| Bioactivity | 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]. |
| Target | pIC50: 6.8 (GluN1/GluN2A NMDA receptor) |
| Invitro | 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]. |
| In Vivo | TCN-201 (10 mg/kg; i.p.) is ineffective in CSD blood-oxygen level-dependent (BOLD) response in rats[4]. |
| Name | TCN 201 |
| CAS | 852918-02-6 |
| Formula | C21H17ClFN3O4S |
| Molar Mass | 461.89 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture and light *该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
| 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. |
TCN 201
CAS: 852918-02-6 F: C21H17ClFN3O4S W: 461.89
TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDA receptor, with a pIC50 of 6.8. TCN 20
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