TCN 201

Modify Date: 2024-01-08 21:55:29

TCN 201 Structure
TCN 201 structure
Common Name TCN 201
CAS Number 852918-02-6 Molecular Weight 461.894
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C21H17ClFN3O4S Melting Point N/A
MSDS USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of TCN 201


TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDAR. TCN 201 antagonism is dependent on the GluN1-agonist concentration. TCN 201 allows pharmacological identification of native GluN2A-containing NMDAR populations[1].

 Names

Name N-[[4-(benzamidocarbamoyl)phenyl]methyl]-3-chloro-4-fluorobenzenesulfonamide
Synonym More Synonyms

 TCN 201 Biological Activity

Description TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDAR. TCN 201 antagonism is dependent on the GluN1-agonist concentration. TCN 201 allows pharmacological identification of native GluN2A-containing NMDAR populations[1].
Related Catalog
Target

NMDAR[1]

In Vitro TCN 201 (10 μM) produces only slight inhibition of GluN1/GluN2B NMDAR-mediated currents in oocytes[1]. TCN 201 (10-30 μM) antagonism of NMDAR-mediated responses is both subtype- and glycine-dependent and more potent than TCN 213 in oocytes[1]. TCN 201 (0.1-100 μM) does not produce complete block of NMDAR-mediated responses in oocytes[1]. TCN 201 (10 μM) antagonism of NMDAR-mediated currents shows a negative correlation with their ifenprodil sensitivity in rat cortical neurons[1]. TCN 201 (1-9 μM) suppresses cortical spreading depression (CSD) in chick retina[2].
In Vivo TCN-201 (10 mg/kg; i.p.) is ineffective in CSD g blood-oxygen level-dependent (BOLD) response in rats[3].
References

[1]. 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.

[2]. Bu F, et, al. NR2A contributes to genesis and propagation of cortical spreading depression in rats. Sci Rep. 2016 Mar 22;6:23576.

[3]. Shatillo A, et, al. Involvement of NMDA receptor subtypes in cortical spreading depression in rats assessed by fMRI. Neuropharmacology. 2015 Jun; 93:164-70.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C21H17ClFN3O4S
Molecular Weight 461.894
Exact Mass 461.061218
PSA 116.24000
LogP 4.13
Index of Refraction 1.625
Storage condition 2-8°C

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Hazard Codes Xi
Risk Phrases 22-36/37/38
Safety Phrases 26-36/37/39
RIDADR NONH for all modes of transport

 Articles3

More Articles
Sensitivity of N-methyl-D-aspartate receptor-mediated excitatory postsynaptic potentials and synaptic plasticity to TCN 201 and TCN 213 in rat hippocampal slices.

J. Pharmacol. Exp. Ther. 352(2) , 267-73, (2014)

Whereas ifenprodil has been used as a selective GluN1/GluN2B (NR1/NR2B, B-type) receptor antagonist to distinguish between GluN2B (NR2B) and GluN2A (NR2A)-containing N-methyl-d-aspartate receptors (NM...

PAR1-activated astrocytes in the nucleus of the solitary tract stimulate adjacent neurons via NMDA receptors.

J. Neurosci. 35(2) , 776-85, (2015)

Severe autonomic dysfunction, including the loss of control of the cardiovascular, respiratory, and gastrointestinal systems, is a common comorbidity of stroke and other bleeding head injuries. Previo...

Extrasynaptic glutamate release through cystine/glutamate antiporter contributes to ischemic damage.

J. Clin. Invest. 124(8) , 3645-55, (2014)

During brain ischemia, an excessive release of glutamate triggers neuronal death through the overactivation of NMDA receptors (NMDARs); however, the underlying pathways that alter glutamate homeostasi...

 Synonyms

Benzoic acid, 4-[[[(3-chloro-4-fluorophenyl)sulfonyl]amino]methyl]-, 2-benzoylhydrazide
tcn 201
qcr-22
N-{4-[(2-Benzoylhydrazino)carbonyl]benzyl}-3-chloro-4-fluorobenzenesulfonamide
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