Zurück zu Ihrem Suchergebnis

Beschreibung

A dihydroquinilone-pyrazoline NMDA antagonist, which is selective for NMDA receptors that are comprised of recombinant subunits GluN1/GluN2C (IC50 = 5.4 microM) and GluN1/GluN2D (2.2 microM) over GluN1/GluN2B (206 microM) 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.