parameters and Finnish Diabetes Risk Score (FINDRISC)
Current Diabetes Reviews Role of Cervical Cancer Radiotherapy in the Expression of EGFR and p53 Gene
Current Proteomics What is the Current Role for Vitamin D and the Risk of Stroke?
Current Neurovascular Research Non-Pharmacologic Treatment Options in Rheumatologic Disease
Current Rheumatology Reviews Expanded Temporal Binding Windows in People with Mild Cognitive Impairment
Current Alzheimer Research Induced Stem Cells as a Novel Multiple Sclerosis Therapy
Current Stem Cell Research & Therapy GABAB Receptors as Potential Therapeutic Targets
Current Drug Targets - CNS & Neurological Disorders RNAi for the Treatment of Prion Disease: A Window for Intervention in Neurodegeneration?
CNS & Neurological Disorders - Drug Targets Neurotoxicity of β-Amyloid Protein: Oligomerization, Channel Formation and Calcium Dyshomeostasis
Current Pharmaceutical Design The Linkage Between Inflammation and Immune Tolerance: Interfering with Inflammation in Cancer
Current Cancer Drug Targets Arab Countries Research Activities in Engineering During 1977- 2012: A Bibliometric Analysis Approach
Recent Innovations in Chemical Engineering