glun1/glun2a

(RS)-(Tetrazol-5-yl)glycine (LY 285265) 是一种高效且选择性的 N-甲基-D-天冬氨酸 (NMDA) 受体激动剂。它能够诱导小鼠癫痫发作反应和 Fos。它对 GluN1 GluN2D 和 GluN1 GluN2A 的EC50分别为 99 nM，1.7 μM。

TCN 213 是一种可克服的(surmountable)、甘氨酸依赖的 GluN1 GluN2A NMDAR 选择性拮抗剂，当甘氨酸的含量为75、 750、7500 nM 时，IC50s 值分别为 0.55、3.5、40 μM。它可用于在药理学上监测 NMDAR 表达在发育中的皮层神经元中的转换。

UBP608 is an allosteric modulator of NMDA receptor family. It selectively inhibits GluN1 GluN2A receptors with a 23-fold selectivity compared to GluN1 GluN2D receptors.

PEAQX, also known as NVP-AAM077; is a competitive antagonist at the NMDA receptor. Although originally described as 100-fold selective for GluN1 GluN2A receptors vs. GluN1 GluN2B receptors, more detailed studies of the Ki of PEAQX revealed it only shows a 5 fold difference in affinity for GluN1 GluN2A vs. GluN1 GluN2B receptors. It is also a potent anticonvulsant in animal tests.

NAB-14 is a powerful and selective chemical compound that acts as a non-competitive antagonist for GluN2C and GluN2D receptors. With an IC50 value of 580 nM for GluN1 GluN2D, NAB-14 demonstrates high potency. This compound exhibits a remarkable selectivity of more than 800-fold towards recombinant GluN2C and GluN2D when compared to GluN2A and GluN2B. Furthermore, NAB-14 possesses the ability to penetrate the blood-brain-barrier effectively [1].

TCN 201 是选择性的、有效的，非竞争性的GluN1 GluN2A NMDA 受体拮抗剂，pIC50值为 6.8。与 GluN1 GluN2B NMDA 受体 (pIC50<4.3) 相比，它对 GluN1 GluN2A NMDA 受体具有选择性。

(3S,6R)-NML 是一种 NMDA 受体拮抗剂，pIC50值为 4.8 (GluN1-GluN2A)、4.6 (GluN1-GluN2B)、5.0 (GluN1-GluN2C) 和 5.0 (GluN1-GluN2D)。(3S,6R)-NML 适用于抑郁症的研究。