"目錄號(hào): HY-14564A
Membrane Transporter/Ion ChannelNeuronal Signaling-
GTS-21二鹽酸鹽是一種選擇性α7煙堿型乙酰膽堿受體 (α7nAChR) 激動(dòng)劑却舀。
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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
VA Office of Research and Development-University of Colorado, Denver
Schizophrenia
August 2015
Phase 1-Phase 2
University of Colorado, Denver-National Institute of Mental Health (NIMH)
Schizophrenia-Schizoaffective Disorder
July 2011
Phase 2
University of Colorado, Denver
Obesity
November 2015
Phase 1
CoMentis
Alzheimer Disease
November 2006
Phase 2
University of Colorado, Denver
Autism
June 2015
Phase 1
University of Colorado, Denver-National Institute of Mental Health (NIMH)
Schizophrenia-Psychotic Disorders
March 2004
Phase 1
Radboud University-CoMentis
Endotoxemia-Sepsis-Vagal Activity
August 2008
University of Florida
Tobacco Use Disorder
June 29, 2017
Phase 2
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References
