7-Chlorokynurenic acid is an antagonist of NMDA receptor acting at the glycine site. It can also act as competitive inhibitor of L-glutamate transport into synaptic vesicles.

UCPH 101 selectively but not competitively inhibit excitatory amino acid transporter 1 (EAAT1) with IC50 of 660 nM. It exhibits relatively weak inhibition of other subtypes.

GT 949 is a potent and selective EAAT2 positive allosteric modulator with EC50 of 0.26 nM.

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

Chicago Sky Blue 6B is a potent inhibitor of L-glutamate uptake into synaptic vesicles and also inhibits macrophage migration inhibitory factor (MIF) with IC50 of 0.81 μM.

L-CCG-IV is a potent agonist of the NMDA receptor.

DL-TBOA is a competitive and non-transportable blocker of excitatory amino acid transporters with IC50 values of 70, 6, 6, 4.4 and 3.2 μM for EAAT1, EAAT2, EAAT3, EAAT4 and EAAT5 respectively.

cis-ACBD is a competitive and selective inhibitor of glutamate uptake.

(±)-HIP-A is a non-competitive blocker of excitatory amino acid transporter (EAAT).

High affinity EAAT1 and EAAT2 blocker

MPDC is a potent inhibitor of the Na+-dependent high-affinity synaptosomal glutamate transporter.