Gavestinel
Chemical Name: 4,6-Dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propenyl]-1H-indole-2-carboxylic acid sodium salt
Purity: ≥98%
Biological Activity
Gavestinel is a 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
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
-
Substituted indole-2-carboxylates as in vivo potent antagonists acting at the strychnine-insensitive glycine binding site.
Di Fabio et al.
J.Med.Chem., 1997;40:841 -
Receptor binding characteristics of the novel NMDA receptor glycine site antagonist [3H]GV150526A in rat cerebral cortical membranes.
Mugnaini et al.
Eur.J.Pharmacol., 2000;391:233 -
Pharmacokinetics, metabolism and excretion of the glycine antagonist GV150526A in rat and dog.
Kajbaf et al.
Xenobiotica., 2003;33:415
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