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TCN-201
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C21H17ClFN3O4S
- MW: 461.89
Description
TCN-201 is a subunit-selective negative allosteric modulator of GluN1/GluN2A NMDA receptors. It inhibits human recombinant GluN1/GluN2A receptors with a pIC50 of 6.8 and is much less active at GluN1/GluN2B receptors, with a pIC50 below 4.3. TCN-201 binds at the GluN1–GluN2A ligand-binding-domain interface and reduces receptor activation by decreasing the apparent affinity of the GluN1 co-agonist site for glycine or D-serine.
Inhibition by TCN-201 is therefore strongly dependent on co-agonist concentration but largely independent of glutamate concentration. This mechanism makes the compound a useful tool for distinguishing GluN2A-containing receptors and for studying NMDA receptor allostery, glycine-site coupling, synaptic transmission, plasticity, and excitotoxic signaling.
Key Features
- GluN2A-selective NMDA receptor negative allosteric modulator (NAM or allosteric antagonist)
- pIC50: 6.8 at GluN1/GluN2A receptors
- pIC50: below 4.3 at GluN1/GluN2B receptors
- Reduces glycine and D-serine co-agonist potency
- Binds the GluN1–GluN2A ligand-binding-domain interface
Applications
- GluN2A NMDA receptor pharmacology
- NMDA receptor subunit-composition studies
- Glycine-site and allosteric coupling research
- Synaptic plasticity and excitotoxicity models
- Glutamatergic neurotransmission
More Information
| Parent CAS No. | 852918-02-6 |
|---|---|
| Chemical Name | N-(4-(2-Benzoylhydrazinecarbonyl)benzyl)-3-chloro-4-fluorobenzenesulfonamide |
| SMILES | C1(Cl)C=C(S(=O)(=O)NCC2C=CC(C(=O)NNC(=O)C3C=CC=CC=3)=CC=2)C=CC=1F |
| MFCD | MFCD06683895 |
| 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 |
| CID | 4787937 |
| Short Description | NR2A antagonist |
References
- E Bettini 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.
- KB Hansen et al. Subunit-selective allosteric inhibition of glycine binding to NMDA receptors. J Neurosci. 2012 May 2;32(18):6197-208.
- S Edman 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.
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