Drug intelligence / Profile preview

RO 25-6981

Development stage
Preclinical
Lead developer
Roche
Modality
Small Molecules
Administration
Intraperitoneal, Intrathecal (in Preclinical And Research Settings)
01

Overview

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].

Other names
RO 25-6981 maleateRO25-6981 maleateRO-25-6981 maleate
02

Targets

GRIN2B (N-methyl-D-aspartate Receptor Subunit Combination: NR1a/NR2B)

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