Fenobam

Biological Activity

Fenobam is a potent 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 K_d values of 54 and 31 nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration in vivo; also exhibits analgesic properties.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Osteosarcoma cell proliferation and survival requires mGluR5 receptor activity and is blocked by Riluzole
   S Liao, Y Ruiz, H Gulzar, Z Yelskaya, L Ait Taouit, M Houssou, T Jaikaran, Y Schvarts, K Kozlitina, U Basu-Roy, A Mansukhani, SS Mahajan
   PLoS ONE, 2017;12(2):e0171256.
2. Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
   Porter et al.
   J.Pharmacol.Exp.Ther., 2005;315:711
3. 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.
   J.Pharmacol.Exp.Ther., 2009;330:834
4. Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine
   Kufahl et al.
   F1000Res., 2013;1:10.12688/f1000resear
5. Orthosteric and allosteric action of the C5a receptor antagonists
   Liu et al.
   Nature Structural & Molecular Biology, 2018;25:472
6. Description of a clinically validated anxiolytic with mGlu5 antagonist properties.
   Porter et al.
   Neuropharmacology, 2005;49:267

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