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CAS No.: 543906-09-8

Mavoglurant Catalog No. CSN13469

Synonyms: AFQ056

Mavoglurant is a structurally non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5.

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靶点选择性

生物活性

实验方案

技术信息

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

更多
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1909 mL
- 15.9545 mL
- 31.9090 mL
- 5 mM
- 0.6382 mL
- 3.1909 mL
- 6.3818 mL
- 10 mM
- 0.3191 mL
- 1.5955 mL
- 3.1909 mL

技术信息

CAS号

543906-09-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H23NO3

运输

蓝冰

分子量

313.39

别名

AFQ056

溶解度

DMSO	47.0 mg/mL (150.0 mM)

动物实验配方

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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 ... more >> Novartis Investigative Site Nuernberg, Germany Collapse <<
NCT00718341	Fragile X Syndrome	Phase 2	Completed	-	France ... more >> Novartis Investigator Site Bron cedex, France, 69677 Italy Novartis Investigator Site Rome, Italy, 00168 Switzerland Novartis Investigator Site Lausanne, Switzerland, 1011 Collapse <<
NCT01442259	Mild Moderate ... more >> or Severe Renal Impairment Collapse <<	Phase 1	Completed	-	Germany ... more >> Novartis Investigative Site Kiel, Germany Collapse <<
NCT00986414	Parkinson Disease ... more >> Dyskinesias Collapse <<	Phase 2	Completed	-	-
NCT01092065	Parkinson's Disease	Phase 2	Completed	-	United States, California ... more >> The Parkinsons Institute Sunnyvale, California, United States, 94085 United States, Colorado Colorado Neurological Institute Englewood, Colorado, United States, 80113 United States, Indiana Indiana University School of Medicine Indianapolis, Indiana, United States, 46202 United States, Kansas University of Kansas Medical Center - Parkinson's Disease and Movement Disorders Center Kansas City, Kansas, United States, 66160 Collapse <<
NCT03341715	Familial Alcoholism Vulnerabil... more >>ity Collapse <<	Early Phase 1	Not yet recruiting	November 30, 2018	United States, Connecticut ... more >> Hartford Hospital Not yet recruiting Hartford, Connecticut, United States, 06102 Contact: Godfrey D Pearlson, MD 203-737-3416 Godfrey.Pearlson@hhchealth.org Principal Investigator: Godfrey D Pearlson, MD Collapse <<
NCT00414856	Gastroesophageal Reflux Diseas... more >>e Collapse <<	Phase 1	Completed	-	Belgium ... more >> Novartis Investigative site Brussels, Belgium France Novartis Investigative site Paris, France Germany Novartis Investigative Site Nuernberg, Germany Switzerland Novartis Investigative site Bern, Switzerland Collapse <<
NCT01482143	Fragile X Syndrome	Phase 1	Completed	-	United States, California ... more >> Novartis Investigative Site Sacramento, California, United States, 95817 United States, Illinois Novartis Investigative Site Chicago, Illinois, United States, 60612 United States, Tennessee Novartis Investigative Site Nashville, Tennessee, United States, 37232-7548 Spain Novartis Investigative Site Sant Cugat, Catalunya, Spain, 08190 Collapse <<
NCT00582673	Parkinson's Disease	Phase 2	Completed	-	Germany ... more >> Novartis Investigator Site Dresden, Germany Novartis Investigator Site Kassel, Germany Novartis Investigator Site Leun, Germany Novartis Investigator Site Marburg, Germany Novartis Investigator Site Tuebingen, Germany Collapse <<
NCT01357239	Fragile X Syndrome	Phase 2	Completed	-	-
NCT01357239	-	-	Completed	-	-
