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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
NS(C1=CC2=C(NC(C3=CC=CC4=C3C=CC=C4)C5C2C=CC5)C=C1)(=O)=O
InChI
1S/C22H20N2O2S/c23-27(25,26)15-11-12-21-20(13-15)17-8-4-10-19(17)22(24-21)18-9-3-6-14-5-1-2-7-16(14)18/h1-9,11-13,17,19,22,24H,10H2,(H2,23,25,26)
InChI 密鑰
SIZWDJIHABLBSP-UHFFFAOYSA-N
生化/生理作用
TQS is a type-II positive allosteric modulator of α7 nAChR. TQS potentiates agonist-invoked responses, and dramatically reduces the rate of desensitization of α7 nAChR. The compound has no agonist activity alone. The EC50 for potentiation of submaximal doses of acetylcholine is 6.2µM.
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
The Journal of pharmacology and experimental therapeutics, 367(2), 203-214 (2018-08-17)
Chronic pain and inflammatory diseases can be regulated by complex mechanisms involving α7 nicotinic acetylcholine receptors (nAChRs), making this subtype a promising drug target for anti-inflammatory therapies. Recent evidence suggests that suchtreatment of inflammatory pain may rely on metabotropic-like rather
Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site.
Proceedings of the National Academy of Sciences of the United States of America, 108(14), 5867-5872 (2011-03-26)
Conventional nicotinic acetylcholine receptor (nAChR) agonists, such as acetylcholine, act at an extracellular "orthosteric" binding site located at the interface between two adjacent subunits. Here, we present evidence of potent activation of α7 nAChRs via an allosteric transmembrane site. Previous
Molecular pharmacology, 72(3), 715-724 (2007-06-15)
Selective modulation of alpha7 nicotinic acetylcholine receptors (nAChRs) is thought to regulate processes impaired in schizophrenia, Alzheimer's disease, and other dementias. One approach to target alpha7 nAChRs is by positive allosteric modulation. Structurally diverse compounds, including PNU-120596, 4-naphthalene-1-yl-3a,4,5,9b-tetrahydro-3-H-cyclopenta[c]quinoline-8-sulfonic acid amide
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