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

Caldwell, Nicola and Harms, Jonathan E. and Partin, Kathryn M. and Jamieson, Craig (2015) Rational design of a novel AMPA receptor modulator through a hybridization approach. ACS Medicinal Chemistry Letters. (https://doi.org/10.1021/ml5004553)

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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.

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• Item metadata

  Item type:	Article
  ID code:	51911
  Dates:	Date Event 2015 Published 11 February 2015 Published Online 11 February 2015 Accepted
  Subjects:	Science > Chemistry
  Department:	Faculty of Science > Pure and Applied Chemistry
  Depositing user:	Pure Administrator
  Date deposited:	25 Feb 2015 05:12
  Last modified:	08 Apr 2024 22:06
  URI:	https://strathprints.strath.ac.uk/id/eprint/51911