NCT01385592	Dyskinesias P... more >>arkinson Disease Movement Disorders Parkinsonian Disorders Collapse <<	Phase 2	Completed	-	United States, California ... more >> Novartis Investigative Site Sunnyvale, California, United States, 94089 United States, Colorado Novartis Investigative Site Englewood, Colorado, United States, 80113 Canada, Ontario Novartis Investigative Site London, Ontario, Canada, N6A 4G5 Canada, Quebec Novartis Investigative Site Gatineau, Quebec, Canada, J9J 0A5 France Novartis Investigative Site Clermont-Ferrand Cedex 1, France, 63003 Novartis Investigative Site Lille Cedex, France, 59037 Novartis Investigative Site Pessac, France, 33604 Novartis Investigative Site Poitiers, France, 86021 Germany Novartis Investigative Site Beelitz-Heilstaetten, Germany, 14547 Novartis Investigative Site Berlin, Germany, 12163 Novartis Investigative Site Bochum, Germany, 44791 Novartis Investigative Site Duesseldorf, Germany, 40225 Novartis Investigative Site Kassel, Germany, 34128 Novartis Investigative Site Leipzig, Germany, 04103 Novartis Investigative Site Muenchen, Germany, 80804 Novartis Investigative Site München, Germany, 81675 Novartis Investigative Site Stadtroda, Germany, 07646 Novartis Investigative Site Westerstede/Oldenburg, Germany, 26655 Hungary Novartis Investigative Site Budapest, Hungary, 1085 Novartis Investigative Site Kaposvár, Hungary, 7400 Novartis Investigative Site Szeged, Hungary, H-6725 Italy Novartis Investigative Site Bolzano, BZ, Italy, 39100 Novartis Investigative Site Pisa, PI, Italy, 56126 Novartis Investigative Site Roma, RM, Italy, 00163 Spain Novartis Investigative Site Sant Cugat, Barcelona, Spain, 08190 Novartis Investigative Site Barcelona, Cataluña, Spain, 08036 Novartis Investigative Site Madrid, Spain, 28006 Novartis Investigative Site San Sebastian, Spain, 20014 Collapse <<
NCT00888004	Parkinson's Disease ... more >> L-dopa Induced Dyskinesia Collapse <<	Phase 2	Completed	-	Germany ... more >> Novartis Investigative Site Dresden, Germany Novartis Investigative Site Kassel, Germany Novartis Investigative Site Leun-Biskirchen, Germany Novartis Investigative Site Marburg, Germany Novartis Investigative Site Tubingen, Germany Collapse <<
NCT01173731	Parkinson Disease ... more >> Dyskinesia, Drug-Induced Levodopa Collapse <<	Phase 2	Completed	-	United States, California ... more >> Novartis Investigative Site Sunnyvale, California, United States, 94089 United States, Colorado Novartis Investigative Site Englewood, Colorado, United States, 80113 United States, Indiana Novartis Investigative Site Indianapolis, Indiana, United States, 46202 Australia, Victoria Novartis Investigative Site Heidelberg, Victoria, Australia, 3081 Novartis Investigative Site Parkville, Victoria, Australia, 3050 Novartis Investigative Site Prahran, Victoria, Australia, 3181 Canada, Ontario Novartis Investigative Site Ottawa, Ontario, Canada, K1G 4G3 Canada, Quebec Novartis Investigative Site Gatineau, Quebec, Canada, J9J 0A5 Novartis Investigative Site Greenfield Park, Quebec, Canada, J4V 2J2 France Novartis Investigative Site Clermont-Ferrand Cedex 1, France, 63003 Novartis Investigative Site Lille Cedex, France, 59037 Novartis Investigative Site Pessac, France, 33604 Germany Novartis Investigative Site Bochum, Germany, 44791 Novartis Investigative Site Dresden, Germany, 01307 Novartis Investigative Site Kassel, Germany, 34128 Novartis Investigative Site Marburg, Germany, 35039 Novartis Investigative Site Muenchen, Germany, 80804 Novartis Investigative Site Stadtroda, Germany, 07646 Novartis Investigative Site Tuebingen, Germany, 72076 Italy Novartis Investigative Site Lido di Camaiore, LU, Italy, 55041 Novartis Investigative Site Roma, RM, Italy, 00163 Novartis Investigative Site Napoli, Italy, 80131 Collapse <<
NCT01019473	Huntington's Disease ... more >> Chorea Collapse <<	Phase 2	Terminated	-	Germany ... more >> Novartis Investigator Site Berlin, Germany Novartis Investigator Site Bochum, Germany Novartis Investigator Site Munster, Germany Novartis Investigator Site Taufkirchen, Germany Novartis Investigator Site Tubingen, Germany Novartis Investigator Site Ulm, Germany United Kingdom Novartis Investigator Site Birmingham, United Kingdom Novartis Investigator Site Cardiff, United Kingdom Novartis Investigator Site Manchester, United Kingdom Novartis Investigator Site Oxford, United Kingdom Collapse <<
