GT 949 is a positive allosteric modulator of excitatory amino acid transporter 2 (EAAT2; EC50 = 0.26 nM for stimulating glutamate uptake by COS-7 cells expressing EAAT2).1 It is selective for EEAT2 over the serotonin (5-HT) transporter (SERT), the norepinephrine transporter (NET), and the dopamine transporter (DAT; IC50s = >1 mM for all). GT 949 (10 nM) reduces neuronal death induced by L-glutamate, but not hydrogen peroxide, in primary embryonic rat neuron-glia cultures.2
1.Kortagere, S., Mortensen, O.V., Xia, J., et al.Identification of novel allosteric modulators of glutamate transporter EAAT2ACS Chem. Neurosci.9(3)522-534(2018) 2.Falcucci, R.M., Wertz, R., Green, J.L., et al.Novel positive allosteric modulators of glutamate transport have neuroprotective properties in an in vitro excitotoxic modelACS Chem. Neurosci.10(8)3437-3453(2019)