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44

抑制剂 & 化合物

1

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Cat. No. Product Name Target Signaling Pathways
T39429 AHN 1-055 hydrochloride

3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride

Dopamine Receptor GPCR/G Protein; Neuroscience
AHN 1-055 hydrochloride (3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride) 与多巴胺转运蛋白具有高亲和力,是多巴胺摄取抑制剂,IC50为 71 nM。
T22714 Decynium 22

Others Others
Decynium 22 是有机阳离子转运蛋白和单胺转运蛋白的抑制剂,具有抗抑郁作用。
T0322 Fipexide

Dopamine Receptor; AChR GPCR/G Protein; Neuroscience
Fipexide 是对氯苯乙酸衍生物,是哌嗪化学类的精神活性药物,作为促智药物,有用于老年痴呆的研究潜力。它可降低了纹状体腺苷酸环化酶的活性,通过多巴胺能神经传递对认知表现出积极的作用。
T11087 DOV-216,303 Free Base

DOV-216303

Dopamine Receptor; Serotonin Transporter; Norepinephrine GPCR/G Protein; Neuroscience
DOV-216,303 Free Base (DOV-216303) 是血清素、去甲肾上腺素和多巴胺再摄取的抑制剂,IC50 为 14、20 和 78 nM。 DOV-216,303 Free Base 具有抗抑郁作用。
T1993 J-147

J147

Epigenetic Reader Domain; Dopamine Receptor; Monoamine Oxidase Chromatin/Epigenetic; GPCR/G Protein; Neuroscience
J-147 是一种高效的、具有口服活性的、可透过血脑屏障神经保护剂,可增强认知能力。它抑制单胺氧化酶 B 和多巴胺转运体,EC50分别为 1.88 μM 和 0.649 μM。它有研究阿尔茨海默氏症的潜力。
T6414 Bisacodyl

比沙可啶,Fenilaxan,Dulcolax,Brocalax

Others Others
Bisacodyl (Fenilaxan) 是刺激性缓泻剂,可直接作用于结肠以产生排便。它能够直接激活结肠巨噬细胞来增加 PGE2的分泌。PGE2充当旁分泌因子并减少结肠中 AQP3 的表达,抑制水从腔向血管一侧的转移,进而产生通便作用。
T3526 Dasotraline hydrochloride

SEP-225289 hydrochloride,达索曲林盐酸盐

Dopamine Receptor; 5-HT Receptor; Serotonin Transporter; Norepinephrine GPCR/G Protein; Neuroscience
Dasotraline hydrochloride (SEP-225289 hydrochloride) 是具有阻断多巴胺 (IC50=4 nM),去甲肾上腺素 (IC50=6 nM) 和三羟色胺转运蛋白 (IC50=11 nM)的三重再摄取抑制剂。
T10758L Centanafadine hydrochloride

EB-1020 hydrochloride

Dopamine Receptor; Serotonin Transporter; Adrenergic Receptor; Norepinephrine GPCR/G Protein; Neuroscience
Centanafadine hydrochloride (EB-1020 hydrochloride) 是一种去甲肾上腺素(NE)/多巴胺(DA)转运的双抑制剂,还能抑制5-羟色胺(serotonin)转运体。它对人 NE,DA 和5-羟色胺转运体的 IC50值分别为6 nM,38 nM 和 83 nM。
T0766 Promazine hydrochloride

Romtiazin hydrochloride,Sinophenin hydrochloride,盐酸丙嗪

Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; AChR GPCR/G Protein; Neuroscience
Promazine hydrochloride (Romtiazin hydrochloride) 是一种抗精神病药,也是一种多巴胺受体 (D2) 拮抗剂,能够抑制多巴胺能神经传递。
T1871 GBR 12935 dihydrochloride

GBR12935,GBR-12935,GBR 12935

Dopamine Receptor GPCR/G Protein; Neuroscience
GBR 12935 dihydrochloride (GBR 12935) 是一种多巴胺再吸收抑制剂。
T2092 Amitifadine hydrochloride

DOV-21947 hydrochloride,EB-1010 hydrochloride

Dopamine Receptor; 5-HT Receptor; Serotonin Transporter; Norepinephrine GPCR/G Protein; Neuroscience
Amitifadine hydrochloride (EB-1010 hydrochloride) 是一种 5-羟色胺-去甲肾上腺素-多巴胺的再摄取抑制剂(SNDRI),其在 HEK 293 细胞中测得的 IC50值分别为 12, 23, 96 nM。
T1336 Benztropine mesylate

Benzotropine mesylate,苯扎托品,Benzatropine mesylate,Benztropine methanesulfonate,甲磺酸苯扎托品

