Selective and competitive GluN1 NMDAR receptor antagonist which shows preference for the GluN1 glycine binding site (IC50 = 5 nM). CGP-78608 prevents glycine binding to GluN1 (but not to GluN3) to strongly reduce receptor desensitization, and enhance GluN1/3 receptor activation. Also displays anticonvulsant properties.
Solubility & Handling
Storage instructions
Room temperature
Solubility overview
Soluble in NaOH(aq) (50mM, gentle warming)
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors.
Ametamey SM et al (2000) Bioorg Med Chem Lett 10(1) : 75-8.