TCN 201
Chemical Name: 3-Chloro-4-fluoro-N-[4-[[2-(phenylcarbonyl)hydrazino]carbonyl]benzyl]benzenesulfonamide
Purity: ≥99%
Biological Activity
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.
Technical Data
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.
Background References
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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 -
TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner.
Edman et al.
Neuropharmacology, 2012;63:441 -
Subunit-selective allosteric inhibition of glycine binding to NMDA receptors.
Hansen et al.
J.Neurosci., 2012;32:6197 -
Reinstatement of nicotine seeking is mediated by glutamatergic plasticity.
Gipson et al.
Proc.Natl.Acad.Sci.U S A [Epub ahead of print], 2013; -
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
Product Datasheets
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Citations for TCN 201
The citations listed below are publications that use Tocris products. Selected citations for TCN 201 include:
14 Citations: Showing 1 - 10
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Hevin/Sparcl1 drives pathological pain through spinal cord astrocyte and NMDA receptor signaling.
Authors: Gang Et al.
JCI Insight 2022;7
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GluN2B but Not GluN2A for Basal Dendritic Growth of Cortical Pyramidal Neurons.
Authors: Petra Et al.
Front Neuroanat 2020;14:571351
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HIV gp120-induced neuroinflammation potentiates NMDA receptors to overcome basal suppression of inhibitory synapses by p38 MAPK.
Authors: Xinwen Et al.
J Neurochem 2019;148:499-515
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Glutamatergic and dopaminergic modulation of cortico-striatal circuits probed by dynamic calcium imaging of networks reconstructed in microfluidic chips.
Authors: Lassus Et al.
Sci Rep 2018;8:17461
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Astrocytes Control Circadian Timekeeping in the Suprachiasmatic Nucleus via Glutamatergic Signaling.
Authors: Brancaccio Et al.
Neuron 2017;93:1420
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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
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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
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NR2A contributes to genesis and propagation of cortical spreading depression in rats.
Authors: Bu Et al.
Sci Rep 2016;6:23576
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NR2A-Containing NMDARs in the Prefrontal Cortex Are Required for Working Memory and Associated with Age-Related Cognitive Decline.
Authors: McQuail Et al.
J Neurosci 2016;36:12537
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The distinct role of NR2B subunit in the enhancement of visual plasticity in adulthood.
Authors: Liu Et al.
Mol Brain 2015;8:49
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miR-26a and miR-384-5p are required for LTP maintenance and spine enlargement.
Authors: Gu Et al.
Nat Commun 2015;6:6789
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Sensitivity of N-MthD.-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
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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
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Age-dependent regulation of synaptic connections by DA D2 receptors.
Authors: Jia Et al.
Nat Neurosci 2013;16:1627
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