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28

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0137	Mirtazapine 米氮平,6-Azamianserin,Org3770	Dopamine Receptor; 5-HT Receptor; Opioid Receptor; Adrenergic Receptor; Histamine Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Mirtazapine (6-Azamianserin) 是一种有效的具有口服活性的去甲肾上腺素能和特异性血清素能抗抑郁剂 (NaSSA)。它也是一种5-HT2、5-HT3、组胺 H1 受体和 α2-肾上腺素受体拮抗剂，pKi 值分别为 8.05、8.1、9.3 和 6.95。
T13458	(Z)-Thiothixene Thiothixene,Navane,cis-Thiothixene	Serotonin Transporter	Neuroscience
	(Z)-Thiothixene (Thiothixene) 是一种血清素受体拮抗剂。
T21011	Buspirone Buspirone free base,Ansial,丁螺环酮	5-HT Receptor	GPCR/G Protein; Neuroscience
	Buspirone (Buspirone free base) 是一种azaspiro 化合物，具有抗焦虑药、镇静剂、血清素能激动剂和EC 3.4.21.26(脯氨酸寡肽酶)抑制剂的作用。
T8438	4i CHEMBL1269981,5-HT3 antagonist-4i	5-HT Receptor	GPCR/G Protein; Neuroscience
	4i (CHEMBL1269981) 是一种 5-HT3 受体拮抗剂，可调节血清素系统。
T60325	Viloxazine Emovit,Viloxazin	5-HT Receptor; Norepinephrine	GPCR/G Protein; Neuroscience
	Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].
T2395	Vortioxetine 沃替西汀,Lu AA 21004	5-HT Receptor; Serotonin Transporter	GPCR/G Protein; Neuroscience
	Vortioxetine (Lu AA 21004) 是5-HT1A、5-HT1B、5-HT3A、5-HT7受体和 5-羟色胺转运体抑制剂，Ki 值分别为 15、33、3.7、19 和 1.6 nM。它作为抗抑郁药，用于治疗重度抑郁症。
T21629	Loxapine	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	Loxapine 是 D2DR 和 D4DR 抑制剂和5-羟色胺能受体拮抗剂，是一种抗精神病药物，主要用于治疗精神分裂症。
T21569	1-(1-Naphthyl) piperazine hydrochloride 1-naphthalen-1-ylpiperazine hydrochloride,1-(Naphthalen-1-yl)piperazine hydrochloride	Others	Others
	1-(1-Naphthyl) piperazine hydrochloride (1-naphthalen-1-ylpiperazine hydrochloride) 是一种 5-羟色胺能配体，可与多种 5-羟色胺 (5-HT) 受体非选择性结合。
T20828	Citalopram Cipram,Lu 10-171,Lu-10-171 Lu10-171	5-HT Receptor	GPCR/G Protein; Neuroscience
	Citalopram (Lu 10-171) 是一种具有口服活性的、选择性的血清素再摄取抑制剂 (SSRI)，是一种选择性5-羟色胺再摄取抑制剂，是一种 S(+)-对映体 (Escitalopram) 和 R(-)-对映体的外消旋混合物。Citalopram 具有抗抑郁活性，可增强血清素能神经传递，可用于研究老年痴呆。
T68090	Laprafylline	Others	Others
	Laprafylline 是一种黄嘌呤化合物，对体内支气管收缩有抑制作用，且具有抗肿瘤活性。Laprafylline在低浓度时可充当竞争性血清素能拮抗剂，在高难度时抑制由hist引起的收缩。
T4297	Flibanserin BIMT-17BS,氟立班丝氨,Girosa,BIMT-17	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	Flibanserin (Girosa) 一种具有口服活性的 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂，Ki 值分别为 1 和 49 nM。它与多巴胺 D4 受体结合，Ki 值在 4 到 24 nM 之间。它是一种血清素能抗抑郁药，用于治疗性欲减退症。
T21526	α-Guanidinoglutaric Acid	Others	Others
	α-Guanidinoglutaric Acid 存在于猫大脑皮层钴诱导的致癫痫病灶组织中。 α-Guanidinoglutaric Acid 诱导的癫痫发作与血清素功能异常有关，它们是由 5-HT 水平的降低引起的。
T1483	Citalopram hydrobromide Lu 10-171,Nitalapram HBr,Bonitrile HBr,XU-62-320,Lu 10-171 HBr,氢溴酸西酞普兰,Citalopram HBr	5-HT Receptor; Serotonin Transporter; Autophagy	Autophagy; GPCR/G Protein; Neuroscience
	Citalopram hydrobromide (XU-62-320) 是一种选择性 5-羟色胺再摄取抑制剂，可选择性地抑制 CNS 神经元对 5-羟色胺的再摄取，从而增强中枢神经系统中的 5-羟色胺能活性，也具有抗抑郁活性。它抑制兔血小板中 5-HT 的摄取，IC50为 14 nM。
T1279	Vilazodone 维拉佐酮,SB659746A,EMD 68843	5-HT Receptor; Serotonin Transporter	GPCR/G Protein; Neuroscience
	Vilazodone (SB659746A) 是一种可口服的选择性 5 -羟色胺再摄取抑制剂 (SSRI) 和部分5-HT1A 受体激动剂。它有抗抑郁作用，可用于抑郁症和情绪性疾病的研究。
T9169	MPP+ iodide	Mitochondrial Metabolism; Autophagy	Autophagy; Metabolism
	MPP+ iodide 是一种 5-羟色胺转运体的高亲和力底物，也是一种神经毒素 MPTP 的有毒代谢物，通过选择性破坏黑质多巴胺能神经元，在动物模型中引起帕金森病症状。它被多巴胺转运体吸收进入多巴胺能神经元，通过影响呼吸链复合体 I 对线粒体发挥神经毒性作用。
