GluN2B (formally NR2B) selective, competitive antagonist of the NMDA receptor. Blocks NMDA-evoked current in mouse cortical neurons (IC50 = 480 nM); also inhibits NMDA-evoked responses in oocytes expressing GluN2B (formally NR2B), but not GluN2A (formally NR2A), subunits (IC50 ~300 nM). Exhibits neuroprotective properties in vivo and in vitro.

Isomangiferin 是 Uncaira 物种的主要四环羟吲哚生物碱成分，抑制 NMDA 受体，IC50 为 43.2 uM。

CGP 78608 hydrochlorid 是 NMDA 受体甘氨酸结合位点的一种高效选择性拮抗剂，IC50 为 6 nM。CGP 78608 作为 GluN1/GluN3A 介导的甘氨酸电流的增强剂，EC50 值为 26.3 nM。具有抗惊厥活性。