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Functional analysis of a novel positive allosteric modulator of AMPA receptors derived from a structure-based drug design strategy

Harms, Jonathan E. and Benveniste, Morris and Maclean, John K.F. and Partin, Kathryn M. and Jamieson, Craig (2013) Functional analysis of a novel positive allosteric modulator of AMPA receptors derived from a structure-based drug design strategy. Neuropharmacology, 64. pp. 45-52. ISSN 0028-3908

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Abstract

Pos. allosteric modulators of α-amino-3-hydroxy-5-methyl-isoxazole-propionic acid (AMPA) receptors facilitate synaptic plasticity and can improve various forms of learning and memory. These modulators show promise as therapeutic agents for the treatment of neurol. disorders such as schizophrenia, ADHD, and mental depression. Three classes of pos. modulator, the benzamides, the thiadiazides, and the biarylsulfonamides differentially occupy a solvent accessible binding pocket at the interface between the two subunits that form the AMPA receptor ligand-binding pocket. Here, we describe the electrophysiol. properties of a new chemotype derived from a structure-based drug design strategy (SBDD), which makes similar receptor interactions compared to previously reported classes of modulator. This pyrazole amide deriv., JAMI1001A, with a promising developability profile, efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.This article is part of a Special Issue entitled ‘Cognitive Enhancers'. [on SciFinder(R)]

Item type: Article
ID code: 41469
Notes: M1 - Copyright (C) 2012 American Chemical Society (ACS). All Rights Reserved. CAPLUS AN 2012:987385(Journal; Online Computer File)
Keywords: electrophysiology, benzamides, cyclothiazide, deactivation, desensitization, kinetics, Pharmacy and materia medica, Chemistry, Cellular and Molecular Neuroscience, Pharmacology
Subjects: Medicine > Pharmacy and materia medica
Science > Chemistry
Department: Faculty of Science > Pure and Applied Chemistry
Related URLs:
    Depositing user: Pure Administrator
    Date Deposited: 16 Oct 2012 10:59
    Last modified: 27 Mar 2014 10:35
    URI: http://strathprints.strath.ac.uk/id/eprint/41469

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