TCN213 是一种可克服的(surmountable)、甘氨酸依赖的GluN1/GluN2A NMDAR选择性拮抗剂，当甘氨酸的含量为75、 750、7500 nM时，IC50s 值分别为 0.55、3.5、40 μM。它可用于在药理学上监测 NMDAR 表达在发育中的皮层神经元中的转换。

TCN213 is an antagonist of NMDA receptor that has a selective for NR1/NR2A over NR1/NR2B

TCN 213 antagonism of GluN1/GluN2A NMDA receptors was dependent on glycine but independent of glutamate concentrations in external recording solutions.?Antagonism by TCN 213 was surmountable and gave a Schild plot with unity slope.?TCN 213 block of GluN1/GluN2B NMDA receptor-mediated currents was negligible.?In cortical neurones, at a early developmental stage predominantly expressing GluN2B-containing NMDA receptors, TCN 213 failed to antagonize NMDA receptor-mediated currents or to prevent GluN2B-dependent, NMDA-induced excitoxicity.?In older cultures (DIV 14) or in neurones transfected with GluN2A subunits, TCN 213 antagonized NMDA-evoked currents.?Block by TCN 213 of NMDA currents inversely correlated with block by ifenprodil, a selective GluN2B antagonist.

556803-08-8

C18H24N4OS2

376.54

TCN213

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