SML4086
NitroSynapsin hydrochloride
≥98% (HPLC)
别名:
(1s,3r,5R,7S)-3-Amino-5,7-diethyladamantan-1-yl nitrate hydrochloride, 3-amino-5,7-diethyl-tricyclo[3.3.1.13,7]decan-1-ol 1-nitrate hydrochloride, NMI 6979 hydrochloride, NMT3 hydrochloride, NitroMemantine hydrochloride, YQW 036 hydrochloride
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所有图片(1)
About This Item
质量水平
方案
≥98% (HPLC)
表单
powder
储存条件
desiccated
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
N[C@]1(C2)C[C@@]3(CC)C[C@]2(O[N+]([O-])=O)C[C@](C1)(CC)C3.Cl
生化/生理作用
Extrasynaptic eNMDAR-selective blocker (over synaptic sNMDAR) with improved efficacy than memantine in cultures and in vivo; potent inhibitor of the SARS-CoV-2 virus entry.
NitroSynapsin is an NMDAR blocker that preferentially targets extrasynaptic over synaptic NMDA receptors (eNMDAR over sNMDAR) via a dual allosteric mechanism of open-channel blockage and NO/redox modulation. NitroSynapsin is significantly more effective than memantine (5 µM) in inhibiting the activation of rat cotical neurons due to NMDA release from co-cultured astrocytes upon stimulation by Aβ1-42 oligomers. When administered in the triple transgenic (3× tg) AD mouse model in vivo (216 mmol/kg bid. ip.), NitroSynapsin, but not memantine, significantly improves the location-novelty recognition. It is a potent inhibitor of the SARS-CoV-2 virus entry that prevents the virus spike protein binding to ACE2 (angiotensin-converting enzyme 2).
NitroSynapsin is an NMDAR blocker that preferentially targets extrasynaptic over synaptic NMDA receptors (eNMDAR over sNMDAR) via a dual allosteric mechanism of open-channel blockage and NO/redox modulation. NitroSynapsin is significantly more effective than memantine (5 µM) in inhibiting the activation of rat cotical neurons due to NMDA release from co-cultured astrocytes upon stimulation by Aβ1-42 oligomers. When administered in the triple transgenic (3× tg) AD mouse model in vivo (216 mmol/kg bid. ip.), NitroSynapsin, but not memantine, significantly improves the location-novelty recognition. It is a potent inhibitor of the SARS-CoV-2 virus entry that prevents the virus spike protein binding to ACE2 (angiotensin-converting enzyme 2).
注意
Hygroscopic
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral - Skin Irrit. 2
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
Shu-Ichi Okamoto et al.
Neurobiology of disease, 127, 390-397 (2019-04-01)
Tuberous sclerosis (TSC) is an autosomal dominant disorder caused by heterozygous mutations in the TSC1 or TSC2 gene. TSC is often associated with neurological, cognitive, and behavioral deficits. TSC patients also express co-morbidity with anxiety and mood disorders. The mechanism
Chang-Ki Oh et al.
Nature chemical biology, 19(3), 275-283 (2022-09-30)
Prevention of infection and propagation of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a high priority in the Coronavirus Disease 2019 (COVID-19) pandemic. Here we describe S-nitrosylation of multiple proteins involved in SARS-CoV-2 infection, including angiotensin-converting enzyme 2 (ACE2)
Maria Talantova et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(27), E2518-E2527 (2013-06-19)
Synaptic loss is the cardinal feature linking neuropathology to cognitive decline in Alzheimer's disease (AD). However, the mechanism of synaptic damage remains incompletely understood. Here, using FRET-based glutamate sensor imaging, we show that amyloid-β peptide (Aβ) engages α7 nicotinic acetylcholine
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