Dopamine Receptor; AChR; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Benztropine mesylate (Benztropine methanesulfonate) 是一种可口服的中枢性抗胆碱能剂,用于帕金森氏病的研究。它是抗组胺剂,抑制多巴胺的吸收。它也是人 D2多巴胺受体的变构拮抗剂,具有抗癌症干细胞的作用。
T0991 Desipramine hydrochloride

NSC-114901,Desmethylimipramine,盐酸去甲咪嗪,JB-8181,EX-4355,Norimipramine,G-35020

Dopamine Receptor; 5-HT Receptor; Serotonin Transporter; Adrenergic Receptor GPCR/G Protein; Neuroscience
Desipramine hydrochloride (Norimipramine) 是一种二苯并氮杂类衍生物三环类抗抑郁药,可作为选择性去甲肾上腺素再摄取抑制剂。 它还显示出较弱的 5-羟色胺再摄取抑制、α1 阻断、抗组胺和抗胆碱能作用。
T7745 Diclofensine hydrochloride

4-(3,4-二氯苯)-7-甲氧基-2-甲基-1,2,3,4-四氢异喹啉盐酸盐,Ro 8-4650 hydrochloride

Others; Dopamine Receptor GPCR/G Protein; Neuroscience; Others
Diclofensine hydrochloride (Ro 8-4650 hydrochloride) 是一种高效单胺再摄取抑制剂,在大鼠脑突触体中能够阻断多巴胺 (IC50=0.74 nM)、去甲肾上腺素 (IC50=2.3 nM) 和 5-羟色胺 (IC50=3.7 nM)。
T7153 Vanoxerine dihydrochloride

GBR-12909 dihydrochloride,伐诺司林二盐酸盐,I893 dihydrochloride

Dopamine Receptor GPCR/G Protein; Neuroscience
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) 是一种竞争性的、有效的、选择性的多巴胺再摄取抑制剂,能够与多巴胺转运体 (DAT) 上的靶点结合。
T7341 Diclofensine

Ro 8-4650,(+/-)-双氮奋兴

Dopamine Receptor; Monoamine Transporter GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
Diclofensine (Ro 8-4650) 是一种高效单胺再摄取抑制剂,在大鼠脑突触体中能够阻断多巴胺 (IC50=0.74 nM)、去甲肾上腺素 (IC50=2.3 nM) 和 5-羟色胺 (IC50=3.7 nM)。
T7734 BETA-CFT sulfate

Others Others
BETA-CFT sulfate 是BETA-CFT 的衍生物。BETA-CFT 是多巴胺转运蛋白(DATs)的拮抗剂。
T23234 Rimcazole dihydrochloride

Others Others
Rimcazole dihydrochloride 是 Rimcazole 的盐酸盐,是一种σ受体拮抗剂。Rimcazole dihydrochloride 还与多巴胺转运蛋白结合,抑制多巴胺的摄取。
T0948 Adrenalone hydrochloride

Adrenalone HCl,肾上腺酮盐酸盐,盐酸肾上腺酮

Adrenergic Receptor GPCR/G Protein; Neuroscience
Adrenalone hydrochloride (Adrenalone HCl) 是一种多巴胺β氧化酶 (dopamine β oxidase) 抑制剂,结构与去甲肾上腺素转运蛋白 (NET) 配体相似,IC50=36.9 μM。它是一种肾上腺素能 (adrenergic) 激动剂,用作局部血管收缩剂和止血剂。
T41194 FFN 102 mesylate

Others Others
FFN 102 mesylate 是pH 响应型荧光假神经递质(FFN),作为选择性多巴胺转运蛋白(DAT)和VMAT2底物。FFN 102 mesylate 与38个中枢神经系统受体(包括多巴胺和血清素受体)无明显结合。它的Ex-max在pH 值5时为340 nm,在pH 值7.5时为370 nm,在pH 值为5和7.5时,Em-max为435 nm。
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。
T22959 m-Chlorophenylbiguanide hydrochloride

1-(3-Chlorophenyl)biguanidehydrochloride,1-(3-氯苯基)双胍

5-HT Receptor GPCR/G Protein; Neuroscience
m-Chlorophenylbiguanide hydrochloride 是一种 5-HT3 受体激动剂。它选择性结合 5-HT3(Ki: 0.002 µM) 超过 5-HT1A(Ki: 10 µM) 和 5-HT2(Ki: 10 µM) 受体,但也结合多巴胺转运蛋白上的高亲和力和低亲和力位点( DAT;IC50:在大鼠尾状壳核突触体膜中分别为 0.4 和 34.8 µM)。
T0255 Clomipramine hydrochloride

Clomipramine HCl,Anafranil,盐酸氯米帕明

Dopamine Receptor; 5-HT Receptor; Serotonin Transporter; Norepinephrine; GST GPCR/G Protein; Neuroscience; oxidation-reduction
Clomipramine hydrochloride (Anafranil) 是一种5-羟色胺转运体(Ki:0.14 nM)、去甲肾上腺素转运体(Ki:54 nM)和多巴胺转运体(Ki:3 nM)阻断剂。
T0869 Atomoxetine hydrochloride

