Rational Design of a Novel AMPA Receptor Modulator through a Hybridization Approach.
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SUBMITTER: Caldwell N
PROVIDER: S-EPMC4394345 | biostudies-literature | 2015 Apr
REPOSITORIES: biostudies-literature
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Rational Design of a Novel AMPA Receptor Modulator through a Hybridization Approach.
Caldwell Nicola N Harms Jonathan E JE Partin Kathryn M KM Jamieson Craig C
ACS medicinal chemistry letters 20150211 4
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic 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 prom ...[more]
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