Xanomeline

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Chemical Structure| 131986-45-3 同义名 : LY-246708
CAS号 : 131986-45-3
货号 : A114713
分子式 : C14H23N3OS
纯度 : 99%
分子量 : 281.42
MDL号 : MFCD00867179
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Xanomeline is a subtype selective muscarinic M 1 receptor agonist and a potential new treatment for Alzheimer's disease. Intraperitoneal administration of xanomeline significantly suppressed serum and splenic TNF levels, alleviated sickness behavior, and increased survival during lethal murine endotoxemia[3]. Moreover, xanomeline is a potent agonist at 5-HT1A and 5-HT1B receptors and an antagonist at 5-HT2 receptor subtypes. Xanomeline induced an increase in cytoplasmic Ca2+ concentration in SH-SY5Y cells expressing recombinant human 5-HT2C receptors[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03697252 Schizophrenia Phase 2 Recruiting November 5, 2019 United States, Arkansas ... 展开 >> Woodland International Research Group, LLC Recruiting Little Rock, Arkansas, United States, 72211 United States, California Synergy East Recruiting Lemon Grove, California, United States, 91945 Collaborative Neuroscience Network, LLC. Recruiting Long Beach, California, United States, 90806 NRC Research Institute Recruiting Orange, California, United States, 92868 Artemis Institute for Clinical Research Recruiting San Diego, California, United States, 92103 United States, Georgia Atlanta Center for Medical Research Recruiting Atlanta, Georgia, United States, 30331 United States, Maryland CBH Health, LLC Recruiting Gaithersburg, Maryland, United States, 20877 United States, New Jersey Hassman Research Institute Recruiting Berlin, New Jersey, United States, 08009 United States, Ohio Midwest Clinical Research Center (and IP Shipment) Recruiting Dayton, Ohio, United States, 45417 United States, Texas Community Clinical Research, Inc. Recruiting Austin, Texas, United States, 78754 InSite Clinical Research, LLC Recruiting DeSoto, Texas, United States, 75115 Pillar Clinical Research, LLC Recruiting Richardson, Texas, United States, 75080 收起 <<
NCT02831231 Schizophrenia Phase 1 Completed - United States, Ohio ... 展开 >> Medpace Cincinnati, Ohio, United States, 45227 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.55mL

0.71mL

0.36mL

17.77mL

3.55mL

1.78mL

35.53mL

7.11mL

3.55mL

参考文献

[1]van Harten PN, Tenback DE. Tardive dyskinesia: clinical presentation and treatment. Int Rev Neurobiol. 2011;98:187-210.

[2]Si W, Zhang X, et al. A novel derivative of xanomeline improves fear cognition in aged mice. Neurosci Lett. 2010 Apr 5;473(2):115-9.

[3]Rosas-Ballina M, Valdés-Ferrer SI, Dancho ME, Ochani M, Katz D, Cheng KF, Olofsson PS, Chavan SS, Al-Abed Y, Tracey KJ, Pavlov VA. Xanomeline suppresses excessive pro-inflammatory cytokine responses through neural signal-mediated pathways and improves survival in lethal inflammation. Brain Behav Immun. 2015 Feb;44:19-27.

[4]Watson J, Brough S, Coldwell MC, Gager T, Ho M, Hunter AJ, Jerman J, Middlemiss DN, Riley GJ, Brown AM. Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors. Br J Pharmacol. 1998 Dec;125(7):1413-20.