kainate receptor antagonist (IC50
= 130 nM); also blocks recombinant homomeric GLUK7
receptors. Displays 12,700-fold selectivity for GLUK5
. Exhibits no activity at mGlu group I or NMDA receptors at concentrations of up to 10 μ
M. Apparent KD
value is 18 ± 4 nM for depression of kainate responses on the dorsal root.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists.
Mayer et al.
Antagonism of recombinant and native GluK3-containing kainate receptors.
Perrais et al.
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: Role of the substituent at the 5-position of the uracil ring in development of highly potent and selective GLUK5 kainate receptor antagonists.
Dolman et al.
The citations listed below are publications that use Tocris products. Selected citations for UBP 310 include:
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