CGP 78608 hydrochloride_product_DataBase

Bioactivity	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].
Invitro	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].
In Vivo	CGP-78608 hydrochloride displays potent anticonvulsant effects after i.p. administration in the electroshock-induced convulsions assay in mice[1].
Name	CGP 78608 hydrochloride
CAS	1135278-54-4
Formula	C11H14BrClN3O5P
Molar Mass	414.58
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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