CGP 78608 hydrochloride

Modify Date: 2024-01-09 13:48:38

CGP 78608 hydrochloride Structure
CGP 78608 hydrochloride structure
Common Name CGP 78608 hydrochloride
CAS Number 1135278-54-4 Molecular Weight 414.58
Density N/A Boiling Point N/A
Molecular Formula C11H14BrClN3O5P Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name CGP 78608 hydrochloride

 CGP 78608 hydrochloride Biological Activity

Description 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].
Related Catalog
In Vitro 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C11H14BrClN3O5P
Molecular Weight 414.58