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Submit ReviewTCN 201
Description: GluN1/GluN2A-selective NMDA antagonist
Chemical Name: 3-Chloro-4-fluoro-N-[4-[[2-(phenylcarbonyl)hydrazino]carbonyl]benzyl]benzenesulfonamide
Purity: ≥99% (HPLC)
Biological Activity for TCN 201
TCN 201 is a NMDA receptor antagonist selective for GluN1/GluN2A (formally NR1/NR2A) over GluN1/GluN2B (formally NR1/NR2B) containing receptors (pIC50 values are 6.8 and <4.3, respectively, in human recombinant GluN1/GluN2A (formally NR1/NR2A) and GluN1/GluN2B (formally NR1/NR2B) FLIPR/Ca2+ assays).
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
Compound Libraries for TCN 201
TCN 201 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for TCN 201
| M. Wt | 461.89 |
| Formula | C21H17ClFN3O4S |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 852918-02-6 |
| PubChem ID | 4787937 |
| InChI Key | FYIBXBFDXNPBSF-UHFFFAOYSA-N |
| Smiles | ClC1=C(F)C=CC(S(NCC2=CC=C(C(NNC(C3=CC=CC=C3)=O)=O)C=C2)(=O)=O)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TCN 201
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.19 | 100 |
Preparing Stock Solutions for TCN 201
The following data is based on the product molecular weight 461.89. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.17 mL | 10.83 mL | 21.65 mL |
| 5 mM | 0.43 mL | 2.17 mL | 4.33 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.17 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets for TCN 201
References for TCN 201
References are publications that support the biological activity of the product.
Bettini et al (2010) Identification and characterization of novel NMDA receptor antagonists selective for NR2A- over NR2B-containing receptors. J.Pharm.Exp.Ther. 335 644 PMID: 20810618
Shin et al (2011) Subtype selective NMDA receptor antagonists induce recovery of synapses lost following exposure to HIV-1 Tat. Br.J.Pharmacol. 166 1002 PMID: 22142193
Edman et al (2012) TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner. Neuropharmacology 63 441 PMID: 22579927
Hansen et al (2012) Subunit-selective allosteric inhibition of glycine binding to NMDA receptors. J.Neurosci. 32 6197 PMID: 22553026
Gipson et al (2013) Reinstatement of nicotine seeking is mediated by glutamatergic plasticity. Proc.Natl.Acad.Sci.U S A [Epub ahead of print] PMID: 23671067
If you know of a relevant reference for TCN 201, please let us know.
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Keywords: TCN 201, TCN 201 supplier, TCN201, NMDA, receptor, agonist, selective, NR1/NR2A, antagonist, GluN1, GluN2A, Receptors, 4154, Tocris Bioscience
14 Citations for TCN 201
Citations are publications that use Tocris products. Selected citations for TCN 201 include:
Hu et al (2015) miR-501-3p mediates the activity-dependent regulation of the expression of AMPA receptor subunit GluA1. J Pharmacol Exp Ther 208 949 PMID: 25800054
Izumi and Zorumski (2015) Sensitivity of N-MthD.-aspartate receptor-mediated excitatory postsynaptic potentials and synaptic plasticity to TCN 201 and TCN 213 in rat hippocampal slices. PeerJ 352 267 PMID: 25413830
Gu et al (2015) miR-26a and miR-384-5p are required for LTP maintenance and spine enlargement. Nat Commun 6 6789 PMID: 25858512
Liu et al (2015) The distinct role of NR2B subunit in the enhancement of visual plasticity in adulthood. Mol Brain 8 49 PMID: 26282667
Bu et al (2016) NR2A contributes to genesis and propagation of cortical spreading depression in rats. Sci Rep 6 23576 PMID: 27001011
McQuail et al (2016) NR2A-Containing NMDARs in the Prefrontal Cortex Are Required for Working Memory and Associated with Age-Related Cognitive Decline. J Neurosci 36 12537 PMID: 27807032
Xinwen et al (2019) HIV gp120-induced neuroinflammation potentiates NMDA receptors to overcome basal suppression of inhibitory synapses by p38 MAPK. J Neurochem 148 499-515 PMID: 30520043
Lassus et al (2018) Glutamatergic and dopaminergic modulation of cortico-striatal circuits probed by dynamic calcium imaging of networks reconstructed in microfluidic chips. Sci Rep 8 17461 PMID: 30498197
Tian et al (2016) STEP activation by Gαq coupled GPCRs opposes Src regulation of NMDA receptors containing the GluN2A subunit Scientific Reports 6 36684 PMID: 27857196
Chen et al (2016) β-arrestin-2 regulates NMDA receptor function in spinal lamina II neurons and duration of persistent pain. Nature Communications 7 12531 PMID: 27538456
Gang et al (2022) Hevin/Sparcl1 drives pathological pain through spinal cord astrocyte and NMDA receptor signaling. JCI Insight 7 PMID: 36256481
Petra et al (2020) GluN2B but Not GluN2A for Basal Dendritic Growth of Cortical Pyramidal Neurons. Front Neuroanat 14 571351 PMID: 33281565
Brancaccio et al (2017) Astrocytes Control Circadian Timekeeping in the Suprachiasmatic Nucleus via Glutamatergic Signaling. Neuron 93 1420 PMID: 28285822
Jia et al (2013) Age-dependent regulation of synaptic connections by DA D2 receptors. Nat Neurosci 16 1627 PMID: 24121738
Do you know of a great paper that uses TCN 201 from Tocris? Please let us know.
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