CGP 78608 hydrochloride
Cat. No. 1493
Alternative Name: PAMQX
Chemical Name: [(1S)-1-[[(7-Bromo-1,2,3,4-tetrahyd
Biological ActivityPotent 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 InformationSold with the permission of Novartis Pharma AG
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
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.
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.
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.
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