同义名 :	AFQ056
	CAS号 :	543906-09-8
	货号 :	A487431
	分子式 :	C19H23NO3
	纯度 :	99%+
	分子量 :	313.39
	MDL号 :	MFCD18633263
	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

Mavoglurant (AFQ056), a selective metabotropic glutamate receptor 5 (mGluR5) inhibitor, was tested for levodopa-induced dyskinesia (LID) in patients with Parkinson's Disease[3]. Negative modulation of mGluR5 activity improves eye gaze behavior and alters sympathetically-driven reactivity to faces in patients with FXS (fragile X syndrome) [4]. Chronic administration of a specific mGluR5 antagonist, Mavoglurant, was able to restore sociability behaviour of Fmr1 knockout mice to levels of wild type littermates[5]. In dogs, mavoglurant reduced the number of TLESRs (Transient lower esophageal sphincter relaxations) after intravenous and oral administration[6].

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
NCT00414752	Smoking Abstinence	Phase 1	Completed	-	Germany ... 展开 >> Novartis Investigative Site Nuernberg, Germany 收起 <<
NCT00718341	Fragile X Syndrome	Phase 2	Completed	-	France ... 展开 >> Novartis Investigator Site Bron cedex, France, 69677 Italy Novartis Investigator Site Rome, Italy, 00168 Switzerland Novartis Investigator Site Lausanne, Switzerland, 1011 收起 <<
NCT01442259	Mild Moderate ... 展开 >> or Severe Renal Impairment 收起 <<	Phase 1	Completed	-	Germany ... 展开 >> Novartis Investigative Site Kiel, Germany 收起 <<

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	3.19mL 0.64mL 0.32mL	15.95mL 3.19mL 1.60mL	31.91mL 6.38mL 3.19mL

参考文献

[1]Kumar R, Hauser RA, et al. Mavoglurant (AFQ056) in combination with increased levodopa dosages in Parkinson's disease patients. Int J Neurosci. 2016;126(1):20-4. [2]Petrov D, Pedros I, et al. Mavoglurant as a treatment for Parkinson's disease. Expert Opin Investig Drugs. 2014 Aug;23(8):1165-79. [3]Negida A, Ghaith HS, Fala SY, Ahmed H, Bahbah EI, Ebada MA, Aziz MAE. Mavoglurant (AFQ056) for the treatment of levodopa-induced dyskinesia in patients with Parkinson's disease: a meta-analysis. Neurol Sci. 2021 Aug;42(8):3135-3143 [4]Hessl D, Harvey D, Sansone S, Crestodina C, Chin J, Joshi R, Hagerman RJ, Berry-Kravis E. Effects of mavoglurant on visual attention and pupil reactivity while viewing photographs of faces in Fragile X Syndrome. PLoS One. 2019 Jan 17;14(1):e0209984 [5]Gantois I, Pop AS, de Esch CE, Buijsen RA, Pooters T, Gomez-Mancilla B, Gasparini F, Oostra BA, D'Hooge R, Willemsen R. Chronic administration of AFQ056/Mavoglurant restores social behaviour in Fmr1 knockout mice. Behav Brain Res. 2013 Feb 15;239:72-9 [6]Rouzade-Dominguez ML, Pezous N, David OJ, Tutuian R, Bruley des Varannes S, Tack J, Malfertheiner P, Allescher HD, Ufer M, Rühl A. The selective metabotropic glutamate receptor 5 antagonist mavoglurant (AFQ056) reduces the incidence of reflux episodes in dogs and patients with moderate to severe gastroesophageal reflux disease. Neurogastroenterol Motil. 2017 Aug;29(8)