Biochem/physiol Actions

Target K_i: 54 nM and 31 nM at recombinant mGlu₅ receptors of rat and human, respectively

Primary TargetmGlu₅ receptors

General description

A potent negative allosteric modulator highly selective for mGluR₅ (IC₅₀ = 87 nM; K_d = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Porter, R., et al. 2005. J. Pharmacol. Exp. Ther.315, 711.r>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.

Packaging

5 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)