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Description

A negative allosteric modulator selective for NR2B containing NMDA receptors (IC50 = 1, >100, and >100 µ,M for NR2B, NR2A, and NR2C, respectively). Also a potent ligand for alpha1 receptor (Ki = 0.013 µ,M), one of the two types of unique non-opioid, non-phencyclidine brain alpha receptors. Blocks neuronal voltage-gated Ca2+100, and >100 µ,M for NR2B, NR2A, and NR2C, respectively). Also a potent ligand for ς,1 receptor (Ki = 0.013 µ,M), one of the two types of unique non-opioid, non-phencyclidine brain ς, receptors. Blocks neuronal voltage-gated Ca2+ channels and selectively inhibits the rapid component of the delayed rectifier K+ current (IKr). A neuroprotective agent in acute ischemic stroke. Prolongs the QT interval in EKG.