CGP 78608 hydrochloride

CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity[1][2].

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

CGP-78608 hydrochloride decreases glycine sensitivity of GluN1/GluN3A receptors through an inter-subunit allosteric effect between GluN1 and GluN3A agonist-binding domain (ABD) sites[2]. CGP 78608 hydrochloride reduces or abolishes ammonia-dependent cGMP synthesis which is a causative factor of ammonia neurotoxicity[3].

CGP-78608 hydrochloride displays potent anticonvulsant effects after i.p. administration in the electroshock-induced convulsions assay in mice[1].

[1]. Catarzi D, et al. Competitive Gly/NMDA receptor antagonists. Curr Top Med Chem. 2006;6(8):809-21.

[2]. Grand T, et al. Unmasking GluN1/GluN3A excitatory glycine NMDA receptors. Nat Commun. 2018 Nov 13;9(1):4769.

[3]. Hilgier W, et al. A novel glycine site-specific N-methyl-D-aspartate receptor antagonist prevents activation of the NMDA/NO/CGMP pathway by ammonia. Brain Res. 2004 Jul 23;1015(1-2):186-8.