For research use only. Not for therapeutic Use.
TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDA receptor, with a pIC50 of 6.8. TCN 201 is selective for GluN1/GluN2A NMDA receptor over GluN1/GluN2B NMDA receptor (pIC50<4.3)[1][2].
TCN 201 (compound 1) is selective for GluN1/GluN2A NMDAR over GluN1/GluN2B NMDAR, with pIC50s of 6.8 and <4.3, respectively[1].
TCN 201 (10 μM) produces only slight inhibition of GluN1/GluN2B NMDAR-mediated currents in oocytes[2].
TCN 201 (10-30 μM) antagonism of NMDAR-mediated responses is both subtype- and glycine-dependent and more potent than TCN 213 in oocytes[2].
TCN 201 (0.1-100 μM) does not produce complete block of NMDAR-mediated responses in oocytes[2].
TCN 201 (10 μM) antagonism of NMDAR-mediated currents shows a negative correlation with their ifenprodil sensitivity in rat cortical neurons[2].
TCN 201 (1-9 μM) suppresses cortical spreading depression (CSD) in chick retina[3].
TCN-201 (10 mg/kg; i.p.) is ineffective in CSD blood-oxygen level-dependent (BOLD) response in rats[4].
| Catalog Number | R057578 |
| CAS Number | 852918-02-6 |
| Synonyms | N-[[4-(benzamidocarbamoyl)phenyl]methyl]-3-chloro-4-fluorobenzenesulfonamide |
| Molecular Formula | C21H17ClFN3O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C21H17ClFN3O4S/c22-18-12-17(10-11-19(18)23)31(29,30)24-13-14-6-8-16(9-7-14)21(28)26-25-20(27)15-4-2-1-3-5-15/h1-12,24H,13H2,(H,25,27)(H,26,28) |
| InChIKey | FYIBXBFDXNPBSF-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C=C1)C(=O)NNC(=O)C2=CC=C(C=C2)CNS(=O)(=O)C3=CC(=C(C=C3)F)Cl |
| Reference | [1]. Bettini E, et, al. Identification and characterization of novel NMDA receptor antagonists selective for NR2A- over NR2B-containing receptors. J Pharmacol Exp Ther. 2010 Dec; 335(3): 636-44. [2]. Edman S, et, al. TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner. Neuropharmacology. 2012 Sep; 63(3): 441-9. [3]. Bu F, et, al. NR2A contributes to genesis and propagation of cortical spreading depression in rats. Sci Rep. 2016 Mar 22;6:23576. [4]. Shatillo A, et, al. Involvement of NMDA receptor subtypes in cortical spreading depression in rats assessed by fMRI. Neuropharmacology. 2015 Jun; 93:164-70. |
