"目录号: HY-15257 ee.: 99.90%
GPCR/G Protein-
Mavoglurant是一种结构新颖的非竞争性mGlu5受体拮抗剂，IC50为30 nM。
mGluR
相关产品
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
NCT01456663
Novartis Pharmaceuticals-Novartis
Hepatic Impairment
May 2011
Phase 1
NCT01491932
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders-Anti-Dyskinesia Agents
March 2012
Phase 2
NCT01433354
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
November 2011
Phase 2-Phase 3
NCT01348087
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
August 2011
Phase 2
NCT01019473
Novartis Pharmaceuticals-Novartis
Huntington's Disease-Chorea
November 2009
Phase 2
NCT01813019
Novartis Pharmaceuticals-Novartis
Patient Diagnosed With OCD and Resistant to SSRI Treatment-Failed SSRI Over 12 Weeks at Appropriate Doses
November 2013
Phase 2
NCT01491529
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders-Anti-Dyskinesia Agents
April 2012
Phase 2
NCT01385592
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders
November 2011
Phase 2
NCT02920892
Elizabeth Berry-Kravis-National Institute of Neurological Disorders and Stroke (NINDS)-Rush University Medical Center
Fragile X Syndrome
June 5, 2017
Phase 2
NCT00888004
Novartis
Parkinson's Disease-L-dopa Induced Dyskinesia
March 2009
Phase 2
NCT01173731
Novartis Pharmaceuticals-Novartis
Parkinson Disease-Dyskinesia, Drug-Induced-Levodopa
October 2010
Phase 2
NCT00582673
Novartis
Parkinson's Disease
October 2007
Phase 2
NCT01357239
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
May 2011
Phase 2
NCT01253629
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
November 2010
Phase 2
NCT00414856
Novartis
Gastroesophageal Reflux Disease
August 2006
Phase 1
NCT01482143
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
March 2012
Phase 1
NCT01442259
Novartis Pharmaceuticals-Novartis
Mild Moderate-or Severe Renal Impairment
January 2011
Phase 1
NCT01092065
Novartis
Parkinson's Disease
March 2010
Phase 2
NCT00986414
Novartis
Parkinson Disease-Dyskinesias
September 2009
Phase 2
NCT01456663
Novartis Pharmaceuticals-Novartis
Hepatic Impairment
May 2011
Phase 1
NCT01491932
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders-Anti-Dyskinesia Agents
March 2012
Phase 2
NCT01433354
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
November 2011
Phase 2-Phase 3
NCT01348087
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
August 2011
Phase 2
NCT01019473
Novartis Pharmaceuticals-Novartis
Huntington's Disease-Chorea
November 2009
Phase 2
NCT01813019
Novartis Pharmaceuticals-Novartis
Patient Diagnosed With OCD and Resistant to SSRI Treatment-Failed SSRI Over 12 Weeks at Appropriate Doses
November 2013
Phase 2
NCT01491529
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders-Anti-Dyskinesia Agents
April 2012
Phase 2
NCT01385592
Novartis Pharmaceuticals-Novartis
Dyskinesias-Parkinson Disease-Movement Disorders-Parkinsonian Disorders
November 2011
Phase 2
NCT02920892
Elizabeth Berry-Kravis-National Institute of Neurological Disorders and Stroke (NINDS)-Rush University Medical Center
Fragile X Syndrome
June 5, 2017
Phase 2
NCT00888004
Novartis
Parkinson's Disease-L-dopa Induced Dyskinesia
March 2009
Phase 2
NCT01173731
Novartis Pharmaceuticals-Novartis
Parkinson Disease-Dyskinesia, Drug-Induced-Levodopa
October 2010
Phase 2
NCT00582673
Novartis
Parkinson's Disease
October 2007
Phase 2
NCT01357239
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
May 2011
Phase 2
NCT01253629
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
November 2010
Phase 2
NCT00414856
Novartis
Gastroesophageal Reflux Disease
August 2006
Phase 1
NCT01482143
Novartis Pharmaceuticals-Novartis
Fragile X Syndrome
March 2012
Phase 1
NCT01442259
Novartis Pharmaceuticals-Novartis
Mild Moderate-or Severe Renal Impairment
January 2011
Phase 1
NCT01092065
Novartis
Parkinson's Disease
March 2010
Phase 2
NCT00986414
Novartis
Parkinson Disease-Dyskinesias
September 2009
Phase 2
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References
[1].Vranesic I, et al. AFQ056/mavoglurant, a novel clinically effective mGluR5 antagonist: identification, SAR and pharmacological characterization. Bioorg Med Chem. 2014 Nov 1;22(21):5790-5803.