AFQ056 (Mavoglurant, AFQ-056) is a potent, subtype-selective and non-competitive inhibitor of mGluR5 with IC50 of 30 nM.
AFQ056 displays >300 fold selectivity for the mGluR5 over other metabotropic family of GPCRs.
AFQ056 antagonizes hmGluR5-mediated responses with IC50s of 110 and 30 nM in Ca2+- and PI-turnover assays in L(tk-) cells stably expressing mGluR5. AFQ056 (Mavoglurant) (0.1-10 mg/kg; a single p.o.) inhibits the stress-induced hyperthermia (SIH) in a dose-dependent manner in mice.
Fmr1 KO mice have a deficit in inhibition of the startle response after a prepulse and that AFQ056 can rescue this phenotype, shows potential for treatment of fragile X syndrome (FXS).
