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RO 25-6981 is a potent and highly selective, activity-dependent antagonist of N-methyl-D-aspartate (NMDA) receptors containing the GluN2B (previously NR2B) subunit. It displays over 5000-fold selectivity for GluN1C/GluN2B over GluN1C/GluN2A subunit combinations, with IC50 values in the low nanomolar range. RO 25-6981 exhibits neuroprotective, anti-convulsant, antidepressant, and anti-inflammatory effects in preclinical models, and is often used in research on neuroprotection, depression, epilepsy, and neuropathic pain. It is not approved for human therapeutic use and is used primarily for research purposes. The compound was developed by F. Hoffmann-La Roche as a tool compound for neuroscience research[1][2][3][4][5][7][8].
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