Merck, 5.04684, Fenobam

General description
A potent negative allosteric modulator highly selective for mGluR₅ (IC₅₀ = 87 nM; Kd = 54 nM and 31 nM at recombinant mGlu₅ receptors of rat and human, respectively). Biologically active admitted orally or systematically. Frequently used for assessing the functional roles of mGlu₅ receptors in a variety of brain functions (i.e. learning and memory, circadian rhythms, reward and decision making, and locomotion) and disorders (i.e. addition, depression, seizures, anxiety disorder, Parkinson′s disease, Alzheimer′s disease, and Down syndrome). A leading therapeutic candidate for treatment of fragile X syndrome.
Biochem/physiol Actions
Primary Target
mGlu₅ receptors
Target Ki: 54 nM and 31 nM at recombinant mGlu₅ receptors of rat and human, respectively
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Porter, R., et al. 2005. J. Pharmacol. Exp. Ther.315, 711.
Jacob, W., et al. 2009. Neuropharmacology57, 97.
Berry-Kravis, E., et al. 2009. J. Medical Genetics.46, 266.
Watterson, R., et al. 2012. Psychopharmacol.2012, 1.
Simonyi, A., et al. 2010. Eur. J. Pharmacol.639, 17.
Westmark, J., et al. 2010. J. Alzheimer′s Disease20, 1009.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)