| Description | TCN 213 is an antagonist of NMDA receptor that has a selective for NR1/NR2A over NR1/NR2B |
| In vitro | 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. |
| Target activity | GluN1/GluN2A NMDAR:0.55-40 μM (IC50) |
| Synonyms | TCN213 |
| molecular weight | 376.54 |
| Molecular formula | C18H24N4OS2 |
| CAS | 556803-08-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 30 mg/mL (79.67 mM) |
| References | 1. Mckay S , Griffiths N H , Butters P A , et al. Direct pharmacological monitoring of the developmental switch in NMDA receptor subunit composition using TCN 213, a GluN2A-selective, glycine-dependent antagonist[J]. British Journal of Pharmacology, 2012, 166(3):924-937. |