General description

A dihydroquinilone-pyrazoline NMDA antagonist, which is selective for NMDA receptors that are comprised of recombinant subunits GluN1/GluN2C (IC₅₀ = 5.4 µM) and GluN1/GluN2D (2.2 µM) over GluN1/GluN2B (206 µM) and GluN1/ClucN2A (undetectable) in Xenopus oocytes. Similar selectivity is observed in whole-cell HEK patch-clamp assays with IC₅₀ values for GluN2C and GluN2D that are at least 50-fold lower than those for recombinant GluN2A, GluN2B, GluA1, or GluK2-containing receptors. It inhibits NMDA by blocking a conformational change necessary for channel opening and is non-competitive with co-agonists, glutamate and glycine.

Legal Information

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

Other Notes

Acker, T., et al. 2011. Mol. Pharmacol.80, 782.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Warning

Toxicity: Regulatory Review (Z)