SYM 2081Cat. No. 0903 |
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Chemical Name: (2S,4R)-4-Methylglutamic acid |
Biological Activity
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. Also available as part of the Excitatory Amino Acid Transporter Inhibitor Tocriset™ and Kainate Receptor Tocriset™.Licensing Information
Sold with the permission of Annovis Inc.Certificate of Analysis / Safety Data Sheet
References
Jones et al (1997) Desensitization of kainate receptors by kainate, glutamate and diastereomers of 4-methylglutamate. Neuropharmacology 36 853. PMID: 9225313.
Zhou et al (1997) (2S,4R)-4-Methylglutamic acid (SYM 2081): a selective, high affinity ligand for kainate receptors. J.Pharmacol.Exp.Ther. 280 422. PMID: 8996224.
Donevan et al (1998) The methylglutamate, SYM 2081, is a potent and highly selective agonist at kainate receptors. J.Pharmacol.Exp.Ther. 285 539. PMID: 9580595.
Savidge et al (1999) Characterisation of kainate receptor mediated whole-cell currents in rat cultured cerebellar granule cells. Neuropharmacology 38 375. PMID: 10219975.
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Keywords: SYM 2081, supplier, Inhibitor, EAAT2, kainate, receptors, agonist, selective, EAAT, Excitatory, Amino, Acid, Transporters, GLT-1, Glutamate, Monoamine, Neurotransmitter, iGluR, Ionotropic, SYM2081
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