CGP 78608 hydrochloride
Chemical Name: [(1S)-1-[[(7-Bromo-1,2,3,4-tetrahydro-2,3-dioxo-5-quinoxalinyl)methyl]amino]ethyl]phosphonic acid hydrochloride
Purity: ≥98%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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Antagonism of N-MthD.-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition.
Whittemore et al.
J.Pharmacol.Exp.Ther., 1997;282:326 -
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.
Ametamey et al.
Bioorg.Med.Chem.Lett., 2000;10:75 -
N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists.
Auberson et al.
Bioorg.Med.Chem.Lett., 1999;9:249 -
Synthesis and characterisation of [125I]-N-(N-benzylpiperidin-4-yl)-4-iodobenzamide, a new sigma receptor radiopharmaceutical: high affinity binding to MCF-7 breast tumor cells.
John et al.
J.Med.Chem., 1994;37:1737 -
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.
John et al.
J.Med.Chem., 1994;37:1737 -
Unmasking GluN1/GluN3A excitatory glycine NMDA receptors.
Grand et al.
Nat.Commun., 2018;9:4769
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