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Category: Ion ChannelsarrowLigand-gated Ion ChannelsarrowGlutamate (Ionotropic) ReceptorsarrowNMDA SelectivearrowGlycine SitearrowAntagonists
Cat.No. Product Name
1493 CGP 78608 hydrochloride
Alternative name(s): PAMQX
Price and Availability

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CGP 78608

Other Information:

Sold with the permission of Novartis Pharma AG
Chemical Name: [(1S)-1-[[(7-Bromo-1,2,3,4-tetrahydro-2,3-dioxo-5-quino xalinyl)methyl]amino]ethyl]phosphonic acid hydrochloride

Biological Activity:

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 μM respectively). Anticonvulsant in vivo following systemic administration.

Technical Data:

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M.Wt: 414.58
Formula: C11H13BrN3O5P.HCl
Storage: Store at RT
Solubility: Soluble to 50 mM in 1eq. NaOH
Purity: >98%
CAS No: [206648-13-7]

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    References:

    Auberson et al (1999) N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists. Bioorg.Med.Chem.Lett. 9 249. Ametamey et al (2000) Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)l-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors. Bioorg.Med.Chem.Lett. 10 75.
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    Keywords: CGP 78608, Ligand-gated Ion Channels, Potent, Selective Glycine-site NMDA Antagonist, PAMQX, CGP78608, Tocris Bioscience
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