Rational design of a novel AMPA receptor modulator through a hybridization approach

Nicola Caldwell, Jonathan E. Harms, Kathryn M. Partin, Craig Jamieson

Research output: Contribution to journalArticle

7 Citations (Scopus)
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Abstract

The α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptors are a family of glutamate ion channels of considerable interest in excitatory neurotransmission and associated disease processes. Here, we demonstrate how exploitation of the available X-ray crystal structure of the receptor ligand binding domain enabled the development of a new class of AMPA receptor positive allosteric modulators (7) through hybridization of known ligands (5 and 6), leading to a novel chemotype with promising pharmacological properties.
Original languageEnglish
JournalACS Medicinal Chemistry Letters
Early online date11 Feb 2015
DOIs
Publication statusPublished - 2015

Keywords

  • AMPA receptor
  • structure based drug design
  • hybridization
  • electrophysiology

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