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33

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8702	SKF-83566	Dopamine Receptor; 5-HT Receptor; AChR	GPCR/G Protein; Neuroscience
	SKF-83566 是一种具有血脑渗透性和口服活性的 D1 样多巴胺受体拮抗剂和一种较弱的竞争性 5-HT2 受体拮抗剂，Ki 为 11 nM。它是竞争性多巴胺转运蛋白抑制剂，可用于研究帕金森氏症和对尼古丁渴望的缓解的相关研究。
T7180	Sultopride hydrochloride LIN-1418 hydrochloride,盐酸舒托必利,盐酸舒必利	Dopamine Receptor	GPCR/G Protein; Neuroscience
	Sultopride hydrochloride (LIN-1418 hydrochloride) 是一种多巴胺 D2受体的选择性拮抗剂。
T27252	ELB-139 ELB139
	ELB-139 is a GABA A receptor agonist. ELB139 increases 5-HT in the striatum and prefrontal cortex of rats.
T14083	Abaperidone	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	Abaperidone 是一种有效的 5-HT2A 受体和多巴胺 D2 受体拮抗剂，对 5-HT2A 受体的 IC50 为 6.2 nM，对多巴胺 D2 受体的IC50 为 17 nM。Abaperidone是一种潜在的非典型抗精神化合物，可降低大鼠纹状体和前额叶皮层中的基础hsp70 mRNA表达。
T12483	Piperidine-MO-1	Others	Others
	Piperidine-MO-1是多巴胺受体 (dopamine receptor) 调节剂，在大鼠纹状体中增加DOPAC 的 ED50 值为68 μmol/kg。
TP1597L	Secretoneurin, rat acetate Secretoneurin, rat acetate(149146-12-3 Free base)	Others	Others
	Secretoneurin, rat acetate 是一种 33 个氨基酸的多肽，由分泌粒蛋白 II (SgII) 的蛋白水解加工产生。它在体内和体外诱导大鼠纹状体中的多巴胺释放，它对单核细胞和嗜酸性粒细胞有很强的趋化作用，但对粒细胞没有。
T22781L	FFN 511 hydrochloride FFN 511 hydrochloride(1004548-96-2 Free base)
	FFN 511 hydrochloride 是一种针对神经元囊泡单胺转运体 2 (VMA T2) 的荧光假神经递质 (FFNs)。FFN 511 hydrochloride 可抑制 5-羟色胺与含 VMA T2 的膜结合，可用于标记活体皮质-纹状体急性切片中的多巴胺能神经末梢。激发和发射最大值分别为 406 和 501 nm。
T6951	Pramipexole dihydrochloride hydrate Pramipexole 2HCl Monohydrate,普拉克索盐酸盐水合物,Mirapex,普拉克索	Dopamine Receptor	GPCR/G Protein; Neuroscience
	Pramipexole dihydrochloride hydrate (Mirapex) 是选择性的，具有血脑屏障 (BBB) 渗透性的 D2 型多巴胺受体激动剂，对 D2 型受体、D2、D3、D4亚型受体的 Ki 分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM，可用于研究帕金森综合症和腿多动综合征。
TP1920L1	Acein acetate	RAAS	Endocrinology/Hormones
	Acein acetate 是高亲和力血管紧张素转换酶 (ACE) 配体 (Kd = 2.79 nM)。浓度高达 500 nM 时对 ACE 酶活性没有显着影响。增强 NMDA + D-丝氨酸诱导的多巴胺从体外纹状体切片和体内纹状体的释放。
T23265	RS 67333 hydrochloride RS 67333 (hydrochloride),RS 67333 HCl,盐酸RS67333	5-HT Receptor	GPCR/G Protein; Neuroscience
	RS 67333 hydrochloride (RO5203648) 是一种有效的、选择性的5-HT4 受体 (5-HT4R) 部分激动剂，在豚鼠纹状体中的 pKi 为 8.7。RS 67333 hydrochloride 对其他几种受体的亲和力较低，包括 5-HT1A、5-HT1D、5-HT2A、5-HT2C、多巴胺 D1、D2 和毒蕈碱 M1-M3 受体。RS 67333 hydrochloride 具有神经保护作用，可用于阿尔茨海默病研究。
T37190	L-Allylglycine	Dehydrogenase; GABA Receptor	Membrane transporter/Ion channel; Metabolism; Neuroscience
	L-Allylglycine 是 GABA 合成酶（谷氨酸脱羧酶）的有效抑制剂。
T33656	Neurotensin (1-6)
	Neurotensin (1-6) affects dopamine release from striatum.
T26993	CGP 56999A CGP56999A,CGP-56999A
	CGP 56999A is an antagonist of GABA(B) receptor, it enhances expression of brain-derived neurotrophic factor and attenuates dopamine depletion in the rat corpus striatum.
T23722	AMG-7980 AMG7980
	AMG-7980 is a highly specific phosphodiesterase 10A ligand. It shows a good uptake in the striatum.
T10542	Bifeprunox	Others	Others
	Bifeprunox is a potent partial agonist of dopamine D2-like and 5-HT1A receptor (pEC50: 6.37 for hippocampus 5-HT1A; pKis: 7.19 and 8.83 for cortex 5-HT1A and striatum D2). It is an antipsychotic for the research of schizophrenia.
T69449	Cyclindole
	Cyclindole is an antipsychotic with a tricyclic structure that was never marketed. It displaces spiperone binding in vitro and elevates dopamine levels in the striatum, indicating it acts as a D₂ receptor antagonist.
T28336	PD 142505-0028 CI 1017,CI1017,CI-1017,PD-142505-0028,PD42505-0028
	PD 142505-0028, a functionally M1-selective muscarinic agonist, rapidly increases glutamate but not aspartate concentrations in the striatum of anesthetized rats. Additionally, it inhibited production of amyloidogenic A beta and increased secretion of sol
T36233	Dicrotalic anhydride 3-hydroxy-3-Methylglutaric anhydride	Others	Others
	Dicrotalic anhydride（3-hydroxy-3-Methylglutaric anhydride) 可诱导大鼠纹状体DNA损伤。
T38221	N,N-Dipropyldopamine (hydrobromide)
