Product overview

Name CGP 78608 hydrochloride
Alternative names PAMQX
Purity >98%
Description

Selective, competitive GluN1 NMDAR receptor antagonist. Enhances GluN1/3 activation.

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Biological Data

Biological description

Selective and competitive GluN1 NMDAR receptor antagonist which shows preference for the GluN1 glycine binding site (IC50 = 5 nM). CGP-78608 prevents glycine binding to GluN1 (but not to GluN3) to strongly reduce receptor desensitization, and enhance GluN1/3 receptor activation. Also displays anticonvulsant properties.

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in NaOH(aq) (50mM, gentle warming)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Dilution

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Chemical Data

Purity >98%
Chemical name [(1S)-1-[[(7-Bromo-1,2,3,4-tetrahydro-2,3-dioxo-5-quinoxalinyl)methyl]amino]ethyl]phosphonic acid hydrochloride
Molecular Weight 414.58
Chemical structure CGP 78608 hydrochloride  [1135278-54-4] Chemical Structure
Molecular Formula

C11H13BrN3O5P.HCl

CAS Number 1135278-54-4
PubChem identifier 24978530
SMILES O=C2C(NC1=CC(Br)=CC(CN[C@@H]([P@](O)(O)=O)C)=C1N2)=O.Cl
InChiKey MZQQZBPMRPDKTB-JEDNCBNOSA-N

References for CGP 78608 hydrochloride

References are publications that support the biological activity of the product
  • Allosteric modulation of GluN1/GluN3 NMDA receptors by GluN1-selective competitive antagonists.

    Rouzbeh N et al (2023) The Journal of general physiology 155 :
  • Unmasking GluN1/GluN3A excitatory glycine NMDA receptors.

    Grand T et al (2018) Nature communications 9 : 4769
  • Prolongation of levodopa responses by glycineB antagonists in parkinsonian primates.

    Papa SM et al (2004) Ann Neurol 56(5) : 723-7.
  • Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors.

    Ametamey SM et al (2000) Bioorg Med Chem Lett 10(1) : 75-8.
  • N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists.

    Auberson YP et al (1999) Bioorg Med Chem Lett 9(2) : 249-54.

5 Item(s)