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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

378.12

C₁₁H₁₃BrN₃O₅P

206648-13-7

C[C@H](P(O)(O)=O)NCC1=CC(Br)=CC(NC2=O)=C1NC2=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

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

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

  [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.  [Content Brief]