nr2b-nmda

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。

Ro 25-6981 是一种有效的选择性活性依赖性 NMDA 受体阻滞剂，含有 NR2B 亚基，对克隆受体亚基组合 NR1C NR2B 和 NR1C NR2A 的 IC50 分别为 0.009 和 52 μM。 Ro 25-6981 可用于帕金森病的研究。

Co 101244 hydrochloride (4-Piperidinol, 1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-Methylphenyl)Methyl]-,hydrochloride) 是一种含有 NR2B 的 NMDA 受体拮抗剂。

TCS 46b 是一种具有口服活性的 NR1A NR2B NMDA 受体拮抗剂。

BZAD01 是一种选择性 NMDA NR1A 2B 受体拮抗剂。

Radiprodil (RGH-896) 是一种具有口服活性的、NMDA 受体 NR2B 亚类的选择性拮抗剂。它有用于神经性疼痛和其它慢性疼痛的相关研究潜力。

Ifenprodil tartrate 是典型的非竞争性 NMDA 受体拮抗剂，抑制 GIRK (Kir3)，通过基底 GIRK 活性减少内向电流，有用做脑血管舒张试剂的潜力。它对 NR1A NR2B 受体亲和力是 NR1A NR2A 受体的 400 倍。

NMDA-IN-1是一种 NR2B 选择性 NMDA 拮抗剂，对NMDA 的Ki 值为 0.85 nM，对NR2B Ca2+ influx 的IC50值为 9.7 nM。

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。

Ro 25-6981 Maleate 是一种具有选择性的 NR2B 亚基特异性 NMDA 受体 拮抗剂，具有抗惊厥抗抑郁活性，可用于研究帕金森和癫痫等神经系统疾病。

WMS-1405是ifenprodil的衍生物。作为一种高效的NR2B选择性NMDA受体拮抗剂，WMS-1405展示出了5.4 nM的Ki值。通过中心构建基块合成，WMS-1405由于其基本氮原子与苯基残基之间的特定距离，显示出高NR2B亲和性。WMS-1405具有成为治疗兴奋毒性的NMDA拮抗剂的潜力。

EMD-95885 是一种专门针对含NR2B的NMDA受体的拮抗剂，IC50为3.9 nM，不与NMDA受体的其他位点发生相互作用。

NR2B-containing NMDA receptors antagonist

σ receptor agonist and NR2B subunit-selective NMDA receptor antagonist

BMT-108908 is a Negative Allosteric Modulator. It is selective for the NR2B Subtype of The NMDA Receptor Impair Cognition in Multiple Domains.

Ro 25-6981 HCl is an effective and selective NMDA glutamate receptors containing the NR2B subunit antagonist.

Besonprodil is a drug that acts as an NMDA antagonist and is selective for the NR2B subunit.

CP-283097 is an N-methyl-D-aspartic acid (NMDA) receptor antagonist with NR2B subunit.

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.

NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits remarkable binding affinities, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound finds valuable application in scientific investigations focusing on neuropathic pain and Parkinson’s disease.

Nelonemdaz potassium (also known as Salfaprodil) is a potent NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). This compound exhibits remarkable neuroprotection against cell death induced by both NMDA and free radicals, in addition to its role as a free radical scavenger.

EVT-101, also known as ENS-101, is an experimental medication which originated from Roche and is under development by Evotec AG for the treatment of major depressive disorder. It acts as a selective NMDA receptor subunit 2B (NR2B) antagonist.

Ro 04-5595 is a selective antagonist of NMDA receptors NR2B subunits. Ro 04-5595 had an EC 50 of 186 ± 32 nmol L. Ro 04-5595 was predicted to bind the EVT-101 binding site, not the ifenprodil-binding site. Specific binding, defined with a new NR2B-specific antagonist Ro 04-5595 at 10 microM was fully inhibited by several compounds with the following rank order of affinities--Ro 25-6981 > CP-101,606 > Ro 04-5595 = ifenprodil >> eliprodil > haloperidol > spermine > spermidine > MgCl2 > CaCl2--and partially inhibited by competitive glutamate recognition site antagonists. Complementary high-resolution autoradiographic images using [3H]Ro04-5595 demonstrated strong binding in NR2B receptor-rich regions and low binding in cerebellum where NR2B concentration is low.

CO-101244 Free Base is an NMDA receptor NR2B subunit blocker.