Selective, potent mGlu5 receptor antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM at rat and human recombinant mGlu5 receptors, respectively). Displays inverse agonist properties and blocks mGlu5 receptor basal activity (IC50 = 84 nM). Orally active, atypical anxiolytic.
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in DMSO to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Wållberg A et al. Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues. Bioorg Med Chem Lett16:1142-5 (2006).
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Porter RH et al. Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J Pharmacol Exp Ther315:711-21 (2005).
Read more (PubMed: 16040814) »