| Chemical Properties | Back Directory | [solubility ]
Soluble to 100 mM in 2.2eq. NaOH | [form ]
Powder | [color ]
White to off-white | [SMILES]
BrC1=CC(NC2=O)=C(C(CN[C@@H](P(O)(O)=O)C)=C1)NC2=O.Cl |
| Hazard Information | Back Directory | [Uses]
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 hydrochloride 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]. | [Definition]
ChEBI: CGP 78608 hydrochloride is a hydrochloride that is the monohydrochloride salt of CGP 78608. Potent and selective NMDA antagonist that acts through the glycine site (IC50 = 5 nM). Displays >500-fold selectivity over kainate and AMPA receptors (IC50 values are 2.7 and 3 muM respectively). Anticonvulsant in vivo following systemic administration. It has a role as a prodrug, a NMDA receptor antagonist and an anticonvulsant. It is a conjugate base of a CGP 78608(1+). | [in vivo]
CGP-78608 hydrochloride displays potent anticonvulsant effects after i.p. administration in the electroshock-induced convulsions assay in mice[1]. | [IC 50]
NMDA Receptor | [storage]
Store at RT | [References]
[1] Catarzi D, et al. Competitive Gly/NMDA receptor antagonists. Curr Top Med Chem. 2006;6(8):809-21. DOI:10.2174/156802606777057544
[2] Grand T, et al. Unmasking GluN1/GluN3A excitatory glycine NMDA receptors. Nat Commun. 2018 Nov 13;9(1):4769. DOI:10.1038/s41467-018-07236-4
[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. DOI:10.1016/j.brainres.2004.05.014 |
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MedChemExpress
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www.medchemexpress.com |
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