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GTS-21二盐酸盐(DMBX-A)

GTS-21二盐酸盐(DMBX-A)用途

GTS-21二盐酸盐是一种选择性α7烟碱型乙酰胆碱受体 (α7nAChR) 激动剂。

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GTS-21二盐酸盐(DMBX-A)名称

[ CAS 号 ]:
156223-05-1

[ 中文名 ]:
(1:2),(3E)-3-[(2,4-二甲氧基苯基)亚甲基]-3,4,5,6-四氢-2,3-联吡啶盐酸盐

[ 英文名 ]:
GTS-21

[中文别名 ]:

[英文别名 ]:

3-(2,4-dimethoxybenzylidene)anabaseine
3-(2,4)-DiMethoxybenzylidineanabaseine
GTS-21
DMXB-A
GTS 21 2HCl
GTS-21 (dihydrochloride)

GTS-21二盐酸盐(DMBX-A)生物活性

[ 描述 ]:

GTS-21二盐酸盐是一种选择性α7烟碱型乙酰胆碱受体 (α7nAChR) 激动剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 胆碱受体

信号通路 >> 神经信号通路 >> 胆碱受体

研究领域 >> 炎症/免疫

[参考文献]

[1]. Yue Y, et al. GTS-21 attenuates lipopolysaccharide-induced inflammatory cytokine production in vitro by modulating the Akt and NF-κB signaling pathway through the α7 nicotinic acetylcholine receptor. Int Immunopharmacol. 2015 Dec;29(2):504-12.

[2]. Nullens S, et al. EFFECT OF GTS-21, AN ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR AGONIST, ON CLP-INDUCED INFLAMMATORY, GASTROINTESTINAL MOTILITY, AND COLONIC PERMEABILITY CHANGES IN MICE. Shock. 2016 Apr;45(4):450-9.

[相关活性小分子]

GTS-21二盐酸盐(DMBX-A)物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
485.6±45.0 °C at 760 mmHg

[ 熔点 ]:
216-217℃ (decomposition)

[ 分子式 ]:
C₁₉H₂₂Cl₂N₂O₂

[ 分子量 ]:
381.30

[ 闪点 ]:
247.5±28.7 °C

[ PSA ]:
43.71000

[ LogP ]:
2.64

[ 外观性状 ]:
powder,faint yellow to dark yellow

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.580

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: >5mg/mL

GTS-21二盐酸盐(DMBX-A)安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
DW1764860

[ 海关编码 ]:
2933399090

GTS-21二盐酸盐(DMBX-A)海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

GTS-21二盐酸盐(DMBX-A)文献

Central muscarinic cholinergic activation alters interaction between splenic dendritic cell and CD4+CD25- T cells in experimental colitis.

PLoS ONE 9(10) , e109272, (2014)

The cholinergic anti-inflammatory pathway (CAP) is based on vagus nerve (VN) activity that regulates macrophage and dendritic cell responses in the spleen through alpha-7 nicotinic acetylcholine recep...

Pro-cognitive activity in rats of 3-furan-2-yl-N-p-tolyl-acrylamide, a positive allosteric modulator of the α7 nicotinic acetylcholine receptor.

Br. J. Pharmacol. 172 , 5123-35, (2015)

α7 nicotinic acetylcholine receptors (α7 nAChRs) may represent useful targets for cognitive improvement. The aim of this study is to compare the pro-cognitive activity of selective α7-nAChR ligands, i...

The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS6740 and GTS-21 reduce lipopolysaccharide-induced TNF-α release from microglia.

J. Neuroimmunol. 251(1-2) , 65-72, (2012)

The anti-inflammatory properties of, particularly the α7, nicotinic acetylcholine receptors (nAChRs) in the peripheral immune system are well documented. There are also reports of anti-inflammatory ac...

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