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31

抑制剂 & 化合物

8

天然产物

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Cat. No. Product Name Target Signaling Pathways
T12234 NMDA-IN-1

NMDAR Neuroscience
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。
T60612 Neboglamine hydrochloride

Neboglamine (CR-2249, XY-2401) hydrochloride 是NMDA 受体甘氨酸位点的正向调节剂,具有口服活性,可用于研究精神分裂症。
TP1179L Porcine dynorphin A(1-13) acetate

Dynorphin A Porcine Fragment 1-13 acetate,Porcine dynorphin A(1-13) acetate(72957-38-1 free base)

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Porcine dynorphin A(1-13) acetate (Dynorphin A Porcine Fragment 1-13 acetate)(72957-38-1 free base) 是一种有效的内源性 κ opioid 受体激动剂,在生理浓度下具有镇痛作用。暴露于强啡肽 A (1-13) 会导致单个神经元中 [Ca2+]i 的急剧增加,类似于急性 NMDA 治疗所见的增加。
T1751 Eliprodil

依利罗地,SL-820715

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
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。
T3486 3-MATIDA

GluR; NMDAR Neuroscience
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。
T0825 Ebselen

SPI-1005,PZ-51,依布硒,CCG-39161

Phosphatase; Virus Protease; Calcium Channel; COX; HIV Protease Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
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。
T60513 NMDA-IN-2

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。
T61470 NMDA receptor antagonist 5

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].
T60685 NMDA receptor modulator 3

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。
T22734 DL-AP7

Others Others
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。
T60695 DPQ

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。
T60306 NMDA receptor antagonist 4

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。
T76358 Neuropeptide Y (1-24) (human)

Neuropeptide Y (1-24) (human) 是一种神经肽,它能够抑制大鼠输精管电刺激引发的抽搐反应,同时在体内刺激 N-methyl-D-aspartate (NMDA) 促使大鼠海马背侧 CA3 区神经元激活。
T60471 Lanicemine dihydrochloride

Lanicemine (AZD6765) dihydrochloride 是NMDA 通道的低捕获拮抗剂,Ki 值为 0.56-2.1 μM,在CHO 和爪蟾卵母细胞的IC50分别为 4-7 μM 和 6.4 μM。Lanicemine (AZD6765) dihydrochloride 具有持续的抗抑郁功效。
T60235 (Rac)-Lanicemine

(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。
T78231 DAO-IN-1

Others Others
DAO-IN-1是高效的D-氨基酸氧化酶(DAO)抑制剂,其IC50值为269 nM。DAO负责d-丝氨酸的代谢,而d-丝氨酸是NMDA受体的共激动剂。
T79375 NMDA receptor antagonist 8

iGluR Membrane transporter/Ion channel; Neuroscience
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。
T27269 Ensaculin HCl

KA 672,KA672,Ensaculin,Anseculin Hydrochloride,KA-672 HCl

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
T74195 4′-Demethylnobiletin

4′-Demethylnobiletin 是一种生物活性代谢物,可以激活PKA/ERK/CREB 信号通路,增强海马神经元中 CRE 介导的转录,并通过刺激ERK 信号逆转与 NMDA 受体拮抗相关的记忆障碍。
T73682 (R)-Lanicemine

(R)-Lanicemine ((R)-AZD6765) 是 Lanicemine 的低活性的 R 型异构体。Lanicemine (AZD6765) 是一种低捕获的NMDA 受体拮抗剂,Ki 为 0.56-2.1 μM。CHO 和爪蟾卵母细胞中,IC50分别为 4-7 μM 和 6.4 μM。具有抗抑郁作用。
T74129 L-Homocysteic acid

L-Homocysteic acid (L-HCA) 是一种内源性兴奋性氨基酸,可作为NMDA 受体激动剂 (EC50: 14 μM)。L-Homocysteic acid 具有神经毒性,可用于神经系统疾病的研究。
T13112 Tat-NR2B9c

Tat-NR2Bct,NA-1

NO Synthase; iGluR Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
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。
T79569 AChE/Aβ-IN-1

AChE/Aβ-IN-1(compound 32)是一种双功能化合物,既表现出高效的AChE抑制活性,IC50值为86 nM,又能作为NMDA受体(GluN1-1b/GluN2B亚基组合)的拮抗剂,其IC50为3.876 μM。此外,它能够抑制Aβ聚集,且表现出优秀的血脑屏障穿透能力和神经保护效果,能在大鼠模型中显著改善认知和空间记忆障碍。
T79857 Risevistinel

