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
Warning
Toxicity: Standard Handling (A)
Reconstitution
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
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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