"目錄號: HY-15257 ee.: 99.90%
Mavoglurant是一種結(jié)構(gòu)新穎的非競爭性mGlu5受體拮抗劑喜鼓，IC50為30 nM庄岖。
相關(guān)產(chǎn)品
CTEP-LY341495-LY354740-LY404039-RG7090-MPEP Hydrochloride-Dipraglurant-Topiramate-JNJ-40411813-L-Glutamine-FITM-JNJ16259685-MTEP hydrochloride-(S)-MCPG-ADX-47273-
生物活性
Description
Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5.IC50 value: 30 nMTarget: mGluR5in vitro: Mavoglurant is a selective non-competitive antagonist which showed efficacy in the treatment of L-dopa induced dyskinesias in Parkinson's disease and Fragile X mental retardation in proof of principle studies. Mavoglurant is selective over the other mGluR subtypes, iGluRs and a panel of 238 CNS relevant receptors, transporter or enzymes. [1]In vivo: Mavoglurant shows an improved pharmacokinetic profile in rat and efficacy in the stress-induced hyperthermia test in mice as compared to the prototypic mGluR5 antagonist MPEP.[1]
Clinical Trial
Novartis Pharmaceuticals-Novartis
Hepatic Impairment
May 2011
Phase 1
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders-Anti-Dyskinesia Agents
March 2012
Phase 2
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
November 2011
Phase 2-Phase 3
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
August 2011
Phase 2
Novartis Pharmaceuticals-Novartis
Huntington's Disease-Chorea
November 2009
Phase 2
Novartis Pharmaceuticals-Novartis
Patient Diagnosed With OCD and Resistant to SSRI Treatment-Failed SSRI Over 12 Weeks at Appropriate Doses
November 2013
Phase 2
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders-Anti-Dyskinesia Agents
April 2012
Phase 2
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders
November 2011
Phase 2
Elizabeth Berry-Kravis-National Institute of Neurological Disorders and Stroke (NINDS)-Rush University Medical Center
Fragile X Syndrome
June 5, 2017
Phase 2
Novartis
Parkinson's Disease-L-dopa Induced Dyskinesia
March 2009
Phase 2
Novartis Pharmaceuticals-Novartis
Parkinson Disease-Dyskinesia, Drug-Induced-Levodopa
October 2010
Phase 2
Novartis
Parkinson's Disease
October 2007
Phase 2
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
May 2011
Phase 2
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
November 2010
Phase 2
Novartis
Gastroesophageal Reflux Disease
August 2006
Phase 1
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
March 2012
Phase 1
Novartis Pharmaceuticals-Novartis
Mild Moderate-or Severe Renal Impairment
January 2011
Phase 1
Novartis
Parkinson's Disease
March 2010
Phase 2
Novartis
Parkinson Disease-Dyskinesias
September 2009
Phase 2
Novartis Pharmaceuticals-Novartis
Hepatic Impairment
May 2011
Phase 1
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders-Anti-Dyskinesia Agents
March 2012
Phase 2
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
November 2011
Phase 2-Phase 3
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
August 2011
Phase 2
Novartis Pharmaceuticals-Novartis
Huntington's Disease-Chorea
November 2009
Phase 2
Novartis Pharmaceuticals-Novartis
Patient Diagnosed With OCD and Resistant to SSRI Treatment-Failed SSRI Over 12 Weeks at Appropriate Doses
November 2013
Phase 2
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders-Anti-Dyskinesia Agents
April 2012
Phase 2
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders
November 2011
Phase 2
Elizabeth Berry-Kravis-National Institute of Neurological Disorders and Stroke (NINDS)-Rush University Medical Center
Fragile X Syndrome
June 5, 2017
Phase 2
Novartis
Parkinson's Disease-L-dopa Induced Dyskinesia
March 2009
Phase 2
Novartis Pharmaceuticals-Novartis
Parkinson Disease-Dyskinesia, Drug-Induced-Levodopa
October 2010
Phase 2
Novartis
Parkinson's Disease
October 2007
Phase 2
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
May 2011
Phase 2
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
November 2010
Phase 2
Novartis
Gastroesophageal Reflux Disease
August 2006
Phase 1
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
March 2012
Phase 1
Novartis Pharmaceuticals-Novartis
Mild Moderate-or Severe Renal Impairment
January 2011
Phase 1
Novartis
Parkinson's Disease
March 2010
Phase 2
Novartis
Parkinson Disease-Dyskinesias
September 2009
Phase 2
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References
