An NMDA receptor antagonist
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Gavestinel (sodium salt)

Item No. 32845

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4,6-dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propen-1-yl]-1H-indole-2-carboxylic acid, monosodium salt
CAS Number
153436-38-5
Synonyms
  • GV150526A
Molecular Formula
C18H11Cl2N2O3 • Na
Formula Weight
397.2
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
O=C(NC1=CC=CC=C1)/C=C/C2=C(C([O-])=O)NC3=CC(Cl)=CC(Cl)=C23.[Na+]
InChi Code
InChI=1S/C18H12Cl2N2O3.Na/c19-10-8-13(20)16-12(17(18(24)25)22-14(16)9-10)6-7-15(23)21-11-4-2-1-3-5-11;/h1-9,22H,(H,21,23)(H,24,25);/q;+1/p-1/b7-6+;
InChi Key
GRSDSTMFQHAESM-UHDJGPCESA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $41

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    5 mg

    $119

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    10 mg

    $196

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    Product Description

    Gavestinel is an NMDA receptor antagonist.1,2 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.3 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.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Di Fabio, R., Capelli, A.M., Conti, N., et al. Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site. J. Med. Chem. 40(6), 841-850 (1997).

    2. Donati, D., and Di Fabio, R. Synthesis and pharmacological properties of novel glycine antagonists. Pharm. Acta Helv. 74(2-3), 239-245 (2000).

    3. Tomasini, M.C., Antonelli, T., Trist, D.G., et al. Protective effect of GV150526A on the glutamate-induced changes in basal and electrically-stimulated cytosolic Ca++ in primary cultured cerebral cortical cells. Neurochem. Int. 32(4), 345-351 (1998).

    4. Bordi, F., Pietra, C., Ziviani, L., et al. The glycine antagonist GV150526 protects somatosensory evoked potentials and reduces the infarct area in the MCAo model of focal ischemia in the rat. Exp. Neurol. 145(2 Pt 1), 425-433 (1997).