Mavoglurant

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]. Mavoglurant is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. In Vitro: 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 C_max (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), C_max (plasma; brain) (3330 pmol/mL; 8400 pmol/g) and T_max (≤0.08 h)^[1].