Chemical Name: N-(3-Chlorophenyl)-N'-(4,5-dihydro-1-methyl-4-oxo-1H-imidazol-2-yl)urea
Biological ActivityPotent and selective non-competitive mGlu5 negative allosteric modulator (NAM) that also displays inverse agonist properties; blocks mGlu5 constitutive activity in vitro (IC50 = 87 nM). Acts at an allosteric modulatory site shared with MPEP and binds the mGlu5 receptor with Kd values of 54 and 31 nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration in vivo; also exhibits analgesic properties.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
Porter et al.
The metabotropic glutamate receptor subtype 5 antagonist fenobam is analgesic and has improved in vivo selectivity compared with the prototypical antagonist 2-methyl-6-(phenylethynyl)-pyridine.
Montana et al.
Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine
Kufahl et al.
Orthosteric and allosteric action of the C5a receptor antagonists
Liu et al.
Nature Structural & Molecular Biology, 2018;25:472
Description of a clinically validated anxiolytic with mGlu5 antagonist properties.
Porter et al.
Citation for Fenobam
The citations listed below are publications that use Tocris products. Selected citations for Fenobam include:
1 Citation: Showing 1 - 1
Metabotropic glutamate receptor 5 (mGluR5) regulates bladder nociception.
Authors: Crock Et al.
Mol Pain 2012;8:20
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