GLUK5 kainate receptor antagonist (IC50 = 130nM); also blocks recombinant homomeric GLUK7 receptors. Displays 12,700-fold selectivity for GLUK5 over GLUK6. Exhibits no activity at mGlu group I or NMDA receptors at concentrations of up to 10µM. Apparent KD value is 18 ± 4nM for depression of kainate responses on the dorsal root.
Chemical Name: (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-thiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione
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