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).
Biochem/physiol Actions
Primary Target GluN2B NMDA Receptor
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Yuan, H., et al. 2015. Neuron.85, 1305. Tahirovic, Y., et al. 2008. J. Med. Chem.51, 5506.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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