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ChemMedChem. 2013 Feb;8(2):226-30. doi: 10.1002/cmdc.201200554. Epub 2012 Dec 20.

A combined bioinformatics and chemoinformatics approach for developing asymmetric bivalent AMPA receptor positive allosteric modulators as neuroprotective agents.

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  • 1Chemical Biology Program, Department of Pharmacology & Toxicology, Center for Addiction Research, University of Texas Medical Branch, 301 University Boulevard, Galveston, TX 77555, USA.


PAMs new in town! An effective, combined bioinformatics and chemoinformatics approach was applied to the design of novel asymmetric bivalent α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor positive allosteric modulators (PAMs) with marked potency in vitro and efficacy in vivo for preventing neuroapoptosis. The novel chemotype could provide pharmacological probes and potential therapeutic agents for glutamatergic hypofunction and its related neurological and psychiatric disorders.

Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

[PubMed - indexed for MEDLINE]
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