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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 5 mg/mL (clear solution)
儲存溫度
2-8°C
SMILES 字串
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 密鑰
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.
特點和優勢
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.
訊號詞
Warning
危險分類
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
標靶器官
Central nervous system, Respiratory system
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Structural basis for negative allosteric modulation of GluN2A-containing NMDA receptors
Yi F, et al.
Neuron, 91(6), 1316-1329 (2016)
Giacomo Sitzia et al.
Neuropharmacology, 174, 108136-108136 (2020-06-01)
In Parkinson's disease (PD) reduced levels of dopamine (DA) in the striatum lead to an abnormal circuit activity of the basal ganglia and an increased output through the substantia nigra pars reticulata (SNr) and the globus pallidus internal part. Synaptic
Yong-Tao He et al.
European journal of pharmacology, 854, 62-69 (2019-04-06)
Src Homology 2 domain-containing protein tyrosine phosphatase 1 (SHP1) interacts specifically with GluN2A subunit of N-methyl-D-aspartate (NMDA) subtype of glutamate receptors in spinal cord dorsal horn. This molecular interaction is involved in the development of GluN2A-dependent spinal sensitization of nociceptive
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)
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