SYM 2081

SYM 2081 is an agonist of the kainate receptor. It induces currents in Xenopus oocytes expressing homomeric GluK1 or GluK5 subunit-containing receptors (EC50s = 0.16 and 0.23 µM, respectively). It induces desensitization in HEK293 cells expressing homomeric GluK2 subunit-containing kainate receptors when used at concentrations ranging from 0.03 to 0.3 µM. SYM 2081 selectively binds to the kainate receptor (IC50 = ~0.035 µM) over the AMPA and NMDA receptors (IC50s = >100 and 7 µM, respectively) but does bind to excitatory amino acid transporter 2 (EAAT2, Kb = 3.4 µM) and inhibits glutamate transport. In vivo, SYM 2081 (10, 50, and 100 mg/kg, i.p.) reduces hind paw withdrawal frequency and increases withdrawal latency to mechanical and thermal stimuli in a rat model of hyperalgesia induced by the transient receptor potential vanilloid 1 (TRPV1) agonist capsaicin (Cay-92350, Cay-10010743).Formal Name: 4R-methyl-L-glutamic acid. CAS Number: 31137-74-3. Synonyms: L-erythro-gamma-methyl-Glutamic Acid, L-erythro-4-methyl-Glutamic Acid, (2S,4R)-4-Methylglutamic Acid. Molecular Formula: C6H11NO4. Formula Weight: 161.2. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly Soluble: 0.1-1 mg/ml, Water: Slightly Soluble: 0.1-1 mg/ml. SMILES: OC([C@@H](N)C[C@@H](C)C(O)=O)=O. InChi Code: InChI=1S/C6H11NO4/c1-3(5(8)9)2-4(7)6(10)11/h3-4H,2,7H2,1H3,(H,8,9)(H,10,11)/t3-,4+/m1/s1. InChi Key: KRKRAOXTGDJWNI-DMTCNVIQSA-N.