mavoglurant

Names

[ Name ]:
mavoglurant

[Synonym ]:
Methyl (3aR,4S,7aR)-4-hydroxy-4-[(3-methylphenyl)ethynyl]octahydro-1H-indole-1-carboxylate
AFQ-056
1H-Indole-1-carboxylic acid,octahydro-4-hydroxy-4-(2-(3-methylphenyl)ethynyl)-,methyl ester,(3aR,4S,7aR)
UNII-GT0I9SV4F6
Mavoglurant [INN]
mavoglurant
1H-Indole-1-carboxylic acid, octahydro-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]-, methyl ester, (3aR,4S,7aR)-
AFQ056

Biological Activity

[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]

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> mGluR

Research Areas >> Neurological Disease

[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.

[Related Small Molecules]

L-Glutamine | CTEP (RO4956371) | LY 354740 | L-(+)Sodium glutamate | ADX-88178 | MPEP (Hydrochloride) | FITM | (S)-MCPG | Basimglurant | LY341495 | Dipraglurant | JNJ-40411813 | LY404039 | JNJ 16259685 | ADX-47273

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
476.3±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₂₃NO₃

[ Molecular Weight ]:
313.391

[ Flash Point ]:
241.8±28.7 °C

[ Exact Mass ]:
313.167786

[ PSA ]:
49.77000

[ LogP ]:
3.51

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.602

[ Storage condition ]:
2-8℃

Related Compounds

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