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37

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T25196	BZAD01 BZAD-01,BZAD 01	NMDAR	Neuroscience
	BZAD01 是一种选择性 NMDA NR1A/2B 受体拮抗剂。
T22674	Co 101244 hydrochloride Co 101244盐酸盐,4-Piperidinol, 1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-Methylphenyl)Methyl]-,hydrochloride	NMDAR	Neuroscience
	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。
T13112L1	Tat-NR2B9c acetate Tat-NR2B9c acetate (500992-11-0 Free base),NA-1 acetate	Others	Others
	Tat-NR2B9c acetate (NA-1 acetate) 是一种突触后密度 95 (PSD-95) 抑制剂，对 PSD-95d2 (PSD-95 PDZ domain 2) 和 PSD-95d1 的 EC50 值分别为 6.7 nM 和 670 nM。它破坏 PSD-95/NMDAR 相互作用，抑制 NR2A 和 NR2B 与 PSD-95 的结合，IC50 值分别为 0.5 μM 和 8 μM。它还抑制神经元一氧化氮合酶 (nNOS)/PSD-95 相互作用，并具有神经保护功效。
T81037	Tat-HA-NR2B9c
	Tat-HA-NR2B9 是一种包括HIV-1 Tat细胞膜转导结构域片段、流感病毒血凝素(HA)表位标签以及NR2B(NR2B9c) C端9个氨基酸的化学复合物。该化合物能够降低大鼠缺血性脑损伤的梗塞面积，同时促进神经功能的恢复。
T35924	Tat-NR2Baa Tat-NR2Baa
	Tat-NR2BAA is an inactive control peptide of Tat-NR2B9c. It shares a similar sequence with Tat-NR2B9c, but possesses a double-point mutation in the COOH terminal tSXV motif. This mutation renders Tat-NR2BAA unable to bind PSD-95. Tat-NR2B9c, on the other hand, is a membrane-permeable peptide that interferes with PSD-95/NMDAR binding. This interference leads to the decoupling of NR2B- and/or NR2A-type NMDARs from PSD-95[1][2].
T76069	Tat-NR2Baa TFA
	Tat-NR2BAA TFA 是 Tat-NR2B9c 的对照肽 (control peptide)，没有活性。Tat-NR2BAA TFA 的序列与 Tat-NR2B9c 相似，但在 COOH 末端 tSXV 基序中有一个双点突变，这使得它无法结合 PSD-95。Tat-NR2B9c TFA 是一种可通透细胞膜的多肽，破坏 PSD-95/NMDAR 的结合。
T13112L	Tat-NR2B9c TFA NA-1 (TFA)	Others	Others
	Tat-NR2B9c TFA is a 20-aa peptide, and acts as an inhibitor of postsynaptic density-95 (PSD-95)(EC50 of 6.7 nM for PSD-95d2), and possesses neuroprotective efficacy.
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。
T5385	Radiprodil RGH-896	NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	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。
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。
T23449	TCS 46b	NMDAR	Neuroscience
	TCS 46b 是一种具有口服活性的 NR1A/NR2B NMDA 受体拮抗剂。
T8920	Sepimostat	iGluR	Membrane transporter/Ion channel; Neuroscience
	Sepimostat 通过 NR2B 亚基的 Ifenprodil 结合位点的 NR2B N-甲基-D-天冬氨酸受体拮抗作用表现出神经保护活性。它抑制 Ifenprodil 结合的 Ki 值为27.7 µM。
T5522	NMDAR antagonist 1	Others; iGluR	Membrane transporter/Ion channel; Neuroscience; Others
	NMDAR antagonist 1 是一种 NR2B 选择性的、口服具有活力的 NMDAR 拮抗剂。
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。
T12758	Ro 25-6981	NMDAR	Neuroscience
	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。
T8450	TCN 213 TCN213	NMDAR	Neuroscience
	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。
T40999	NMDA receptor antagonist 2
	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.
T23457	threo Ifenprodil hemitartrate	Others	Others
	σ receptor agonist and NR2B subunit-selective NMDA receptor antagonist
T23239	Ro 04-5595 hydrochloride	Others	Others
	NR2B-containing NMDA receptors antagonist
T31046	CP-283097 CP283097,UNII-WHL1Z3GN15,CP 283097
	CP-283097 is an N-methyl-D-aspartic acid (NMDA) receptor antagonist with NR2B subunit.
T70055	CO-101244 Free Base
	CO-101244 Free Base is an NMDA receptor NR2B subunit blocker.
T24717	Ro 25-6981 HCl Ro 25 6981 HCl
	Ro 25-6981 HCl is an effective and selective NMDA glutamate receptors containing the NR2B subunit antagonist.
T30428	Besonprodil Besonprodil (USAN),UNII-5K3N2D15WW,253450-09-8,CHEMBL219631,CI-1041
	Besonprodil is a drug that acts as an NMDA antagonist and is selective for the NR2B subunit.
T12758L	Ro 25-6981 Maleate	Others	Others
	Ro 25-6981 Maleate is a potent and selective activity-dependent NMDA receptors blocker containing the NR2B subunit.(IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively).
TQ0233L	Traxoprodil Mesylate
	Traxoprodil Mesylate is a potent noncompetitive N-methyl-D-aspartate (NMDA) receptors antagonist and has selective for the NR2B subunit.
T70049	Ro 04-5595 free base
	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...
T62126	(Rac)-NMDAR antagonist 1
	(Rac)-NMDAR antagonist 1 是一种 NMDAR antagonist 1 的消旋体。其中 NMDAR antagonist 1 是一种有效的、口服具有活力的、NR2B 选择性的 NMDAR 拮抗剂。
T37096	Sepimostat dimethanesulfonate
	Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 μM[1]. Sepimostat (1 to 100 nmol/eye, intravitreal injection) exhibits significant neuroprotective effect[1]. ...
T68255	CJ 036878
	CJ 036878 was developed as an antagonist of the N-methyl-D-aspartate receptor NR2B subunit.
T23809	BMT-108908 BMT108908
	BMT-108908 is a Negative Allosteric Modulator. It is selective for the NR2B Subtype of The NMDA Receptor Impair Cognition in Multiple Domains.
T61319	Onfasprodil
	Onfasprodil, a negative allosteric modulator of NR2B, has been identified as a potential compound for researching Alzheimer's disease. This compound, in combination with a GABA receptor regulator.[1]
TP2060	Conantokin G
	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
T68973	EVT-101 free base
	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.
T41058	Nelonemdaz potassium Neu2000potassium,Salfaprodil
	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.
T83731	Tat-CBD3 TFA
	Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白质-蛋白质相互作用的抑制剂。它还能抑制CRMP2与NMDA受体NR2B亚单位之间的蛋白质-蛋白质相互作用。在无细胞实验中，Tat-CBD3 (10 µM)能将Cav2.2-CRMP2相互作用抑制43%，并在免疫共沉淀实验中抑制NMDA受体NR2B亚单位-CRMP2相互作用。它能在初级大鼠背根神经节 (DRG) 神经元中减少约60%的电压诱导钙电流，并在初级大鼠海马神经元中减少谷氨酸诱导的胞内钙水平增加。Tat-CBD3 (20 mg/kg)在大鼠中脑动脉闭塞 (MCAO) 引发的脑缺血模型中减少梗死体积。鞘内给药Tat-CBD3 (20 µg/5 µl)可防止大鼠卡拉胶诱导的热敏感性。
T37671	CAY10608 CAY10608
	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. CAY...
T37215	5α,6β-Dihydroxycholestanol
	5α,6β-Dihydroxycholestanol is an oxysterol metabolite of cholesterol formed from conversion of cholesterol epoxides by 5,6-epoxysterol hydrolase. It inhibits NMDA-mediated calcium influx in HEK293 cells expressing NR1/NR2B NMDA receptors in a concentration-dependent manner. It also binds to voltage-gated sodium (Nav) channels and decreases action potentials in hippocampal neurons in vitro when used at a concentration of 10 uM. It increases survival of spinal cord motoneurons, cortical neurons, a...

