Potent, selective and non-competitive mGlu5 receptor antagonist. Acts at allosteric modulatory site (Kd values are 54 and 31 nM at rat and human mGlu5 receptors respectively). Shows inverse agonist properties on receptor basal activity (IC50 value = 84 nM). Displays analgesic, anxiolytic and antidepressant effects. Orally active.
Solubility & Handling
Storage instructions
Room temperature
Solubility overview
Soluble in DMSO (100mM)
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
References are publications that support the biological activity of the product
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 MC et al (2009) J Pharmacol Exp Ther 330(3) : 834-43.
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.
Porter RH et al (2005) J Pharmacol Exp Ther 315(2) : 711-21.