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.
Packaging
Packaged under inert gas
Other Notes
Acker, T., et al. 2011. Mol. Pharmacol.80, 782.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
| Quality Level | 100 |
| assay | ≥97% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow-white |
| solubility | DMSO: 10 mg/mL, pale yellow |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | O=C(O)CCC(N1N=C(C2=C(C3=CC=CC=C3)C4=C(NC2=O)C=CC(C)=C4)CC1C5=CC=C(Br)C=C5)=O |
