Formulation: A solid
Formal Name: 4,6-dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propen-1-yl]-1H-indole-2-carboxylic acid, monosodium salt
Purity: ≥98%
Formula Markup: C18H11Cl2N2O3 • Na
Formula Weight: 397,2
Shelf life (days): 1460
CAS Number: 153436-38-5
Notes: Gavestinel is an NMDA receptor antagonist.{60157,60158} It selectively binds to the glycine site of the NMDA receptor over the glutamate binding site of NMDA, AMPA, or ionotropic kainate (GluK) receptors (Kis = 0.003, 10, 7.94, and 3.98 µM, respectively) and is selective for the NMDA receptor over a panel of 70 receptors (IC50s = >10 µM for all). Gavestinel (0.03-0.35 µM) inhibits glutamate-induced increases in intracellular calcium levels in primary rat neonatal cerebral cortical neurons.{60159} It reduces infarct volume in a rat model of focal ischemia induced by middle cerebral artery occlusion (MCAO) when administered intravenously at a dose of 3 mg/kg.{60160}
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