Catalog Number: 4154
Chemical Name: 3-Chloro-4-fluoro-N-[4-[[2-(phenylcarbonyl)hydrazino]carbonyl]benzyl]benzenesulfonamide
Biological Activity
NMDA receptor antagonist selective for NR1/NR2A over NR1/NR2B-containing receptors (pIC50 values are 6.8 and <4.3, respectively, in human recombinant NR1/NR2A and NR1/NR2B FLIPR/Ca2+ assays).
Technical Data
  • M.Wt:
    461.89
  • Formula:
    C21H17ClFN3O4S
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    852918-02-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Subtype selective NMDA receptor antagonists induce recovery of synapses lost following exposure to HIV-1 Tat.
    Shin et al.
    Br.J.Pharmacol., 2011;166:1002
  2. Identification and characterization of novel NMDA receptor antagonists selective for NR2A- over NR2B-containing receptors.
    Bettini et al.
    J.Pharm.Exp.Ther., 2010;335:644
  3. TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner.
    Edman et al.
    Neuropharmacology, 2012;63:441
  4. Subunit-selective allosteric inhibition of glycine binding to NMDA receptors.
    Hansen et al.
    J.Neurosci., 2012;32:6197
  5. Reinstatement of nicotine seeking is mediated by glutamatergic plasticity.
    Gipson et al.
    Proc.Natl.Acad.Sci.U S A [Epub ahead of print], 2013;
Citations:

The citations listed below are publications that use Tocris products. Selected citations for TCN 201 include:

7 Citations: Showing 1 - 7
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  1. β-arrestin-2 regulates NMDA receptor function in spinal lamina II neurons and duration of persistent pain.
    Authors: Chen Et al.
    Nature Communications 2016;7:12531
  2. STEP activation by Gαq coupled GPCRs opposes Src regulation of NMDA receptors containing the GluN2A subunit
    Authors: Tian Et al.
    Scientific Reports 2016;6:36684?
  3. The distinct role of NR2B subunit in the enhancement of visual plasticity in adulthood.
    Authors: Liu Et al.
    Mol Brain 2015;8:49
  4. miR-26a and miR-384-5p are required for LTP maintenance and spine enlargement.
    Authors: Gu Et al.
    Nat Commun 2015;6:6789
  5. Sensitivity of N-methyl-D-aspartate receptor-mediated excitatory postsynaptic potentials and synaptic plasticity to TCN 201 and TCN 213 in rat hippocampal slices.
    Authors: Izumi and Zorumski
    PeerJ 2015;352:267
  6. miR-501-3p mediates the activity-dependent regulation of the expression of AMPA receptor subunit GluA1.
    Authors: Hu Et al.
    J Pharmacol Exp Ther 2015;208:949
  7. Age-dependent regulation of synaptic connections by dopamine D2 receptors.
    Authors: Jia Et al.
    Nat Neurosci 2013;16:1627

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