Cat. No. 2386
Chemical Name: N-(3-Chlorophenyl)-N'-(4,5-dihydro-1
Biological ActivityPotent and selective non-competitive mGlu5 antagonist that 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Montana et al (2009) 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. J.Pharmacol.Exp.Ther. 330 834. PMID: 19515968.
Porter et al (2005) Description of a clinically validated anxiolytic with mGlu5 antagonist properties. Neuropharmacology 49 (Suppl. 1) 267.
Porter et al (2005) Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J.Pharmacol.Exp.Ther. 315 711. PMID: 16040814.
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Citations are publications that use Tocris products.
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Keywords: Fenobam, supplier, Potent, selective, mGlu5, antagonist, mGluR5, antagonists, Group, I, Receptors, Glutamate, Metabotropic, Tocris Bioscience, Glutamate (Metabotropic) Group I Receptor Antagonist products