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Fenobam is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5) that binds to an allosteric site.1 It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate (Item No. 20211) in HEK293 cells expressing the human receptor (IC50 = 58 nM) and inhibits basal activity of mGluR5 in a cell-based assay (IC50 = 84 nM).1 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.2
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1. Fenobam: A clinically validated nonbenzodiazepine anxiolytic Is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J. Pharmacol. Exp. Ther. 315(2), 711-721 (2005).
2. Metabotropic glutamate receptor 5 antagonism with fenobam: Examination of analgesic tolerance and side effect profile in mice. Anesthesiology 115(6), 1239-1250 (2011).