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BMS-986169 is an inhibitor of the glutamate N-methyl-D-aspartate 2B receptor (GluN2B). BMS-986169 has a high binding affinity for the allosteric regulatory site of the GluN2B subunit, with a Ki value of 4.03-6.3 nM. BMS-986169 can inhibit the function of GluN2B receptors in Xenopus oocytes, with an IC50 value of 24.1 nM. BMS-986169 can also inhibit the activity of the hERG channel, with an IC50 value of 28.4 μM. BMS-986169 can be used in research on treatment-resistant depression[1].

[1] Bristow LJ, et al. Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder. J Pharmacol Exp Ther. 2017 Dec;363(3):377-393. DOI:10.1124/jpet.117.242784