A potent negative allosteric modulator highly selective for mGluR5 (IC50 = 87nM; Kd = 54nM and 31nM 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, Parkinsons disease, Alzheimers disease, and Down syndrome). A leading therapeutic candidate for treatment of fragile X syndrome.
Molecular Formula:C₁₁H₁₁ClN₄O₂
Primary Target:mGlu5 receptors
Primary Target IC50:87nM
Primary Target Ki:54nM and 31nM at recombinant mGlu5 receptors of rat and human, respectively.
Solubility:DMSO
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
