质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 5 mg/mL (clear solution)
储存温度
2-8°C
SMILES字符串
Fc1ccc(cc1Cl)S(=O)(=O)NCc2ccc(cc2)C(=O)NNC(=O)c3ccccc3
InChI
1S/C21H17ClFN3O4S/c22-18-12-17(10-11-19(18)23)31(29,30)24-13-14-6-8-16(9-7-14)21(28)26-25-20(27)15-4-2-1-3-5-15/h1-12,24H,13H2,(H,25,27)(H,26,28)
InChI key
FYIBXBFDXNPBSF-UHFFFAOYSA-N
生化/生理作用
TCN-201 is a sulphonamide derivative, that negatively modulates glycine binding to the GluN1 (glutamate receptor subunit) subunit of the receptor.
TCN-201 is the first NMDA receptor antagonist that is specific for NR2A-subunit containing receptors. The pIC50 for NR2A NMDA receptors is 6.8. TCN-201has no effect on NR2B-containing receptors at concentrations up to 50 mM.
特点和优势
This compound is featured on the Glutamate Receptors (Ion Channel Family) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
警示用语：
Warning
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Central nervous system, Respiratory system
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Structural basis for negative allosteric modulation of GluN2A-containing NMDA receptors
Yi F, et al.
Neuron, 91(6), 1316-1329 (2016)
Jean-Baptiste Esmenjaud et al.
The EMBO journal, 38(2) (2018-11-07)
NMDA receptors (NMDARs) are glutamate-gated ion channels that are key mediators of excitatory neurotransmission and synaptic plasticity throughout the central nervous system. They form massive heterotetrameric complexes endowed with unique allosteric capacity provided by eight extracellular clamshell-like domains arranged as
TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner
Edman S, et al.
Neuropharmacology, 63(3), 441-449 (2012)
Yan-Hai Li et al.
Neuroscience letters, 715, 134674-134674 (2019-12-07)
Medial vestibular nucleus (MVN) neurons are involved in the regulation of eye movements to endure the stability of the image during head movement, and play a critical role in plasticity of the vestibulo-ocular reflex (VOR) during the juvenile period. We
Hadir Mahmoud et al.
Molecular brain, 13(1), 31-31 (2020-03-07)
NMDA receptors are heteromeric complexes that contribute to excitatory synaptic transmission and plasticity. The presence of specific variants of GluN2 subunits in these complexes enables diversity in NMDA receptor function and regulation. At brain synapses, there is a switch from
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