DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.

TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs.

NV-6297 (NV6297) is a potent, selective mTORC1 pathway signaling inhibitor without inhibition on mTORC2, inhibits S6K1 phosphorylation (pS6K1 T389) in MCF7 cells with IC50 of 120 nM, directly and selectively targets GLUT-1.

GTS511 (GTS-511) is a potent, selective, brain-permeable activator of EAAT2 with EC50 of 3.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.

GTS476 (GTS-476) is a potent, selective, orally active activator of EAAT2 with EC50 of 35.1 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.

GT951 (GT-951) is a potent, selective activator (positive allosteric modulator) of EAAT2 with EC50 of 0.8 nM in vitro glutamate uptake assays in COS cells overexpressing EAAT2.

(R)-AS-1 is an orally bioavailable, selective positive allosteric modulator (PAM) of the glutamate transporter EAAT2 with EC50 of 11 nM and Emax of 251%, shows potent antiseizure activity in vivo.

UCPH-101 is a selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor.

LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.

MC-100093 (MC100093) is a potent, orally bioavailable upregulator of GLT-1 and devoid of antimicrobial properties.MC-100093 enhanced uptake of glutamate into astrocytes in a mouse neuron/astrocyte co-culture model with IC50 of 0.1 uM.MC-100093 restored the expression of NA core GLT-1.MC-100093 (50 mg/kg) attenuated cue-primed relapse to cocaine-seeking without reducing motivation to consume regular chow or sucrose pellets or affecting body weight.

WAY-213613 (WAY213613) is a potent, non-substrate inhibitor of EAAT2 (GLT-1) with IC50 of 85 nM, displays > 44-fold selectivity over EAAT1 and EAAT3; also exhibits no activity towards ionotropic and metabotropic glutamate receptors.