Uses
GT 949 is a selective EAAT2 positive allosteric modulator (EC50 = 0.26 nM). Enhances the glutamate translocation rate, with no effect on substrate interaction. Increases glutamate removal by 70%. Exhibits no effect on DAT, SERT and NET or NMDA receptors.
Biological Activity
GT949 is a potent and selective positive allosteric modulator (PAM) of the excitatory amino acid transporter EAAT2 (glutamate uptake EC50 = 0.26 nM; COS-7 EAAT2 transfectant), but not EAAT1 or EAAT3. GT949 enhances glutamate uptake of cultured r at astrocytes (EC50 = 1 nM, Emax = 158%) with no potency toward human serotonin (SERT), noradrenaline (NET) and dopamine (DAT) transporters, nor NMDA receptors (murine primary cortical neurons).
