Description
Fenobam is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5) that binds to an allosteric site. It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate in HEK293 cells expressing the human receptor (IC
50 = 58 nM) and inhibits basal activity of mGluR5 in a cell-based assay (IC
50 = 84 nM). Fenobam (10 and 30 mg/kg) reduces stress-induced hyperthermia in mice and increases drinking time in the Vogel conflict test in rats when administered at a dose of 30 mg/kg, indicating anxiolytic-like activity. It induces analgesia in the formalin test in mice when administered at a dose of 30 mg/kg.