NCT03242928	Cocaine-related Disorder	Phase 2	Recruiting	January 8, 2020	Argentina ... more >> Novartis Investigative Site Recruiting Buenos Aires, Argentina, 1058 Novartis Investigative Site Recruiting Buenos Aires, Argentina, 4634 Novartis Investigative Site Recruiting Buenos Aires, Argentina, C1405B0A Spain Novartis Investigative Site Recruiting San Juan de Alicante, Alicante, Spain, 03550 Novartis Investigative Site Recruiting Barcelona, Catalunya, Spain, 08003 Novartis Investigative Site Recruiting Barcelona, Spain, 08036 Switzerland Novartis Investigative Site Recruiting Basel, Switzerland, 4025 Novartis Investigative Site Recruiting Zuerich, Switzerland, 8001 Collapse <<
NCT01348087	-	-	Terminated(Study treatment AFQ... more >>056 failed to demonstrate efficacy in the adult patient with Fragile X Syndrome in 2 other clinical studies (CAFQ056B2214 and CAFQ056A2212)) Collapse <<	-	-
NCT01253629	Fragile X Syndrome	Phase 2	Completed	-	-
NCT01433354	Fragile X Syndrome	Phase 2 Phase 3	Terminated(The study treatment... more >> failed to demonstrate efficacy in target population in two other clinical studies (CAFQ056B2214 and CAFQ056A2212).) Collapse <<	-	-
NCT01456663	Hepatic Impairment	Phase 1	Completed	-	United States, Florida ... more >> Novartis Investigative Site Orlando, Florida, United States, 32809 Germany Novartis Investigative Site Berlin, Germany, 10117 Hungary Novartis Investigative Site Balatonfured, Hungary, 8230 Collapse <<
NCT01491529	Dyskinesias P... more >>arkinson Disease Movement Disorders Parkinsonian Disorders Anti-Dyskinesia Agents Collapse <<	Phase 2	Completed	-	-
NCT01348087	Fragile X Syndrome	Phase 2	Terminated(Study treatment AFQ... more >>056 failed to demonstrate efficacy in the adult patient with Fragile X Syndrome in 2 other clinical studies (CAFQ056B2214 and CAFQ056A2212)) Collapse <<	-	-
NCT01433354	-	-	Terminated(The study treatment... more >> failed to demonstrate efficacy in target population in two other clinical studies (CAFQ056B2214 and CAFQ056A2212).) Collapse <<	-	-
NCT01813019	-	-	Terminated(Study was premature... more >>ly terminated at the time of the first Interim Analysis (IA) as the study did not meet its primary efficacy objective.) Collapse <<	-	-
NCT02920892	Fragile X Syndrome	Phase 2	Recruiting	July 1, 2020	United States, California ... more >> Univeristy of California - Davis Recruiting Davis, California, United States, 95817 Contact: Erika Bickel 916-703-0281 esbickel@ucdavis.edu Principal Investigator: Randi Hagerman, MD United States, Colorado Children's Hospital of Colorado Recruiting Denver, Colorado, United States, 80045 Contact: Nanastasia Welnick 720-777-8606 Nanastasia.Welnick@childrenscolorado.org Contact: Gina Vanderveen 7207775514 Gina.VanderVeen@childrenscolorado.org Principal Investigator: Nicole Tartaglia, MD United States, District of Columbia Children's National Medical Center Recruiting Washington, District of Columbia, United States, 20010 Contact: Grace Tom 202-476-6551 gtom@childrensnational.org Principal Investigator: Andrea Gropman, MD United States, Georgia Emory University Not yet recruiting Atlanta, Georgia, United States, 30033 Contact: Jean Luan McColl 404-778-8619 Principal Investigator: Amy Talboy, MD United States, Illinois Rush University Medical Center Recruiting Chicago, Illinois, United States, 60612 Contact: Katherine Friedmann, RN 312-942-9841 Contact: Anna DeSonia 312-942-7250 Anna_M_DeSonia@rush.edu United States, Massachusetts Boston Children's Hospital Recruiting Boston, Massachusetts, United