Tomoxetine hydrochloride,(R)-Tomoxetine hydrochloride,盐酸托莫西汀,LY 139603,Atomoxetine HCl,LY 139603 HCl

Dopamine Receptor; 5-HT Receptor; Norepinephrine GPCR/G Protein; Neuroscience
Atomoxetine hydrochloride (LY 139603) 是苯氧基-3-丙胺衍生物和选择性非兴奋剂,是去甲肾上腺素再摄取抑制剂,具有认知增强活性。 与人 NET,SERT 和 DAT 的放射性配体结合的 Ki 分别为5,77和1451 nM。
T23501 Vanoxerine

Others Others
Vanoxerine is an antagonist of dopamine transporter (Ki: 16.9nM).
T29920 Altropane

Altropane is a SPECT imaging agent used for viewing dopamine transporter sites.
T10758 Centanafadine

EB-1020

Others Others
Centanafadine is a dual inhibitor of norepinephrine (NE)/dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter).
T24712 Rimcazole

Rimcazole is a sigma receptor antagonist. It also binds to the dopamine transporter and inhibiting dopamine uptake.
T26145 RTI 336

RTI336,RTI-336

RTI 336 is used as a chronic brain dopamine transporter (DAT) inhibitor.
T27036 CL-216303 HCl

DOV-216303,DOV216303,CL 216303,CL-216303,DOV 216303,CL216303

CL-216303 HCl, a dopamine transporter inhibitor and a 5-HT inhibitor, is used potentially for the treatment of depression.
T36949 Niaprazine

5-HT Receptor; Adrenergic Receptor; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Niaprazine 是有效的组胺 H1 受体拮抗剂,具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。
T10842 Clomipramine D3

氯米帕明 D3

Others Others
Clomipramine D3 is the deuterium-labeled Clomipramine. Clomipramine is a serotonin transporter, norepinephrine transporter dopamine transporter blocker (Ki: 0.14, 54 and 3 nM).
T10842L Clomipramine D3 hydrochloride

Others Others
Clomipramine D3 hydrochloride is the deuterium-labeled Clomipramine. Clomipramine is a serotonin transporter, norepinephrine transporter dopamine transporter blocker (Ki: 0.14, 54 and 3 nM).
T24956 (18F)LBT 999

(18F)LBT999,LBT999 18F,LBT 999 18F,LBT-999 18F,(18F)LBT-999

(18F)LBT 999 is a positron emission tomography (PET) tracer, used for the quantification of the dopamine transporter (DAT) in the healthy rat brain.
T31758 Fecnt F-18

J2.661.350G,18F-Fecnt,(18F)-Fecnt

[F-18] FECNT has been widely used to calculate dopamine transporter (DAT) occupancy rates in the brains of non-human primates and can distinguish DAT density differences between Parkinson's disease and healthy human controls.
T37699 Org 24598

Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 |Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibi...
T27689 JNJ-7925476 HCl

JNJ-7925476,JNJ7925476,JNJ 7925476

JNJ-7925476 HCl is a triple monoamine uptake inhibitor. JNJ-7925476 Salt blocks the dopamine transporter (DAT), norepinephrine transporter (NET) and serotonin transporter (SERT) in the central nervous system. The ED(50) values for JNJ-7925476 occupancy of
T70615 TAS-303

TAS-303 is a selective norepinephrine reuptake inhibitor which displays significant norepinephrine transporter (NET) inhibitory activity toward serotonin or dopamine transporters. Radioligand-binding studies showed that TAS-303 selectively and potently inhibited [3H]norepinephrine binding to the human NET.
T79264 Z1078601926

Z1078601926为hDAT (人多巴胺转运蛋白) 的变构抑制剂,且与诺米芬辛表现出协同效应。
T71772 Bicifadine free base

Bicifadine, also known as DOV-220075, CL 220,075, is a SNDR inhibitor potentially for the treatment of lower back pain. Bicifadine has a non-opioid, non-NSAID mechanism for the treatment of pain, which should have less abuse potential than opioid drugs and less propensity to cause gastric ulcers than NSAID drugs. While the drug is purported to be a serotonin (SERT) and noradrenaline transporter (NET) inhibitor, it also has effects at the dopamine transporter (DAT), effectively making it a broad...
T70914 GBR-12935 maleate

GBR-12935 is a potent and selective dopamine reuptake inhibitor. It was originally developed in its 3H radiolabelled form for the purpose of mapping the distribution of dopaminergic neurons in the brain by selective labelling of dopamine transporter proteins. This has led to potential clinical uses in the diagnosis of Parkinson's disease, although selective radioligands such as Ioflupane (¹²³I) are now available for this application. GBR-12935 is now widely used in animal research into Parkin...
T70960 Maprotiline-d3 hydrochloride