T76863	Elezanumab AE12-1Y-QL,ABT-555	TGF-beta/Smad	Stem Cells
	Elezanumab(ABT-555) 是一种有效的人抗 RGMa 单克隆抗体。Elezanumab 通过 SMAD1/5/8 通路发挥对 RGMa 介导的 BMP 信号传导的抑制作用，IC50 约为 97 pM。在神经元损伤和脱髓鞘模型中，Elezanumab 促进神经再生、神经保护和神经恢复。Elezanumab 促进皮质脊髓轴突生长为脊髓灰质，并增强腹角的血清素能神经支配，形成颈部病变尾部的突触连接。
T28034	MGS-0039 BCI 632,BCI-632,MGS0039,BCI632
	MGS-0039 is a group II metabotropic glutamate receptor (mgluR2/3) antagonist. Antidepressant-like action of group II mGlu receptor antagonists does not depend on serotonergic system activation. However, the AMPA receptor seems to play a key role in the an
T68960	F-15599 Fumarate
	F-15599 Fumarate is a highly selective post-synaptic 5-HT(1A) receptor agonist: in-vivo profile in behavioural models of antidepressant and serotonergic activity.
T25786	Medifoxamine fumarate LG-152,LG 152,LG152,Geraxyl,Cledial
	Medifoxamine fumarate, an atypical antidepressant, has additional anxiolytic properties acting by dopaminergic and serotonergic mechanisms.
T23170	PNU-96415E PNU 96415E	Others	Others
	dopamine D4 and serotonergic 5-HT2A receptor antagonist
T35104	Way 100135 Way-100135,Way100135
	Way 100135 is a serotonergic drug of the phenylpiperazine family which is used in scientific research. It acts as a potent 5-HT1A receptor antagonist and a partial agonist of the 5-HT1D receptor, and to a much lesser extent, of the 5-HT1B receptor.
T31864	FPFS-1169 HCl R-(-)-BPAP,FPFS 1169,FPFS-1169 hydrochloride,BPAP-cpd,R-FPFS-1169,FPFS1169
	FPFS-1169 (BPAP-CPD, R-(-)-BPAP, R- FpFS-1169) is a proto-oncogene protein C-Bcl-2 stimulant that is one of the "catecholaminergic and serotonergic enhancers" and may be used for the treatment of Parkinson's disease.
T27523	H77-77 H77/77
	H77-77, a monoamine oxidase (MAO) inhibitor, produces a pronounced protection against phenelzine within the serotonergic and noradrenergic neurons in rats.
T78684	FFN246	5-HT Receptor	GPCR/G Protein; Neuroscience
	FFN246作为serotonin transporter (SERT) 和 vesicular monoamine transporter2 (VMAT2) 的荧光双底物探针，具有392/427 nm的激发和发射光谱。该化合物能够通过SERT依赖性积累，标记小鼠脑组织中的5-羟色胺能神经元。
T27331	Flerobuterol HCl CRL-40996,CRL40996,CRL 40996,Flerobuterol hydrochloride
	Flerobuterol is a β adrenergic receptor agonist potentially for the treatment of major depressive disorder. Flerobuterol enhances serotonergic neurotransmission. Flerobuterol acutely increases 5-HT synthesis, in part, through an elevation of brain Trp ava
T10371	Arotinolol	5-HT Receptor	GPCR/G Protein; Neuroscience
	Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. It is an antihypertensive agent.
T69206	AL-38022A
	AL-38022A is a novel synthetic serotonergic (5-HT) ligand that exhibited high affinity for each of the 5-HT2 receptor subtypes (Ki<or=2.2 nM), but a significantly lower (>100-fold less) affinity for other 5-HT receptors. In addition, AL-38022A displayed a very low affinity for a broad array of other receptors, neurotransmitter transport sites, ion channels, and second messenger elements, making it a relatively selective agent. AL-38022A potently stimulated functional responses via native and clo...
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

