CGP-78608

CGP 78608 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). CGP 78608 has anticonvulsant activities^[1][2]. In Vitro:CGP-78608 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 reduces or abolishes ammonia-dependent cGMP synthesis which is a causative factor of ammonia neurotoxicity^[3]. In Vivo:CGP-78608 displays potent anticonvulsant effects after i.p. administration in the electroshock-induced convulsions assay in mice^[1].