SML0326
GTS-21
≥97% (HPLC), α7 Nicotinic Acetylcholine Receptor Agonist, powder
Synonym(s):
3-(2,4-Dimethoxybenzylidene)-anabaseine dihydrochloride, DMBX-anabaseine, DMXB, DMXB-A, GTS21
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About This Item
Empirical Formula (Hill Notation):
C19H20N2O2 · 2HCl
CAS Number:
Molecular Weight:
381.30
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Product Name
GTS-21, ≥97% (HPLC)
Quality Level
assay
≥97% (HPLC)
form
powder
color
faintly yellow to dark yellow
solubility
H2O: >5 mg/mL
storage temp.
2-8°C
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
Related Categories
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Mauricio Rosas-Ballina et al.
Molecular medicine (Cambridge, Mass.), 15(7-8), 195-202 (2009-07-14)
The cholinergic antiinflammatory pathway modulates inflammatory cytokine production through a mechanism dependent on the vagus nerve and the alpha7 subunit of the nicotinic acetylcholine receptor. GTS-21 [3-(2,4-dimethoxybenzylidene) anabaseine], a selective alpha7 agonist, inhibits inflammatory cytokine production in murine and human
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
M Kox et al.
British journal of anaesthesia, 107(4), 559-566 (2011-07-21)
Mechanical ventilation (MV) induces an inflammatory response that can lead to lung injury. The vagus nerve can limit the inflammatory response through the cholinergic anti-inflammatory pathway. We evaluated the effects of stimulation of the cholinergic anti-inflammatory pathway with the selective
Christopher E Cannon et al.
Neuropharmacology, 64, 191-196 (2012-06-05)
The cognitive deficits associated with schizophrenia are recognized as a core component of the disorder, yet there remain no available therapeutics to treat these symptoms of the disease. As a result, there is a need for establishing predictive preclinical models
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
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