CGP 78608 hydrochloride

Key Product Details

Product Description

CGP 78608 hydrochloride is a potent and selective NMDA antagonist that acts through the glycine site (IC₅₀ = 5 nM). Displays > 500-fold selectivity over kainate and AMPA receptors (IC₅₀ values are 2.7 and 3 μM respectively). Also potentiates GluN1/GluN3A-mediated glycine currents (EC₅₀ = 26.3 nM). Anticonvulsant in vivo following systemic administration.

Licensing Information

Sold with the permission of Novartis Pharma AG

Product Specifications for CGP 78608 hydrochloride

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for CGP 78608 hydrochloride

The following data is based on the product molecular weight 414.58.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.41 mL	12.06 mL	24.12 mL
5 mM	0.48 mL	2.41 mL	4.82 mL
10 mM	0.24 mL	1.21 mL	2.41 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 6 publications citing the usage of this product.

• Grand Unmasking GluN1/GluN3A excitatory glycine NMDA receptors. Nat.Commun. 2018 PMID: 30425244
• Whittemore Antagonism of N-MthD.-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition. J.Pharmacol.Exp.Ther. 1997 PMID: 9223571
• Auberson N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists. Bioorg.Med.Chem.Lett. 1999 PMID: 10021939
• John Synthesis and characterisation of [¹²⁵I]-N-(N-benzylpiperidin-4-yl)-4-iodobenzamide, a new σ receptor radiopharmaceutical: high affinity binding to MCF-7 breast tumor cells. J.Med.Chem. 1994 PMID: 8021913
• Ametamey Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)l-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors. Bioorg.Med.Chem.Lett. 2000 PMID: 10636248

Product Documents for CGP 78608 hydrochloride