TCN 201

Names

[ Name ]:
TCN 201

[Synonym ]:
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

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]:

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[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

[ 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

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...