reuptake of glutamate

7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) is an effecitve and selective antagonist of NMDA receptor with IC50 of 0.56 μM for the glycine B coagonist site. 7-Chlorokynurenic acid inhibits the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM and shows antinociceptive actions after neuraxial delivery.

Hyperforin, a natural product from Hypericum, is commonly used as an antidepressant and also has neurological, inflammatory, antimicrobial, antitumor and antiangiogenic effects. Hyperforin acts as a monoamine reuptake inhibitor (MRI) in vitro, including serotonin, norepinephrine, dopamine, GABA, and glutamate, with an IC 50 of ≈0.1 μg mL. Hyperforin is also capable of inducing the cytochrome P450 enzymes, CYP3A4 and CYP2C9, through binding to and activation of the pregnane X receptor. Hyperforin is capable of activating TRPC6 channels by binding to a specific motif.