nr2c

QNZ46 是一种 NR2C/NR2D 选择性 NMDA 受体非竞争性拮抗剂。

CIQ 是亚基选择性NMDA 受体增强剂，可作用于NR2C 或NR2D 亚基。

NMDA agonist 2 (compound 8d) 是一种对NMDA受体的有效抑制剂，其对GluN1/2C的EC50为0.034 μM。NMDA agonist 2 在神经和精神疾病的治疗中具有重要作用。

NMDA receptor potentiator-1 (Compound 1368) 是一种亚基选择性的 NMDA receptor 增强剂。NMDA receptor potentiator-1 对 NR2C 和 NR2D 表达的 IC50 值分别为 4 μM 和 5 μM。

Eliprodil (SL-820715) 是NR2B-NMDA 受体高效选择性抑制剂，IC50值1uM。它对NR2A-和NR2C-NMDA 受体作用较弱，可用于研究帕金森病和运动障碍治疗的试验。

TCN 237 是NR2B亚基NMDA受体的拮抗剂（Ki = 0.85 nM）。它在全细胞膜片钳实验中，选择性地抑制表达NR2B亚基的NMDA受体的L-M(TK-)细胞中谷氨酸和甘氨酸诱导的电流，而对表达NR2A或NR2D亚基的NMDA受体的L-M(TK-)细胞以及表达NR2C亚基的NMDA受体的HEK293细胞影响较小。TCN 237（3 mg/kg）能够抑制大鼠中由卡拉胶引起的机械痛觉过敏。

N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.