SYM 2081
Chemical Name: (2S,4R)-4-Methylglutamic acid
Purity: ≥97%
Biological Activity
SYM 2081 is a potent and highly selective kainate receptor agonist, with an IC50 for inhibition of [3H]-kainate binding of 35 nM and almost 3,000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively. Also selectively inhibits the cloned excitatory amino acid transporter EAAT2 at higher concentrations.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.
Additional Information
Background References
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The methylglutamate, SYM 2081, is a potent and highly selective agonist at kainate receptors.
Donevan et al.
J.Pharmacol.Exp.Ther., 1998;285:539 -
Desensitization of kainate receptors by kainate, glutamate and diastereomers of 4-methylglutamate.
Jones et al.
Neuropharmacology, 1997;36:853 -
Characterisation of kainate receptor mediated whole-cell currents in rat cultured cerebellar granule cells.
Savidge et al.
Neuropharmacology, 1999;38:375 -
(2S,4R)-4-Methylglutamic acid (SYM 2081): a selective, high affinity ligand for kainate receptors.
Zhou et al.
J.Pharmacol.Exp.Ther., 1997;280:422
Product Datasheets
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Citations for SYM 2081
The citations listed below are publications that use Tocris products. Selected citations for SYM 2081 include:
6 Citations: Showing 1 - 6
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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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Nitric oxide modulates the temporal properties of the glutamate response in type 4 OFF bipolar cells.
Authors: Vielma Et al.
PLoS One 2014;9:e114330
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Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors.
Authors: Rojas Et al.
Mol Pharmacol 2013;83:106
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A Myosin Va mutant mouse with disruptions in glutamate synaptic development and mature plasticity in visual cortex.
Authors: Yoshii Et al.
Addict Biol 2013;33:8472
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Peripheral calcium-permeable AMPA receptors regulate chronic inflammatory pain in mice.
Authors: Gangadharan Et al.
J Clin Invest 2011;121:1608
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Transmission efficacy and plasticity in glutamatergic synapses formed by excitatory interneurons of the substantia gelatinosa in the rat spinal cord.
Authors: Santos Et al.
PLoS One 2009;4:e8047
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