Chemical Name: (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-thiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione
Biological ActivityGluK1 (formerly GLUK5) kainate receptor antagonist (IC50 = 130 nM); also blocks recombinant homomeric GluK3 (forrmerly GLUK7) receptors. Displays 12,700-fold selectivity for GluK1 (formerly GLUK5) over GluK2 (formerly GLUK6). Exhibits no activity at mGlu group I or NMDA receptors at concentrations of up to 10 μM. Apparent KD value is 18 ± 4 nM for depression of kainate responses on the dorsal root.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists.
Mayer 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.
Antagonism of recombinant and native GluK3-containing kainate receptors.
Perrais et al.
Citations for UBP 310
The citations listed below are publications that use Tocris products. Selected citations for UBP 310 include:
2 Citations: Showing 1 - 2
A synaptic signature for ON- and OFF-center parasol ganglion cells of the primate retina.
Authors: Crook Et al.
Vis Neurosci 2014;31:57
Synaptic pathways that shape the excitatory drive in an OFF retinal ganglion cell.
Authors: Buldyrev Et al.
J Neurophysiol 2012;107:1795
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