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UBP 310 is an antagonist of ionotropic glutamate receptor 5 (GluR5 or GluK1; Kd = 130 nM).1,2,3 It less potently binds GluR2 (GluA2) and GluR6 (GluK2; Kds = 106 and 1,626 µM, respectively).4,2 UBP 310 is inactive at metabotropic GluR group I and NMDA receptors.
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1. Mapping the ligand binding sites of kainate receptors: Molecular determinants of subunit-
2. Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-
3. Antagonism of recombinant and native GluK3-
4. Luminescence resonance energy transfer investigation of conformational changes in the ligand binding domain of a kainate receptor. The Journal of Biological Chemisty 283(40), 27074-27078 (2008).