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.

ORCID iDs

Caldwell, Nicola, Harms, Jonathan E., Partin, Kathryn M. and Jamieson, Craig ORCID logoORCID: https://orcid.org/0000-0002-6567-8272;
  • 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:11 Nov 2024 11:00
    URI:https://strathprints.strath.ac.uk/id/eprint/51911
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