CAS: 556803-08-8

TCN-213 is a novel agent that has been shown to inhibit glutamate release from neurons. TCN-213 reduces the amount of glutamate in the synaptic cleft, which may prevent excitotoxicity and subsequent cell death. TCN-213 has been shown to have potent anti-depressant effects in animal models, and it binds to the receptor of the a-type subunit of the N-methyl-D-aspartate (NMDA) class of glutamate receptors. This binding prevents the NMDA receptor from opening, thereby preventing membrane depolarization and neurotransmitter release. The binding affinity for this drug is surmountable, meaning that it can be overcome by high concentrations of glutamate or NMDA. TCN-213 also has a slow off rate, which means that it will stay bound for longer periods of time than other drugs.

Applications TCN 213 is a GluN1/GluN2A NMDA receptors antagonist. References McKay, S. et al.: Brit. J. Pharmacol., 166, 924 (2012)

TCN 213 is an antagonist of NMDA receptor that has a selective for NR1/NR2A over NR1/NR2B

TCN 213