UBP 310
Chemical Name: (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-thiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione
Purity: ≥98%
Biological Activity
UBP 310 is a GluK1 (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.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists.
Mayer et al.
J.Neurosci., 2006;26:2852 -
Antagonism of recombinant and native GluK3-containing kainate receptors.
Perrais et al.
Neuropharmacology, 2009;56:131 -
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.
J.Med.Chem., 2007;50:1558
Product Datasheets
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Citations for UBP 310
The citations listed below are publications that use Tocris products. Selected citations for UBP 310 include:
5 Citations: Showing 1 - 5
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Slow AMPA receptors in hippocampal principal cells.
Authors: Anna L Et al.
Cell Rep 2021;36:109496
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Subunit-selective iGluR antagonists can potentiate heteromeric receptor responses by blocking desensitization
Authors: Pollok and Reiner
Proc Natl Acad Sci USA 2020;117:25851
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Kinetics of Releasable Synaptic Vesicles and Their Plastic Changes at Hippocampal Mossy Fiber Synapses.
Authors: Takeshi Et al.
Neuron 2017;96:1033-1040.e3
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A synaptic signature for ON- and OFF-center parasol ganglion cells of the primate retina.
Authors: Crook Et al.
Vis Neurosci 2014;31:57
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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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