An extremely potent, non-competitive antagonist for mGlu receptor subtype 1 (Ki = 0.34 nM; IC50 = 0.55 nM). 400-fold more selective for mGlu1 than for mGlu5 and no interaction with mGlu2, mGlu3, mGlu4, mGlu6, AMPA or NMDA receptors (IC50 >10 µM). Centrally active following systemic administration. Widely used for studying substance abuse, learning and memory, and neural plasticity.
Biochem/physiol Actions
Primary Target mGlu₁
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
Lavreysen, H., et al. 2004. Neuropharmacology.47, 961.
Steckler, T., et al. 2005. Psychopharmacology.179, 198.
Steckler, T., et al. 2005. Behav. Brain. Res.164, 52.
Mabire, D., et al. 2005. J. Med. Chem.48, 2134. Fukunaga, I., et al. 2007. Br. J. Pharmacol.151, 870.
Knopfel, T., et al. 2007. Br. J. Pharmacol.151, 723.
Achat-Mendes, C., et al. 2012. J. Pharmacol. Exp. Ther.343, 214.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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