Biological Activity
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). Anticonvulsant in vivo following systemic administration. Also available as part of the NMDA Receptor - Glycine Site Tocriset™.
Licensing Information
Sold with the permission of Novartis Pharma AG
Technical Data
| 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 | O=C2C(NC1=CC(Br)=CC(CN[C@@H]([P@](O)(O)=O)C)=C1N2)=O.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 2.2eq. NaOH | 41.46 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 414.58. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
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) Antagonistm of N-methyl-D-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition. J.Pharmacol.Exp.Ther. 282 326 PMID: 9223571
Keywords: CGP 78608 hydrochloride, supplier, Potent, selective, glycine-site, NMDA, antagonists, Glutamate, Receptors, N-Methyl-D-Aspartate, iGlur, Ionotropic, CGP78608, hydrochloride, PAMQX, NMDA, Receptors, NMDA, Receptors, Tocris Bioscience
