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

Description:	Potent and selective NMDA antagonist; acts at glycine site
Alternative Names:	PAMQX
Chemical Name:	[(1S)-1-[[(7-Bromo-1,2,3,4-tetrahydro-2,3-dioxo-5-quinoxalinyl)methyl]amino]ethyl]phosphonic acid hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	414.58

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.

Licensing Information

Sold with the permission of Novartis Pharma AG

Technical Data for CGP 78608 hydrochloride

M. Wt	414.58
Formula	C₁₁H₁₃BrN₃O₅P.HCl
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	1135278-54-4
PubChem ID	24978530
InChi Key	MZQQZBPMRPDKTB-JEDNCBNOSA-N
Smiles	C[C@H](P(O)(O)=O)NCC1=C2NC(C(NC2=CC(Br)=C1)=O)=O.Cl

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

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	2.2eq. NaOH	41.46	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for CGP 78608 hydrochloride

References are publications that support the biological activity of the 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