Fenobam

Product Description

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.

Solubility

Preparing Stock Solutions for Fenobam

The following data is based on the product molecular weight 266.69

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.75 mL	18.75 mL	37.50 mL
5 mM	0.75 mL	3.75 mL	7.50 mL
10 mM	0.37 mL	1.87 mL	3.75 mL
50 mM	0.07 mL	0.37 mL	0.75 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Liu Orthosteric and allosteric action of the C5a receptor antagonists Nature Structural & Molecular Biology 2018 PMID: 29867214
• Kufahl Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine F1000Res. 2013 PMID: 24358885
• Montana 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. 2009 PMID: 19515968
• Porter Description of a clinically validated anxiolytic with mGlu5 antagonist properties. Neuropharmacology
• Porter Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J.Pharmacol.Exp.Ther. 2005 PMID: 16040814