States, 02115 Contact: Kate Pawlowski 857-218-5472 neuronext@childrens.harvard.edu Principal Investigator: Lisa Prock, MD, MPH United States, Missouri St Louis Children's Hospital (Washington University School of Medicine) Recruiting Saint Louis, Missouri, United States, 63110 Contact: Kathleen Black 314-362-7166 black290@wustl.edu Contact: Mangesha Teshome 314-77-8420 teshomem@wustl.edu Principal Investigator: Bryan McGill, MD, PhD United States, New York Columbia University - New York Presbyterian Recruiting New York, New York, United States, 10605 Contact: Elizabeth Aaron 914-997-5242 ea2781@cumc.columbia.edu Principal Investigator: Jeremy Veenstra-VanderWeele, MD United States, Ohio Cincinnati Children's Hospital Medical Center Recruiting Cincinnati, Ohio, United States, 45229 Contact: Nicole McCoy 513-636-0526 nicole.mccoy@cchmc.org, Contact: Hilary Rosselot 513-636-4134 hilary.rosselot@cchmc.org Principal Investigator: Craig Erickson, MD Nationwide Children's Hospital Recruiting Columbus, Ohio, United States, 43205 Contact: Rachel Heffern 614-722-4684 rachel.heffern@nationwidechildrens.org Principal Investigator: Lenora Lehwald, MD United States, Pennsylvania Children's Hospital of Pittsburgh Recruiting Pittsburgh, Pennsylvania, United States, 15213 Contact: Christine Amity 412-383-7549 amitycl@upmc.edu Principal Investigator: Robin Filipink, MD United States, Tennessee Vanderbilt University Medical Center Recruiting Nashville, Tennessee, United States, 37232 Contact: Rebecca Kaiser 615-343-4590 Rebecca.kaiser@vanderbilt.edu Principal Investigator: Angela Maxwell-Horn, MD United States, Texas Children's Health - Children's Medical Center (UTSW) Not yet recruiting Dallas, Texas, United States, 75390 Contact: Deanna Meyer 214-648-2926 Deanna.Myer@UTSouthwestern.edu Principal Investigator: Sailaja Golla, MBBS Collapse <<
NCT01491932	Dyskinesias P... more >>arkinson Disease Movement Disorders Parkinsonian Disorders Anti-Dyskinesia Agents Collapse <<	Phase 2	Completed	-	-
NCT03327792	Alcohol Drinking	Phase 1	Recruiting	June 7, 2019	United States, Connecticut ... more >> CMHC, Substance Abuse Center Recruiting New Haven, Connecticut, United States, 06519 Contact: Dana A Cavallo, Ph.D. 203-974-7607 dana.cavallo@yale.edu Contact: Nick Franco 2039747607 nicholas.franco@yale.edu Principal Investigator: Suchitra Krishnan-Sarin, Ph.D. Collapse <<
NCT01813019	Patient Diagnosed With OCD and... more >> Resistant to SSRI Treatment Failed SSRI Over 12 Weeks at Appropriate Doses Collapse <<	Phase 2	Terminated(Study was premature... more >>ly terminated at the time of the first Interim Analysis (IA) as the study did not meet its primary efficacy objective.) Collapse <<	-	United States, California ... more >> Novartis Investigative Site San Diego, California, United States, 92103 United States, Massachusetts Novartis Investigative Site Watertown, Massachusetts, United States, 02472 United States, New York Novartis Investigative Site Brooklyn, New York, United States, 11229 Bulgaria Novartis Investigative Site Burgas, Bulgaria, 8000 Novartis Investigative Site Pazardzhik, Bulgaria, 4400 Novartis Investigative Site Sofia, Bulgaria, 1431 Novartis Investigative Site Sofia, Bulgaria, 1632 Novartis Investigative Site Varna, Bulgaria, 9020 Czech Republic Novartis Investigative Site Strakonice, Czech Republic, 386 29 Germany Novartis Investigative Site Berlin, Germany, 10117 Novartis Investigative Site Freiburg, Germany, 79106 Novartis Investigative Site Muenchen, Germany, 80336 Novartis Investigative Site Nürnberg, Germany, 90419 Novartis Investigative Site Ulm, Germany, 89081 Switzerland Novartis Investigative Site Bern, Switzerland, 3010 Collapse <<

Mavoglurant Catalog No. CSN13469

靶点选择性

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