	N,N-Dipropyldopamine is a dopamine receptor agonist.1,2,3 It decreases dihydrophenylalanine (DOPA) levels in the limbic forebrain and striatum of reserpinized rats (ED50s = 25 and 20 μmol/kg, respectively), as well as reduces homovanillic acid levels in rat striatum when administered at a dose of 80 μmol/kg.1 N,N-Dipropyldopamine (0.5-16 mg/kg) reduces spontaneous locomotor activity in mice, an effect that can be reversed by the antipsychotic spiroperidol.2,3
T27455	GSK-215083 GSK215083
	GSK-215083 is a PET radioligand for the 5-HT6 receptor. GSK 215083 is a quinoline based compounds and acts by antagonising the 5-HT6 receptor. GSK-215083 binds to receptors 5-hydroxytrypamine-6 (5HT6) in the striatum and 5-hydroxytryptamine-2A (5HT2A) in
T16547	PK14105	Others	Others
	PK14105 has been evaluated biologically as a potential radioligand for positron emission tomography (PET) studies targeting peripheral benzodiazepine binding sites (PBBS) receptors. When administered to rats with unilaterally lesioned striata, PK14105 was observed to quickly cross the blood-brain barrier, displaying significant radioactivity retention in the lesioned striatum, in contrast to the unlesioned striatum or cerebellar vermis. Additionally, PK14105 has the capability to inhibit recepto...
TP1920	Acein
	Acein is a High affinity angiotensin-converting enzyme (ACE) ligand (Kd = 2.79 nM). Exhibits no significant effect on ACE enzymatic activity up to 500 nM concentration. Potentiates NMDA + D-serine-induced dopamine release from striatal slices in vitro and the striatum in vivo.
T76599	Ac-Leu-Val-Lys-Aldehyde
	Ac-Leu-Val-Lys-Aldehyde 是有效的组织蛋白酶 B (cathepsin B) 抑制剂，其 IC50 值为 4 nM。该化合物能显着降低喹啉酸引起的纹状体细胞死亡，并促使 LC3-II 积累。
T76403	[Glp5] Substance P (5-11)
	[Glp5] Substance P (5-11)为一八肽，为大鼠中枢神经系统(CNS)主要P物质片段之一，局部调节大鼠纹状体多巴胺释放。
T29002	Trazium Esilate EGYT3615,EGYT-3615,EGYT 3615
	Trazium esilate is an adrenergic receptor antagonist. Trazium esilate is a weak displacer on a1-, a2- and D2-receptors, however, it induced a2-receptor desenzitization after repeated treatment. It had no influence on rat brain cortical noradrenaline and s
T26564	ADCI SGB-017,SGB017,SGB 017
	ADCI is an inhibitor of voltage-activated sodium channels and N-methyl-D-aspartate (NMDA)-receptor-gated channels. Inhibition of sodium channels by ADCI was voltage dependent. High doses of ADCI increased dopamine metabolism in the prefrontal cortex and/o
T82972	Argininosuccinic acid disodium	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	Argininosuccinic acid disodium 在尿素循环的第四步起关键作用，由ASL(精氨酸琥珀酸裂解酶)催化裂解生成精氨酸和富马酸。此外，该化合物能够降低GSH(还原型谷胱甘肽)浓度，并提升大脑皮层与纹状体中的活性氧产生。Argininosuccinic acid disodium 还可能导致脂质过氧化和蛋白质氧化，并在发育中的大鼠脑内触发氧化应激。
T70456	Nolpitantium Free Base
	Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no eff...
T36176	AMK (hydrochloride)
	AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7...
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...
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...
T83894	4A7C-301-Nurr1 Agonist 4A7C-301-Nuclear Receptor-Related 1
	4A7C-301-Nurr1激动剂是一种核受体相关1（Nurr1）的激动剂。它通过与Nurr1配体结合域（LBD；IC50 = 48.22 nM）结合，增加了在使用SK-N-BE(2)C人神经母细胞瘤细胞进行的报告基因测定中Nurr1-LBD和全长Nurr1的转录活性（EC50s = 6.53 和 50-70 µM，分别）。每天5 mg/kg的4A7C-301-Nurr1激动剂能减少在经MPTP神经毒素或α-突触核蛋白过表达诱导的帕金森病鼠模型中纹状体和黑质compacta部分多巴胺能细胞的死亡，并减少运动和嗅觉缺陷，而不诱发类似运动障碍的行为。
T36947	Pyrithiamine (hydrobromide)
	Pyrithiamine is the pyridine analog of thiamine that prevents growth of organisms that require intact thiamine. [1] It inhibits the growth of bacterial and fungal species at a pyrithiamine:thiamine ratio of 10:1 in growth media and induces symptoms of thiamine deficiency in mice at a dietary ratio of 3:1. These effects are reversible with addition of sufficient thiamine in all species. Pyrithiamine inhibits the formation of cocarboxylase from thiamine in chicken blood in a dose-dependent manner....

