TCN-201 是选择性的、有效的,非竞争性的GluN1/GluN2A NMDA受体拮抗剂,pIC50值为 6.8。与 GluN1/GluN2B NMDA 受体 (pIC50<4.3) 相比,它对 GluN1/GluN2A NMDA 受体具有选择性。
产品描述
TCN-201 is a selective antagonist of NMDA receptors containing the NR2A subunit.
体外活性
TCN-201, a new GluN1/GluN2A-selective NMDA receptor antagonist whose inhibition can be surmounted by glycine.?Electrophysiological recordings from chimeric and mutant rat NMDA receptors suggest that TCN-201 binds to a novel allosteric site located at the dimer interface between the GluN1 and GluN2 agonist binding domains.?Occupancy of this site by TCN-201 inhibits NMDA receptor function by reducing glycine potency.?TCN-201 is therefore a negative allosteric modulator of glycine binding[1].
Cas No.
852918-02-6
分子式
C21H17ClFN3O4S
分子量
461.89
别名
TCN-201
储存和溶解度
DMSO:20mg/ml(43.3mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years