GluN2B NMDA Receptor Antagonist, 93-31

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).

Primary Target
GluN2B NMDA Receptor

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

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

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

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