NYX-783

iGluR Membrane transporter/Ion channel; Neuroscience
Risevistinel (NYX-783),一种N-甲基-D-天冬氨酸 (NMDA) 受体正变构调节剂,旨在缓解与神经退行性疾病相关的认知功能障碍,包括轻度认知障碍、阿尔茨海默病初期、帕金森病及路易体病等病症。
TP1179 Porcine dynorphin A(1-13)

Dynorphin A Porcine Fragment 1-13

Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations. Exposure to dynorphin A (1-13) causes acute increases in [Ca2+]i in individual neurons similar to increases seen with acut
T60578 Procyclidine

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。
TP1910 CALP1

Cell-permeable calmodulin (CaM) agonist that binds to the EF-hand/Ca2+-binding site; produces CaM-dependent activation of phosphodiesterase. Also binds to cytoplasmic sites on other Ca2+ channels, including NMDA and HIV-1 gp120-activated channels, inhibit
T79611 DQP-26

iGluR Membrane transporter/Ion channel; Neuroscience
DQP-26,作为一种高效的NMDAR负变构调制剂,展现出对GluN2C和GluN2D亚单位具有显著的选择性,其IC50值分别仅为0.77 μM和0.44 μM。该化合物在针对NMDAR相关神经系统疾病的研究中显示出潜在应用价值。
T79571 AChE/Aβ-IN-2

AChE/Aβ-IN-2(compound 32)是一种双重功能性化合物,作为乙酰胆碱酯酶(AChE)的有效口服抑制剂,表现出86 nM的IC50,同时也对NMDA受体(GluN1-1b/GluN2B亚基组合)起拮抗作用,其IC50为3.876 μM。该化合物能够抑制Aβ聚集,具有良好的血脑屏障渗透性,并表现出神经保护效果。在大鼠模型中,AChE/Aβ-IN-2展现出改善认知和空间记忆障碍的潜力。
T36521 Alaproclate (hydrochloride)

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 concentratio...
T36101 Psychotridine

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.Pol...

化合物

NMDA-IN-1
Cat.No: T12234
Synonym:
Target: NMDAR
Neboglamine hydrochloride
Cat.No: T60612
Synonym:
Target:
Porcine dynorphin A(1-13) acetate
Cat.No: TP1179L
Synonym: Dynorphin A Porcine Fragment 1-13 acetate,Porcine dynorphin A(1-13) acetate(72957-38-1 free base)
Target: Opioid Receptor
Eliprodil
Cat.No: T1751
Synonym: 依利罗地,SL-820715
Target: NMDAR, iGluR
3-MATIDA
Cat.No: T3486
Synonym:
Target: GluR, NMDAR
Ebselen
Cat.No: T0825
Synonym: SPI-1005,PZ-51,依布硒,CCG-39161
Target: Phosphatase, Virus Protease, Calcium Channel, COX, HIV Protease
NMDA-IN-2
Cat.No: T60513
Synonym:
Target:
NMDA receptor antagonist 5
Cat.No: T61470
Synonym:
Target:
NMDA receptor modulator 3
Cat.No: T60685
Synonym:
Target:
DL-AP7
Cat.No: T22734
Synonym:
Target: Others
DPQ
Cat.No: T60695
Synonym:
Target:
NMDA receptor antagonist 4
Cat.No: T60306
Synonym:
Target:
Neuropeptide Y (1-24) (human)
Cat.No: T76358
Synonym:
Target:
Lanicemine dihydrochloride
Cat.No: T60471
Synonym:
Target:
(Rac)-Lanicemine
Cat.No: T60235
Synonym:
Target:
DAO-IN-1
Cat.No: T78231
Synonym:
Target: Others
NMDA receptor antagonist 8
Cat.No: T79375
Synonym:
Target: iGluR
Ensaculin HCl
Cat.No: T27269
Synonym: KA 672,KA672,Ensaculin,Anseculin Hydrochloride,KA-672 HCl
Target:
4′-Demethylnobiletin
Cat.No: T74195
Synonym:
Target:
(R)-Lanicemine
Cat.No: T73682
Synonym:
Target:
L-Homocysteic acid
Cat.No: T74129
Synonym:
Target:
Tat-NR2B9c
Cat.No: T13112
Synonym: Tat-NR2Bct,NA-1
Target: NO Synthase, iGluR
AChE/Aβ-IN-1
Cat.No: T79569
Synonym:
Target:
Risevistinel
Cat.No: T79857
Synonym: NYX-783
Target: iGluR
Porcine dynorphin A(1-13)
Cat.No: TP1179
Synonym: Dynorphin A Porcine Fragment 1-13
Target:
Procyclidine
Cat.No: T60578
Synonym:
Target:
CALP1
Cat.No: TP1910
Synonym:
Target:
DQP-26
Cat.No: T79611
Synonym:
Target: iGluR
AChE/Aβ-IN-2
Cat.No: T79571
Synonym:
Target:
Alaproclate (hydrochloride)
Cat.No: T36521
Synonym:
Target:
Psychotridine
Cat.No: T36101
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6S0659 Rhynchophylline

