CGP 78608 hydrochloride

Name: CGP 78608 hydrochloride
Brand: Tocris Bioscience
SKU: 1493

Tocris Bioscience, part of Bio-Techne | Catalog # 1493

Citations (5)

COA / SDS

Potent and selective NMDA antagonist; acts at glycine site

Key Product Details

Chemical Name:	[(1S)-1-[[(7-Bromo-1,2,3,4-tetrahydro-2,3-dioxo-5-quinoxalinyl)methyl]amino]ethyl]phosphonic acid hydrochloride
Purity:	≥98%
Molecular Weight:	414.58 kDa

View Full Technical Details for CGP 78608 hydrochloride

Technical Data
Citations

Biological Activity for CGP 78608 hydrochloride

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.

Technical Data for CGP 78608 hydrochloride

M. Wt	414.58 kDa
Formula	C₁₁H₁₃BrN₃O₅P.HCl
Storage	Store at RT
Purity	≥98%
CAS Number	1135278-54-4

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for CGP 78608 hydrochloride

Solubility

Soluble Soluble to 100 mM in 2.2eq. NaOH

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References for CGP 78608 hydrochloride

References are publications that support the biological activity of the product.

Whittemore et al. Antagonism of N-MthD.-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition. J.Pharmacol.Exp.Ther., 1997;282:326 PMID: 9223571
Ametamey et al. 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;10:75 PMID: 10636248
Auberson et al. N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists. Bioorg.Med.Chem.Lett., 1999;9:249 PMID: 10021939
John et al. Synthesis and characterisation of [¹²⁵I]-N-(N-benzylpiperidin-4-yl)-4-iodobenzamide, a new sigma receptor radiopharmaceutical: high affinity binding to MCF-7 breast tumor cells. J.Med.Chem., 1994;37:1737 PMID: 8021913
Grand et al. Unmasking GluN1/GluN3A excitatory glycine NMDA receptors. Nat.Commun., 2018;9:4769 PMID: 30425244