化合物

Cat.No: T8702

Target: Dopamine Receptor, 5-HT Receptor, AChR

Sultopride hydrochloride

Cat.No: T7180

Synonym: LIN-1418 hydrochloride,盐酸舒托必利,盐酸舒必利

Target: Dopamine Receptor

Cat.No: T27252

Synonym: ELB139

Cat.No: T14083

Target: Dopamine Receptor, 5-HT Receptor

Piperidine-MO-1

Cat.No: T12483

Target: Others

Secretoneurin, rat acetate

Cat.No: TP1597L

Synonym: Secretoneurin, rat acetate(149146-12-3 Free base)

Target: Others

FFN 511 hydrochloride

Cat.No: T22781L

Synonym: FFN 511 hydrochloride(1004548-96-2 Free base)

Pramipexole dihydrochloride hydrate

Cat.No: T6951

Synonym: Pramipexole 2HCl Monohydrate,普拉克索盐酸盐水合物,Mirapex,普拉克索

Target: Dopamine Receptor

Cat.No: TP1920L1

Target: RAAS

RS 67333 hydrochloride

Cat.No: T23265

Synonym: RS 67333 (hydrochloride),RS 67333 HCl,盐酸RS67333

Target: 5-HT Receptor

Cat.No: T37190

Target: Dehydrogenase, GABA Receptor

Neurotensin (1-6)

Cat.No: T33656

Cat.No: T26993

Synonym: CGP56999A,CGP-56999A

Cat.No: T23722

Synonym: AMG7980

Cat.No: T10542

Target: Others

Cat.No: T69449

Cat.No: T28336

Synonym: CI 1017,CI1017,CI-1017,PD-142505-0028,PD42505-0028

Dicrotalic anhydride

Cat.No: T36233

Synonym: 3-hydroxy-3-Methylglutaric anhydride

Target: Others

N,N-Dipropyldopamine (hydrobromide)

Cat.No: T38221

Cat.No: T27455

Synonym: GSK215083

Cat.No: T16547

Target: Others

Cat.No: TP1920

Ac-Leu-Val-Lys-Aldehyde

Cat.No: T76599

[Glp5] Substance P (5-11)

Cat.No: T76403

Trazium Esilate

Cat.No: T29002

Synonym: EGYT3615,EGYT-3615,EGYT 3615

Cat.No: T26564

Synonym: SGB-017,SGB017,SGB 017

Argininosuccinic acid disodium

Cat.No: T82972

Target: Reactive Oxygen Species

Nolpitantium Free Base

Cat.No: T70456

AMK (hydrochloride)

Cat.No: T36176

Alaproclate (hydrochloride)

Cat.No: T36521

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

4A7C-301-Nurr1 Agonist

Cat.No: T83894

Synonym: 4A7C-301-Nuclear Receptor-Related 1

Pyrithiamine (hydrobromide)

Cat.No: T36947

Cat. No.	Product Name	Target	Signaling Pathways
T6S2227	Spinosin 斯皮诺素,Flavoayamenin	Others	Others
	Spinosin (Flavoayamenin) 是一种具有神经保护作用的 C-糖苷类黄酮，从 Zizyphus jujube 种子分离得到，能够激活 Nrf2/HO-1 通路，并抑制 Aβ1-42的产生和聚合。

天然产物

Cat.No: T6S2227

Synonym: 斯皮诺素,Flavoayamenin

Target: Others

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