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Submit ReviewCGP 78608 hydrochloride
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)
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.
| 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
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
If you know of a relevant reference for CGP 78608 hydrochloride, please let us know.
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