GTS-21
GTS-21 structure
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Common Name | GTS-21 | ||
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| CAS Number | 156223-05-1 | Molecular Weight | 381.30 | |
| Density | 1.1±0.1 g/cm3 | Boiling Point | 485.6±45.0 °C at 760 mmHg | |
| Molecular Formula | C19H22Cl2N2O2 | Melting Point | 216-217℃ (decomposition) | |
| MSDS | USA | Flash Point | 247.5±28.7 °C | |
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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 receptor (a7nAChR) signaling. Inflammatory bowel disease (IBD) p... |
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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, including the partial agonists, DMXBA and A-582941, as well ... |
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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 actions of nicotine in the CNS, but it is unclear, whether th... |
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The nicotinic α7 receptor agonist GTS-21 improves cognitive performance in ketamine impaired rhesus monkeys.
Neuropharmacology 64 , 191-6, (2013) 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 mo... |
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Functional magnetic resonance imaging of effects of a nicotinic agonist in schizophrenia.
Biol. Psychiatry 35(4) , 938-42, (2010) 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 phas... |
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Nicotinic acetylcholine receptor agonists attenuate septic acute kidney injury in mice by suppressing inflammation and proteasome activity.
PLoS ONE 7(5) , e35361, (2012) Sepsis is one of the leading causes of acute kidney injury (AKI). Septic patients who develop acute kidney injury (AKI) are at increased risk of death. To date there is no effective treatment for AKI or septic AKI. Based on their anti-inflammatory properties,... |
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The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21).
Behav. Brain Res. 113(1-2) , 169-81, (2000) A large decrease in brain nicotinic receptor levels occurs in Alzheimer's disease, relative to muscarinic and other receptors. Neurons possessing high affinity nicotinic receptors seem particularly vulnerable. The low affinity nicotinic receptors which select... |
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Cardiopulmonary arrest and resuscitation disrupts cholinergic anti-inflammatory processes: a role for cholinergic α7 nicotinic receptors.
J. Neurosci. 31(9) , 3446-52, (2011) Cardiac arrest is a leading cause of death worldwide. While survival rates following sudden cardiac arrest remain relatively low, recent advancements in patient care have begun to increase the proportion of individuals who survive cardiac arrest. However, man... |
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Cholinergic agonists regulate JAK2/STAT3 signaling to suppress endothelial cell activation.
Am. J. Physiol. Cell Physiol. 297(5) , C1294-306, (2009) The cholinergic anti-inflammatory pathway is a physiological mechanism that inhibits cytokine production and minimizes tissue injury during inflammation. Previous investigations revealed that cholinergic stimulation (via cholinergic agonists and vagus nerve s... |
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Intrathecal injection of an alpha seven nicotinic acetylcholine receptor agonist attenuates gp120-induced mechanical allodynia and spinal pro-inflammatory cytokine profiles in rats.
Brain. Behav. Immun. 24(6) , 959-67, (2010) Nicotinic acetylcholine receptors (nAchRs) are not only key receptors in the autonomic nervous system, but also are present on immune cells. The alpha seven subunit of nAchR (alpha7nAchR) suppresses pro-inflammation in peripheral monocytes by decreasing pro-i... |