Biochem/physiol Actions

Primary TargetmGlu₁ receptors

General description

A potent, negative allosteric modulator selective for mGlu₁ receptors (IC₅₀ = 6.5 µM). No effect on other mGlu subtype receptors and ionotropic glutamate receptors at concentrations less than 100 µM. Acts by inhibiting an intramolecular interaction between the agonist-bound extracellular domain and the transmembrane domain. Widely used for studies related to peripheral pain and central pain pathways.

Legal Information

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

Other Notes

Luongo L, et al. 2013. Neuropharmacol.66, 317.r>Jin, Y., et al. 2012. Pain Res. Treat.2012, 915706.Tappe-Theodor, A., 2011. Mol Pain.7, 38.r>Litschig, S., et al. 1999. Mol. Pharmacol.55, 453.Annoura, H., et al. 1996. Bioorg. Med. Chem. Lett.6, 763.

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)