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.
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- CAS No.: 206648-13-7
- Formule: C11H13BrN3O5P
- Masse moléculaire:378.12
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 206648-13-7
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Masse moléculaire 378.12
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Formule C11H13BrN3O5P
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SMILES
C[C@H](P(O)(O)=O)NCC1=CC(Br)=CC(NC2=O)=C1NC2=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CGP-78608 Related Classifications
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