glun2a

GNE-0723是一种选择性的NMDAR的阳性变构调节剂，对GluN2A的EC50=21nM，而GluN2C和GluN2D的EC50=6.2~7.4μM，具有可透过血脑屏障（BBB）的优点，可用于改善Dravet综合征（DS）和阿尔茨海默病（AD）。

GluN2A Allosteric modulator 1 (Compound 11) 是一种能够跨越血脑屏障的口服高效且高选择性的GluN2A负变构调节剂。其对GluN2A和GluN2B的IC50分别为0.042 μM和13 μM。此化合物可用于神经系统疾病的研究。

GNE-5729是一种NMDAR 的正向别构调节剂，具有可透过血脑屏障和可口服的优点，对GluN2A，GluN2C和GluN2D的EC50值分别为37 nM，4.7 μM 和9.5 μM，可用于研究神经和精神疾病。

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

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。

GNE-6901 is a selective GluN2A PAM.

GNE-8324 是一种 GluN2A 选择性阳性变构调节剂，选择性地增强抑制性而非兴奋性神经元中 NMDAR 介导的突触反应。GNE-8324 可用于研究神经系统疾病。

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.

(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。

DQP 1105 是一种高效非竞争性NMDA 受体拮抗剂。DQP-1105 抑制含有 GluN2C (IC50:7.0 Μm) 和 GluN2D (IC50:2.7 Μm) 的受体 。 IC50值至少比重组 GluN2B-、GluN2A-、GluA1- 或 GluK2 受体低 50 倍。

MPX-007, a potent NMDA inhibitor, inhibits GluN2A-containing NMDA receptors expressed in HEK cells with IC50s of 27 nM.

GNE-3476 is an NMDA receptor PAM. Ge-3476 has different degrees of activity on different receptors.GNE-3476 has relatively low efficacy on GluN2A, some activity as an AMPAR PAM, and weak activity at GluN2B-containing receptors.

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].

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.

NYX-2925 是一种口服有效的NMDAR 调节剂。NYX-2925 恢复 mPFC 中 GluN2A 和 GluN2B 上活化的Src 和Src 磷酸化位点的水平。NYX-2925 对 CAMKII 没有影响，也没有任何成瘾或镇静 共济失调的副作用。NYX-2925 可用于多种 NMDA 受体介导的中枢神经系统疾病的研究。

TP-050 是一种口服有效的选择性 NMDAR 激动剂，抑制 GluN2A 和 GluN2D 的 EC50值分别为 0.51 μM 和 9.6 µM。TP-050 可穿过血脑屏障 (BBB)。TP-050 诱导海马区的长期增益效应 (LTP)，增强神经元信号传输。

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