nmda-in-1

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。

3-MATIDA 是一种有效的 mGluR-1 拮抗剂（IC50：6.3 μM，大鼠 mGluR-1a）。显示出 ≥ 40 倍于其他受体的选择性：mGluR-5、mGluR-2、mGluR-4 (mGluR-4a) (IC50 > 300 μM)、NMDA 和 GluR (AMPA) (IC50 = 250 μM)。 3-MATIDA 在体外培养的鼠皮质细胞和大鼠海马切片培养物中充当神经保护剂。

Neboglamine hydrochloride (CR-2249 hydrochloride) 是一种具有口服活性的 NMDA 受体正向调节剂，具有神经保护活性，可增强认知，可用于研究精神分裂症和红斑狼疮。

D-Cycloserine (RO-1-9213) 是一种抗生素，靶向细菌细胞壁肽聚糖生物合成酶。它是一种NMDA 部分激动剂，可以改善认知功能，可研究耐多药结核病。

Linalool (Linalol) 是存在芫荽等植物中的单萜类天然产物，是竞争性NMDA 受体拮抗剂，具有抗肿瘤和抗心脏毒性的作用。它通过激活 Nrf2 诱导抗氧化防御和通过抑制 NF-κB 减少炎症反应来保护其免受 LPS GalN 诱导的肝损伤，具有镇痛、抗菌和抗炎的特性。

Methyl eugenol (4-allylveratrole) 是一种苯丙类化合物，存在于植物叶子、果实、根茎中，当植物相应的部位因食草动物进食而受损时，就会释放。它可用于消灭雄性东方果蝇。

1-Aminocyclopropane-1-carboxylic acid (ACC) 是内源性代谢产物的一种。

Ebselen (CCG-39161) 是一种谷胱甘肽过氧化物酶模拟物，是电压依赖性钙通道阻断剂。它抑制Mpro 和COVID-19病毒，是HIV-1衣壳 CTD 二聚化的抑制剂，具有抗炎、抗癌和抗氧化活性。

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。

DPQ 是PARP-1的有效抑制剂，可用于研究神经保护。DPQ 可降低 N-甲基-D-天冬氨酸(NMDA) 诱导的 PARP 激活，将 ATP 恢复至接近正常水平，并且显著减轻 NMDA 暴露模型中的神经元损伤。

Dextromethorphan 是一种非竞争性 NMDA 受体拮抗剂和 sigma-1激动剂，于 1958 年获得 FDA 批准用作止咳药。

Tat-NR2B9c (NA-1) 是一种突触后密度-95（PSD-95）抑制剂，具有神经保护和抗癫痫作用。Tat-NR2B9c 可抑制PSD-95d2、 PSD-95d1 和 PSD-95，可阻止NMDA诱导的神经元NADPH氧化酶的激活，从而阻断超氧化物的产生，可减少中风后急性期的缺血性损伤。

HINT1-IN-1（化合物 8）是针对组氨酸三联核苷酸结合蛋白 1 (HINT1) 的抑制剂，其Ki值为1.14 μM。该化合物影响μ-阿片受体 (MOR) 和 NMDA 受体 (NMDAR) 之间的相互调节。HINT1-IN-1 可以在小鼠模型中增强吗啡的镇痛效果，不引起阿片类耐受性，并且具有独立的镇痛作用。

DL-AP7 是一种竞争性NMDA 拮抗剂和抗惊厥剂。DL-AP7 阻断 NMDA 诱导的惊厥,并导致小鼠在被动回避任务中的学习表现受损。

Ensaculin is a NMDA antagonist and a 5HT1A agonist potentially for the treatment of Alzheimer's disease (AD). Ensaculin showed memory-enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. It e

Saikosaponin A 是银柴胡中的主要活性成分，有抗炎活性，可上调 LXRα的表达。

Psychotridine is an alkaloid that has been found inP. forsterianaand has diverse biological activities.1,2,3It inhibits ADP-, collagen-, or thrombin-induced aggregation of washed isolated human platelets with IC50values of 1.4, 1.4, and 3.9 μM, respectively.1Psychotridine (2.5 or 5 μM) is cytotoxic to HTC rat hepatocellular carcinoma cells.2It reduces paw licking induced by capsaicin in mice when administered at doses of 0.5, 2.5, or 5 mg kg.3 1.Beretz, A., Roth-Georger, A., Corre, G., et al.Polyindolinic alkaloids from Psychotria forsteriana. Potent inhibitors of the aggregation of human plateletsPlanta Med.51(4)300-303(1985) 2.Roth, A., Kuballa, B., Bounthanh, C., et al.Cytotoxic activity of polyindoline alkaloids of Psychotria forsteriana (Rubiaceae) (1)Planta Med.6450-453(1986) 3.Amador, T.A., Verotta, L., Nunes, D.S., et al.Involvement of NMDA receptors in the analgesic properties of psychotridinePhytomedicine8(3)202-206(2001)

Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988). Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4 References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988).

(Rac)-Lanicemine ((Rac)-AZD6765) 是 Lanicemine 的外消旋体。Lanicemine (AZD6765) 是一种低捕获的NMDA 受体拮抗剂，Ki 为 0.56-2.1 μM；在CHO 和非洲爪蟾卵母细胞中，IC50分别为 4-7 μM 和 6.4 μM。Lanicemine 具有抗抑郁作用。

NMDA receptor antagonist 4 (IIc) 是一个非竞争性、电压依赖的、口服活性的 NMDAR 阻断剂，IC50值为1.93 μM。NMDA receptor antagonist 4 可透过血脑屏障，可用于研究阿兹海默症。

NMDA-IN-2 (化合物 6b) 是普鲁卡因的衍生物。NMDA-IN-2是 NMDA 受体2B 亚型的抑制剂。

Procyclidine (Tricyclamol; (±)-Procyclidine) 是一种抗胆碱能剂。它是一种毒蕈碱受体 (muscarinic receptor) 拮抗剂，也是 N-甲基-D-天冬氨酸 (NMDA) 拮抗剂。Procyclidine 可用于帕金森症和相关精神疾病的研究，如Soman 诱发的癫痫。

NMDA receptor modulator 3 (Compound 99) 是一种用于神经障碍研究的，NMDA 受体的调节剂。

NMDA receptor antagonist 5 (Compound 10e), a potent and non-toxic NMDA receptor antagonist, exhibits brain permeability. It is of significance in studying neurological disorders [1].