Dipraglurant

Dipraglurant is a negative allosteric modulator (NAM) of metabotropic glutamate receptor 5 (mGluR5, Ki = 21 nM). It inhibits glutamate-induced calcium mobilization, inositol monophosphate (IP1) accumulation, and ERK1/2 phosphorylation in HEK293A cells expressing rat mGluR5a (pKBs = 5. 6. and 6. respectively). Dipraglurant increases drinking in the Vogel punished drinking task, indicating anxiolytic-like activity, in rats, decreases marble burying in mice, and reduces immobility time in the forced swim test in mice (ED50s = 7. 43, and ~30 mg/kg, respectively). It reduces chorea and dystonia scores in a macaque model of MPTP-induced Parkinson's disease L-DOPA-induced dyskinesia (PD-LID) when administered at a dose of 30 mg/kg.. Solulibility: DMSO: Soluble: =10 mg/ml: Ethanol: Soluble: =10 mg/ml.