CGP 78608 hydrochloride

Pricing Availability   Qty
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)
Datasheet
Citations
Reviews
Literature (6)

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 Data for CGP 78608 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for CGP 78608 hydrochloride

Certificate of Analysis / Product Datasheet
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References for CGP 78608 hydrochloride

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

Ametamey et al (2000) 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. 10 75 PMID: 10636248

Auberson et al (1999) N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists. Bioorg.Med.Chem.Lett. 9 249 PMID: 10021939

John et al (1994) 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. 37 1737 PMID: 8021913

Whittemore et al (1997) Antagonism of N-MthD.-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition. J.Pharmacol.Exp.Ther. 282 326 PMID: 9223571

Grand et al (2018) Unmasking GluN1/GluN3A excitatory glycine NMDA receptors. Nat.Commun. 9 4769 PMID: 30425244


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Citations for CGP 78608 hydrochloride

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Reviews for CGP 78608 hydrochloride

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