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.
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.
Citations for UBP 310
The citations listed below are publications that use Tocris products. Selected citations for UBP 310 include:
3 Citations: Showing 1 - 3
Subunit-selective iGluR antagonists can potentiate heteromeric receptor responses by blocking desensitization
Authors: Pollok and Reiner
Proc Natl Acad Sci USA 2020;117:25851
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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