Novel subtype-selective and weakly desensitizing AMPA receptor partial agonist (Ki
values are 44, 109, 223, 1890 and 2090 nM at GluR5, GluR1, GluR2, GluR3 and GluR4 receptors respectively). Exhibits potent agonist activity at GluR1 and GluR2 subunit-containing AMPA receptors (EC50
values are 24.9 and 13.9 μ
M respectively) and is excitotoxic in vitro
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Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399 as a novel, potent and subtype-selective AMPA receptor full agonist with partial desensitization properties.
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1H-Cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptor ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators.
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Inherent desensitisation-preventing properties of a novel subtype-selective AMPA receptor agonist, (S)-CPW 399, as a possible explanation for its excitotoxic action in cultured cerebellar granule cells.
Sinclair et al.