GRN-529 is a highly potent, selective, orally active mGluR5 negative allosteric modulator with Ki of 5.4 nM, IC50 of 3.1 nM.
GRN-529 displays >1,000-fold selective vs mGluR1.
GRN-529 reduces repetitive behaviors and rescues social deficits in mouse models of autism, demonstrates dose-dependent efficacy across a therapeutically relevant battery of animal models, comprising depression, anxiety and pain, with no effect on rat sexual behavior or motor co-ordination.