化合物

Cat.No: T0137

Synonym: 米氮平,6-Azamianserin,Org3770

Target: Dopamine Receptor, 5-HT Receptor, Opioid Receptor, Adrenergic Receptor, Histamine Receptor

(Z)-Thiothixene

Cat.No: T13458

Synonym: Thiothixene,Navane,cis-Thiothixene

Target: Serotonin Transporter

Cat.No: T21011

Synonym: Buspirone free base,Ansial,丁螺环酮

Target: 5-HT Receptor

Cat.No: T8438

Synonym: CHEMBL1269981,5-HT3 antagonist-4i

Target: 5-HT Receptor

Cat.No: T60325

Synonym: Emovit,Viloxazin

Target: 5-HT Receptor, Norepinephrine

Cat.No: T2395

Synonym: 沃替西汀,Lu AA 21004

Target: 5-HT Receptor, Serotonin Transporter

Cat.No: T21629

Target: Dopamine Receptor, 5-HT Receptor

1-(1-Naphthyl) piperazine hydrochloride

Cat.No: T21569

Synonym: 1-naphthalen-1-ylpiperazine hydrochloride,1-(Naphthalen-1-yl)piperazine hydrochloride

Target: Others

Cat.No: T20828

Synonym: Cipram,Lu 10-171,Lu-10-171 Lu10-171

Target: 5-HT Receptor

Cat.No: T68090

Target: Others

Cat.No: T4297

Synonym: BIMT-17BS,氟立班丝氨,Girosa,BIMT-17

Target: Dopamine Receptor, 5-HT Receptor

α-Guanidinoglutaric Acid

Cat.No: T21526

Target: Others

Citalopram hydrobromide

Cat.No: T1483

Synonym: Lu 10-171,Nitalapram HBr,Bonitrile HBr,XU-62-320,Lu 10-171 HBr,氢溴酸西酞普兰,Citalopram HBr

Target: 5-HT Receptor, Serotonin Transporter, Autophagy

Cat.No: T1279

Synonym: 维拉佐酮,SB659746A,EMD 68843

Target: 5-HT Receptor, Serotonin Transporter

Cat.No: T9169

Target: Mitochondrial Metabolism, Autophagy

Cat.No: T76863

Synonym: AE12-1Y-QL,ABT-555

Target: TGF-beta/Smad

Cat.No: T28034

Synonym: BCI 632,BCI-632,MGS0039,BCI632

F-15599 Fumarate

Cat.No: T68960

Medifoxamine fumarate

Cat.No: T25786

Synonym: LG-152,LG 152,LG152,Geraxyl,Cledial

Cat.No: T23170

Synonym: PNU 96415E

Target: Others

Cat.No: T35104

Synonym: Way-100135,Way100135

Cat.No: T31864

Synonym: R-(-)-BPAP,FPFS 1169,FPFS-1169 hydrochloride,BPAP-cpd,R-FPFS-1169,FPFS1169

Cat.No: T27523

Synonym: H77/77

Cat.No: T78684

Target: 5-HT Receptor

Flerobuterol HCl

Cat.No: T27331

Synonym: CRL-40996,CRL40996,CRL 40996,Flerobuterol hydrochloride

Cat.No: T10371

Target: 5-HT Receptor

Cat.No: T69206

Cat.No: T27269

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

Cat. No.	Product Name	Target	Signaling Pathways
T4S1990	Carvacrol 香荆芥酚,Karvakrol,O-Thymol,cymophenol,香芹酚	Apoptosis; Others; Gamma-secretase; Endogenous Metabolite; Antifungal	Apoptosis; Metabolism; Microbiology/Virology; Neuroscience; Others; Proteases/Proteasome; Stem Cells
	Carvacrol (O-Thymol) 是唇形科植物中的一种单萜酚类天然产物，具有镇痛、抗焦虑、抗抑郁、抗氧化、抗炎和抗癌作用。
T3386	Kaempferitrin Lespedin,Kaempferol,Lespenephryl,Lespenefril,Kaempferol 3,7-dirhamnoside,山奈苷	cell cycle arrest; Glucokinase; IGF-1R	Cell Cycle/Checkpoint; Metabolism; Tyrosine Kinase/Adaptors
	Kaempferitrin (Lespenephryl) 是天然黄酮苷类化合物，具有缓解疼痛、抗糖尿病、消炎、抗肿瘤和化疗作用，可激活胰岛素信号传导。
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。
TN1812	Jujuboside B1 酸枣仁皂苷 B1	5-HT Receptor	GPCR/G Protein; Neuroscience
	Jujubosides have hypnotic effect on normal rats, may be influenced by circadian rhythm and the serotonergic system may involve in the hypnotic effect of jujubosides, jujubosides may be good source of lead compounds for novel hypnotics.

天然产物

Cat.No: T4S1990

Synonym: 香荆芥酚,Karvakrol,O-Thymol,cymophenol,香芹酚

Target: Apoptosis, Others, Gamma-secretase, Endogenous Metabolite, Antifungal

Cat.No: T3386

Synonym: Lespedin,Kaempferol,Lespenephryl,Lespenefril,Kaempferol 3,7-dirhamnoside,山奈苷

Target: cell cycle arrest, Glucokinase, IGF-1R

Cat.No: T6S2227

Synonym: 斯皮诺素,Flavoayamenin

Target: Others

Cat.No: TN1812

Synonym: 酸枣仁皂苷 B1

Target: 5-HT Receptor

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