Biochem/physiol Actions

Reversible: yes

Primary TargetGluN2B NMDA Receptor

General description

A tertiary N-alkylamine that acts as a pH dependent antagonist of GluN2B-NMDA receptors. Shown to be about 10-fold more potent in ischemic tissue (pH 6.9) than in normal healthy tissue (pH 7.6) (IC₅₀ = 190 nM and 1.8 µM, respectively). Effectively reduces the infarct volume in damaged brain tissue in a murine model of ischemic stroke (at 10 mg/kg, ED₅₀ ≤ 1 mg/kg) without impairing coordination or motor function. Also displays binding to hERG (IC₅₀ = 70 nM) and alpha1-adrenergic receptor (IC₅₀ = 4.9 µM).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Yuan, H., et al. 2015. Neuron.85, 1305.Tahirovic, Y., et al. 2008. J. Med. Chem.51, 5506.

Packaging

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)