| Bioactivity | Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease[1][1][2]. | ||||||||||||
| Invitro | Mavoglurant (1 nM-10 μM; 10 min) fully antagonizes hmGluR5-mediated responses with IC50s of 110 and 30 nM in Ca2+- and PI-turnover assays in L(tk-) cells stably expressing mGluR5a[1].Mavoglurant (0.01 nM-10 μM) displaces the binding of the allosteric binding ligand [3H]-AAE327 in a concentration-dependent manner in rat brain membranes, with an IC50 of 47 nM[1]. | ||||||||||||
| In Vivo | Mavoglurant (0.1-10 mg/kg; a single p.o.) inhibits the stress-induced hyperthermia (SIH) in a dose-dependent manner in mice[1].Mavoglurant (9.4 mg/kg; a single p.o.) exhibits moderate oral bioavailability (32%), terminal half-life (2.9 h) and Cmax (plasma; brain) (950 pmol/mL; 3500 pmol/g)[1].Mavoglurant (3.1 mg/kg; a single i.v.) exhibits terminal half-life (0.69 h), Cmax (plasma; brain) (3330 pmol/mL; 8400 pmol/g) and Tmax (≤0.08 h)[1]. Animal Model: | ||||||||||||
| Name | Mavoglurant | ||||||||||||
| CAS | 543906-09-8 | ||||||||||||
| Formula | C19H23NO3 | ||||||||||||
| Molar Mass | 313.39 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. [2]. Jacquemont AS, et, al. Epigenetic modification of the FMR1 gene in fragile X syndrome is associated with differential response to the mGluR5 antagonist AFQ056. Sci Transl Med. 2011 Jan 5;3(64):64ra1. [3]. Petrov D, et, al. Mavoglurant as a treatment for Parkinson's disease. Expert Opin Investig Drugs. 2014 Aug;23(8):1165-79. |
Mavoglurant
CAS: 543906-09-8 F: C19H23NO3 W: 313.39
Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM.
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