SML0326
GTS-21
≥97% (HPLC), α7 Nicotinic Acetylcholine Receptor Agonist, powder
别名:
3-(2,4-Dimethoxybenzylidene)-anabaseine dihydrochloride, DMBX-anabaseine, DMXB, DMXB-A, GTS21
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关于此项目
经验公式（希尔记法）:
C19H20N2O2 · 2HCl
化学文摘社编号:
分子量:
381.30
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
GTS-21, ≥97% (HPLC)
SMILES string
Cl.Cl.COc1ccc(\C=C2/CCCN=C2c3cccnc3)c(OC)c1
InChI
1S/C19H20N2O2.2ClH/c1-22-17-8-7-14(18(12-17)23-2)11-15-5-4-10-21-19(15)16-6-3-9-20-13-16;;/h3,6-9,11-13H,4-5,10H2,1-2H3;2*1H/b15-11+;;
InChI key
BXKYFUGAAFLYJL-BXGYHSFXSA-N
assay
≥97% (HPLC)
form
powder
color
faintly yellow to dark yellow
solubility
H2O: >5 mg/mL
storage temp.
2-8°C
Quality Level
Application
GTS-21 has been used:
- as an α7 nicotinic acetylcholine receptors (nAChR) partial agonist to elucidate its anti-inflammatory effects in mouse macrophages
- to test its protective effect on the renal injury induced by lipopolysaccharide (LPS)
- to test its effect on microvascular inflammation in endotoxemia induced by LPS
Biochem/physiol Actions
GTS-2, a derivative of anisine is an immunomodulatory drug. It is used for treating pancreatitis and septicemia. GTS-2 inhibits the pro-inflammatory cytokines especially the interleukin-6 (IL6) and tumor necrosis factor (TNF) in sepsis and endotoxemia.
GTS-21 is a selective agonist at α-7 nicotinic receptors with anti-inflammatory and cognition enhancing activities. GTS-21 has also been investigated for the treatment of schizophrenia.
GTS-21 is a selective agonist at α-7 nicotinic receptors.
Features and Benefits
This compound is featured on the Acetylcholine Receptors (Nicotinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Bianca Brawek et al.
International journal of molecular sciences, 22(3) (2021-01-28)
Microglia, the innate immune cells of the brain, are commonly perceived as resident macrophages of the central nervous system (CNS). This definition, however, requires further specification, as under healthy homeostatic conditions, neither morphological nor functional properties of microglia mirror those
Ryan E Hibbs et al.
The EMBO journal, 28(19), 3040-3051 (2009-08-22)
The pentameric acetylcholine-binding protein (AChBP) is a soluble surrogate of the ligand binding domain of nicotinic acetylcholine receptors. Agonists bind within a nest of aromatic side chains contributed by loops C and F on opposing faces of each subunit interface.
Caijuan Shi et al.
Journal of molecular modeling, 19(2), 871-878 (2012-10-23)
Nicotinic acetylcholine receptors (nAChRs) are drug targets for neuronal disorders and diseases. Partial agonists for nAChRs are currently being developed as drugs for the treatment of neurological diseases for their relative safety originated from reduced excessive stimulation. In the current
Jason R Tregellas et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 35(4), 938-942 (2009-12-04)
3-(2,4-Dimethoxybenzylidene)-anabaseine (DMXB-A) is a partial agonist at alpha7-nicotinic acetylcholine receptors and is now in early clinical development for treatment of deficits in neurocognition and sensory gating in schizophrenia. During its initial phase 2 test, functional magnetic resonance imaging (fMRI) studies
Peng Sun et al.
Shock (Augusta, Ga.), 49(6), 698-703 (2017-08-12)
Studies have demonstrated that vagus nerve stimulation (VNS) reduces ischemia/reperfusion injury. In this study, we investigated the protective effects of VNS in a rat model of cardiopulmonary resuscitation (CPR). We further investigated whether the beneficial effects of VNS were dependent
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