852918-02-6

852918-02-6 structure

Name: TCN 201
Chemical Name: N-[[4-(benzamidocarbamoyl)phenyl]methyl]-3-chloro-4-fluorobenzenesulfonamide
CAS Number: 852918-02-6
Molecular Formula: C₂₁H₁₇ClFN₃O₄S
Molecular Weight: 461.894
Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
Create Date: 2017-11-08 00:49:05
Modify Date: 2024-01-08 21:55:29
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].

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

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.

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

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

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