glun2b

Rislenemdaz (CERC-301) (CERC-301)是 N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) 的拮抗剂。

GluN2B receptor modulator-1 is a potent and selective allosteric modulator of the GluN2B receptor. It demonstrates negative modulation, inhibiting receptor activity, and exhibits high selectivity towards the GluN2B subunit, with an impressive IC50 value of 31 nM.

GluN2B-NMDAR antagonist-1 是一种具有口服活性的GluN2B-NMDAR 拮抗剂。GluN2B-NMDAR antagonist-1 具有神经保护活性。 GluN2B-NMDAR antagonist-1 可用于缺血性损伤研究。

TAT-GluN2BCTM 是一种靶向DAPK1的膜透性肽，能够促使活性DAPK1定向降解于溶酶体。该化合物通过降低DAPK1的表达，有助于防护神经元免遭氧化应激和NMDAR-介导的兴奋毒性。TAT-GluN2BCTM常用于神经保护性研究领域。

BMS-986163 is a negative allosteric modulator of GluN2B and the prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).

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。

NR2B-containing NMDA receptors antagonist

NP10679 是一种可口服且具有选择性、脑穿透性、高效性和 pH 敏感性的 GluN2B 亚基的 N-methyl-D-aspartate (NMDA) 受体抑制剂。NP10679 抑制 histamine H1 、 hERG 通道和 CYP 酶，可用于研究癫痫和缺血性卒中。

Ifenprodil (RC61-91) 是 NMDA 受体抑制剂，特别是 GluN1(甘氨酸结合 NMDA 受体亚基 1)和 GluN2B(谷氨酸结合 NMDA 受体亚基 2)亚基的抑制剂。此外，它抑制 GIRK 通道并与 α1 肾上腺素能、血清素和 sigma 受体相互作用。

Lu AF90103 (Compound 42e) 是 compound 42d 的甲酯前药，具有穿过血脑屏障的能力。Compound 42d 作为 GluN1 GluN2B 复合物的部分激动剂，其功效为 24%，EC50 值为 78 nM。Lu AF90103 在研究神经精神疾病中极为重要。

NMDA agonist 1 (compound 42d) 是一种高效的NMDA激动剂，Ki值为96 nM，并作为GluN1 GluN2B复合物的部分激动剂，其EC50值为78 nM。

(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。

BMS-986169 is a GluN2B Receptor Negative Allosteric Modulator. BMS-986169 showed a high binding affinity for the GluN2B subunit allosteric modulatory site (Ki: 4.03-6.3 nM) and selectively inhibited GluN2B receptor function in Xenopus oocytes expressing h

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.

Praeruptorin C 是白花前胡中的一种主要成分，是钙拮抗剂，pD2′值为 5.7。

EVT-101 is a GluN2B antagonist, binding at the same GluN1 GluN2B dimer interface as ifenprodil but adopting a remarkably different binding mode involving a distinct subcavity and receptor interactions.

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。

Withaphysalin D 是一种选择性抑制含GluN2B的N-甲基-D-天冬氨酸受体(NMDAR)的化合物。该物质可从睡莲中提取，对神经保护有益，能穿过血脑屏障。

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。

NMDA receptor antagonist7 (Compound (S)-10a) 为针对 GluN2B 亚基具有选择性的 NMDA 受体拮抗剂，展现出 Ki 值为 93 nM 和 IC50 值为 72 nM。该化合物适用于神经退行性疾病的研究。

NMDA receptor antagonist8 (Compound (R)-10a)为针对GluN2B亚基具有选择性的NMDA受体拮抗剂，拥有Ki值为265 nM及IC50值为62 nM，适用于神经退行性疾病的研究。