Chemical Name: (2S,4R)-4-Methylglutamic acid
Biological ActivityPotent 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. Also available as part of the Excitatory Amino Acid Transporter Inhibitor Tocriset™ and Kainate Receptor Tocriset™.
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.
The methylglutamate, SYM 2081, is a potent and highly selective agonist at kainate receptors.
Donevan et al.
Desensitization of kainate receptors by kainate, glutamate and diastereomers of 4-methylglutamate.
Jones et al.
Characterisation of kainate receptor mediated whole-cell currents in rat cultured cerebellar granule cells.
Savidge et al.
(2S,4R)-4-Methylglutamic acid (SYM 2081): a selective, high affinity ligand for kainate receptors.
Zhou et al.
Citations for SYM 2081
The citations listed below are publications that use Tocris products. Selected citations for SYM 2081 include:
5 Citations: Showing 1 - 5
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
Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors.
Authors: Rojas Et al.
Mol Pharmacol 2013;83:106
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
Peripheral calcium-permeable AMPA receptors regulate chronic inflammatory pain in mice.
Authors: Gangadharan Et al.
J Clin Invest 2011;121:1608
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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