"目录号: HY-14564A
Membrane Transporter/Ion ChannelNeuronal Signaling-
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。
nAChR
相关产品
L-Nicotine-PNU-282987-Vinblastine-Carbamoylcholine chloride-PNU-120596-Pancuronium dibromide-Aniracetam-Catharanthine-Varenicline-Hexamethonium Bromide-Vecuronium bromide-Tebanicline hydrochloride-A-867744-Adiphenine hydrochloride-Cisatracurium besylate-
生物活性
Description
GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation. Target: nAChRin vitro: GTS-21 is one of the most potent α7nAChR agonists, has been reported to attenuate pro-inflammatory cytokine production, improve outcomes in sepsis models, pancreatitis, and ischemia-reperfusion injury, and inhibit the production of endotoxin-induced TNF in lung tissue. In addition, recent studies have demonstrated that GTS-21 inhibits the activities of endothelial cells and monocyte macrophages, as well as the secretion of pro-inflammatory cytokines in peripheral blood samples, by regulating the JAK2-STAT3 pathway. [1] in vivo: In septic animals, GTS-21 significantly ameliorated GI motility, lowered systemic and colonic levels of IL-6, decreased colonic permeability, and decreased the number of positive cultures obtained from blood and mesenteric lymph nodes. Splenectomy prevented animals from developing sepsis-induced ileus. Chrna7 mice displayed a more severe septic phenotype, whereas GTS-21 remarkably was also beneficial in these animals. [2]
Clinical Trial
NCT02538081
VA Office of Research and Development-University of Colorado, Denver
Schizophrenia
August 2015
Phase 1-Phase 2
NCT01400477
University of Colorado, Denver-National Institute of Mental Health (NIMH)
Schizophrenia-Schizoaffective Disorder
July 2011
Phase 2
NCT02458313
University of Colorado, Denver
Obesity
November 2015
Phase 1
NCT00414622
CoMentis
Alzheimer Disease
November 2006
Phase 2
NCT02111551
University of Colorado, Denver
Autism
June 2015
Phase 1
NCT00255918
University of Colorado, Denver-National Institute of Mental Health (NIMH)
Schizophrenia-Psychotic Disorders
March 2004
Phase 1
NCT00783068
Radboud University-CoMentis
Endotoxemia-Sepsis-Vagal Activity
August 2008
NCT02432066
University of Florida
Tobacco Use Disorder
June 29, 2017
Phase 2
View MoreCollapse
References
[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.