钩藤碱,Rhynchophyllin,Rhyncophylline,Mitrinermine,Mitrinermin

Calcium Channel; NF-κB Membrane transporter/Ion channel; Metabolism; NF-κB
Rhynchophylline (Mitrinermine) 是一种生物碱类化合物,从钩藤中分离得到,具有很高的生物活性,被广泛用于抗炎、神经保护等方面的研究。
T2768 Saikosaponin A

柴胡皂苷A,柴胡皂苷 A

NF-κB; Antibacterial; Liver X Receptor Metabolism; Microbiology/Virology; NF-κB
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。
T6S1418 Praeruptorin C

Antioxidant; Calcium Channel Membrane transporter/Ion channel; Metabolism; oxidation-reduction
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。
T1589 D-Cycloserine

RO-1-9213,D-环丝氨酸

Others; Antibacterial; Antibiotic; iGluR Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Others
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。
T3S2259 Methyl eugenol

4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether,丁香酚甲醚,丁子香酚甲醚

GABA Receptor Membrane transporter/Ion channel; Neuroscience
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。
T2S2264 Linalool

Linalol,(±)-Linalool,Phantol,沉香醇

Apoptosis; IL Receptor; TNF; Endogenous Metabolite; iGluR Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
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。
T75890 Conantokin G TFA

Conantokin G TFA 是一种 17 个氨基酸的肽,是一种有效,选择性和竞争性的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂。Conantokin G TFA 抑制鼠皮质神经元中NMDA 诱发的电流,IC50为 480 nM,具有神经保护作用。
T4752 1-Aminocyclopropane-1-carboxylic acid

1-Aminocyclopropanecarboxylic acid,1-氨基环丙烷羧酸,1-Amino-1-carboxycyclopropane,ACC

Endogenous Metabolite; NMDAR Metabolism; Neuroscience
1-Aminocyclopropane-1-carboxylic acid (ACC) 是内源性代谢产物的一种。

天然产物

Rhynchophylline
Cat.No: T6S0659
Synonym: 钩藤碱,Rhynchophyllin,Rhyncophylline,Mitrinermine,Mitrinermin
Target: Calcium Channel, NF-κB
Saikosaponin A
Cat.No: T2768
Synonym: 柴胡皂苷A,柴胡皂苷 A
Target: NF-κB, Antibacterial, Liver X Receptor
Praeruptorin C
Cat.No: T6S1418
Synonym:
Target: Antioxidant, Calcium Channel
D-Cycloserine
Cat.No: T1589
Synonym: RO-1-9213,D-环丝氨酸
Target: Others, Antibacterial, Antibiotic, iGluR
Methyl eugenol
Cat.No: T3S2259
Synonym: 4-allylveratrole,eugenyl methyl ether,O-methyleugenol,Eugenol Methyl ether,丁香酚甲醚,丁子香酚甲醚
Target: GABA Receptor
Linalool
Cat.No: T2S2264
Synonym: Linalol,(±)-Linalool,Phantol,沉香醇
Target: Apoptosis, IL Receptor, TNF, Endogenous Metabolite, iGluR
Conantokin G TFA
Cat.No: T75890
Synonym:
Target:
1-Aminocyclopropane-1-carboxylic acid
Cat.No: T4752
Synonym: 1-Aminocyclopropanecarboxylic acid,1-氨基环丙烷羧酸,1-Amino-1-carboxycyclopropane,ACC
Target: Endogenous Metabolite, NMDAR
TargetMol Loading
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