Biological Activity Non-competitive NMDA receptor antagonist that acts at the polyamine modulatory site. Selective for GluN2B (formally NR2B)- over GluN2A (NR2A)- and GluN2C (NR2C)-containing receptors (IC50 values are 1, > 100 and > 100 μM respectively). Also σ1 ligand (Ki = 0.013 μM). Antagonizes neuronal voltage-gated Ca2+ channels and selectively inhibits the rapid component of the delayed rectifier K+ current (IKr). Neuroprotective.
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