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Category: Ion ChannelsarrowLigand-gated Ion ChannelsarrowGlutamate (Ionotropic) ReceptorsarrowNMDA SelectivearrowGlycine SitearrowAntagonists
Cat.No. Product Name
2348 Gavestinel
Alternative name(s): GV 150526A
Price and Availability

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Gavestinel

Other Information:

Sold with the permission of GlaxoSmithKline
Chemical Name: 4,6-Dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propenyl]- 1H-indole-2-carboxylic acid sodium salt

Biological Activity:

Highly potent and selective non-competitive antagonist acting at the strychnine-insensitive glycine binding site of the NMDA receptor-channel complex (Kd = 0.8 nM). Displays > 1000-fold selectivity over NMDA, AMPA and kainate binding sites. Orally bioavailable and active in vivo.

Technical Data:

 Click here for more information on batch specific data
M.Wt: 397.19
Formula: C18H11Cl2N2O3Na
Storage: Desiccate at RT
Solubility: Soluble to 40 mM in DMSO
CAS No: [153436-22-7]

Resources:

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    • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    References:

    Di Fabio et al (1997) Substituted indole-2-carboxylates as in vivo potent antagonists acting at the strychnine-insensitive glycine binding site. J.Med.Chem. 40 841. Mugnaini et al (2000) Receptor binding characteristics of the novel NMDA receptor glycine site antagonist [3H]GV150526A in rat cerebral cortical membranes. Eur.J.Pharmacol. 391 233. Kajbaf et al (2003) Pharmacokinetics, metabolism and excretion of the glycine antagonist GV150526A in rat and dog. Xenobiotica. 33 415.
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    Keywords: Gavestinel, Ligand-gated Ion Channels, Potent & Selective Glycine Site Antagonist. Orally Available & Active In Vivo, GV 150526A, Tocris Bioscience
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