化合物

Cat.No: T25196

Synonym: BZAD-01,BZAD 01

Target: NMDAR

Co 101244 hydrochloride

Cat.No: T22674

Synonym: Co 101244盐酸盐,4-Piperidinol, 1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-Methylphenyl)Methyl]-,hydrochloride

Target: NMDAR

Tat-NR2B9c acetate

Cat.No: T13112L1

Synonym: Tat-NR2B9c acetate (500992-11-0 Free base),NA-1 acetate

Target: Others

Cat.No: T81037

Cat.No: T35924

Synonym: Tat-NR2Baa

Cat.No: T76069

Cat.No: T13112L

Synonym: NA-1 (TFA)

Target: Others

Cat.No: T13112

Synonym: Tat-NR2Bct,NA-1

Target: NO Synthase, iGluR

Cat.No: T5385

Synonym: RGH-896

Target: NMDAR, iGluR

Cat.No: T1751

Synonym: 依利罗地,SL-820715

Target: NMDAR, iGluR

Cat.No: T23449

Target: NMDAR

Cat.No: T8920

Target: iGluR

NMDAR antagonist 1

Cat.No: T5522

Target: Others, iGluR

Cat.No: T12234

Target: NMDAR

Cat.No: T12758

Target: NMDAR

Cat.No: T8450

Synonym: TCN213

Target: NMDAR

NMDA receptor antagonist 2

Cat.No: T40999

threo Ifenprodil hemitartrate

Cat.No: T23457

Target: Others

Ro 04-5595 hydrochloride

Cat.No: T23239

Target: Others

Cat.No: T31046

Synonym: CP283097,UNII-WHL1Z3GN15,CP 283097

CO-101244 Free Base

Cat.No: T70055

Cat.No: T24717

Synonym: Ro 25 6981 HCl

Cat.No: T30428

Synonym: Besonprodil (USAN),UNII-5K3N2D15WW,253450-09-8,CHEMBL219631,CI-1041

Ro 25-6981 Maleate

Cat.No: T12758L

Target: Others

Traxoprodil Mesylate

Cat.No: TQ0233L

Ro 04-5595 free base

Cat.No: T70049

(Rac)-NMDAR antagonist 1

Cat.No: T62126

Sepimostat dimethanesulfonate

Cat.No: T37096

Cat.No: T68255

Cat.No: T23809

Synonym: BMT108908

Cat.No: T61319

Cat.No: TP2060

EVT-101 free base

Cat.No: T68973

Nelonemdaz potassium

Cat.No: T41058

Synonym: Neu2000potassium,Salfaprodil

Cat.No: T83731

Cat.No: T37671

Synonym: CAY10608

5α,6β-Dihydroxycholestanol

Cat.No: T37215

Cat. No.	Product Name	Target	Signaling Pathways
T1186	Ifenprodil Tartrate	Potassium Channel; NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	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。

天然产物

Ifenprodil Tartrate

Cat.No: T1186

Target: Potassium Channel, NMDAR, iGluR

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