CGP 78608 hydrochloride

The Uses of CGP 78608 hydrochloride

CGP 78608 is a potent and selective NMDA antagonist.

Definition

ChEBI: CGP 78608 is a phosphonic acid in which the hydrogen attached to phosphorous is substituted by a 1-{[(7-bromo-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)methyl]amino}ethyl group. 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 muM respectively). Anticonvulsant in vivo following systemic administration. It has a role as a NMDA receptor antagonist and an anticonvulsant. It is a quinoxaline derivative, an organobromine compound, a secondary amino compound and a member of phosphonic acids. It contains a CGP 78608(1+).

Biological Activity

Potent and selective NMDA antagonist that acts through the glycine site (IC 50 = 5 nM). Displays > 500-fold selectivity over kainate and AMPA receptors (IC 50 values are 2.7 and 3 μ M respectively). Anticonvulsant in vivo following systemic administration. Also available as part of the NMDA Receptor - Glycine Site Tocriset™ .