Formulation: A solid
Formal Name: 4R-methyl-L-glutamic acid
Purity: ≥95%
Formula Markup: C6H11NO4
Formula Weight: 161,2
Shelf life (days): 1460
CAS Number: 31137-74-3
Notes: SYM 2081 is an agonist of the kainate receptor.{69870} 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.{69873} 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.{69871,69872} 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 (Item Nos. 92350 / 10010743).{69874}
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