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 GluN1/3A receptor activation. Used to unmask GluN1/GluN3A excitatory glycine NMDA receptors and to demonstrate that excitatory glycine GluN1/GluN3A NMDARs are functionally expressed in native neurons (at least in the juvenile brain). Also displays anticonvulsant properties.
Solubility & Handling
Solubility overview
Soluble in NaOH(aq) (50mM, gentle warming)
Storage instructions
Room temperature
Storage of solutions
Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions
Stable for ambient temperature shipping. Follow storage instructions on receipt.
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.
![CGP 78608 hydrochloride [1135278-54-4] Chemical Structure](https://cdn.hellobio.com/media/catalog/product//h/b/hb0187.png "CGP 78608 hydrochloride [1135278-54-4]")
Understanding purity and quality - a guide for life scientists