Maprotiline-d3 is intended for use as an internal standard for the quantification of maprotiline by GC- or LC-MS. Maprotiline is a tricyclic antidepressant. It binds to the norepinephrine transporter (NET) and is selective for NET over the serotonin and dopamine transporters. Maprotiline also binds to the serotonin (5-HT) receptor subtype 5-HT2A, as well as histamine H1, muscarinic acetylcholine, α1-adrenergic, and dopamine D2 receptors. In vivo, maprotiline inhibits norepinephrine reuptake in r...
T83888 (S)-5-hydroxy-6-methoxy Duloxetine maleate

(S)-5-羟基-6-甲氧基Duloxetine是(S)-duloxetine的一个活性代谢物,主要通过对血清素(5-HT)和去甲肾上腺素的再摄取进行抑制。它通过(S)-duloxetine经过一个5-或6-羟基Duloxetine中间体以及一个儿茶酚Duloxetine中间体形成,这些中间体由细胞色素P450 (CYP)同型酶CYP1A2和CYP2D6形成。(S)-5-羟基-6-甲氧基Duloxetine在脂质膜中抑制5-HT转运体(SERT)、去甲肾上腺素转运体(NET)和多巴胺转运体(DAT),其对人类转运体的抑制常数(Kis)分别为266、920和2,814 nM。
T37800 PF-04449613

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-0444...

化合物

AHN 1-055 hydrochloride
Cat.No: T39429
Synonym: 3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride
Target: Dopamine Receptor
Decynium 22
Cat.No: T22714
Synonym:
Target: Others
Fipexide
Cat.No: T0322
Synonym:
Target: Dopamine Receptor, AChR
DOV-216,303 Free Base
Cat.No: T11087
Synonym: DOV-216303
Target: Dopamine Receptor, Serotonin Transporter, Norepinephrine
J-147
Cat.No: T1993
Synonym: J147
Target: Epigenetic Reader Domain, Dopamine Receptor, Monoamine Oxidase
Bisacodyl
Cat.No: T6414
Synonym: 比沙可啶,Fenilaxan,Dulcolax,Brocalax
Target: Others
Dasotraline hydrochloride
Cat.No: T3526
Synonym: SEP-225289 hydrochloride,达索曲林盐酸盐
Target: Dopamine Receptor, 5-HT Receptor, Serotonin Transporter, Norepinephrine
Centanafadine hydrochloride
Cat.No: T10758L
Synonym: EB-1020 hydrochloride
Target: Dopamine Receptor, Serotonin Transporter, Adrenergic Receptor, Norepinephrine
Promazine hydrochloride
Cat.No: T0766
Synonym: Romtiazin hydrochloride,Sinophenin hydrochloride,盐酸丙嗪
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, AChR
GBR 12935 dihydrochloride
Cat.No: T1871
Synonym: GBR12935,GBR-12935,GBR 12935
Target: Dopamine Receptor
Amitifadine hydrochloride
Cat.No: T2092
Synonym: DOV-21947 hydrochloride,EB-1010 hydrochloride
Target: Dopamine Receptor, 5-HT Receptor, Serotonin Transporter, Norepinephrine
Benztropine mesylate
Cat.No: T1336
Synonym: Benzotropine mesylate,苯扎托品,Benzatropine mesylate,Benztropine methanesulfonate,甲磺酸苯扎托品
Target: Dopamine Receptor, AChR, Histamine Receptor
Desipramine hydrochloride
Cat.No: T0991
Synonym: NSC-114901,Desmethylimipramine,盐酸去甲咪嗪,JB-8181,EX-4355,Norimipramine,G-35020
Target: Dopamine Receptor, 5-HT Receptor, Serotonin Transporter, Adrenergic Receptor
Diclofensine hydrochloride
Cat.No: T7745
Synonym: 4-(3,4-二氯苯)-7-甲氧基-2-甲基-1,2,3,4-四氢异喹啉盐酸盐,Ro 8-4650 hydrochloride
Target: Others, Dopamine Receptor
Vanoxerine dihydrochloride
Cat.No: T7153
Synonym: GBR-12909 dihydrochloride,伐诺司林二盐酸盐,I893 dihydrochloride
Target: Dopamine Receptor
Diclofensine
Cat.No: T7341
Synonym: Ro 8-4650,(+/-)-双氮奋兴
Target: Dopamine Receptor, Monoamine Transporter
BETA-CFT sulfate
Cat.No: T7734
Synonym:
Target: Others
Rimcazole dihydrochloride
Cat.No: T23234
Synonym:
Target: Others
Adrenalone hydrochloride
Cat.No: T0948
Synonym: Adrenalone HCl,肾上腺酮盐酸盐,盐酸肾上腺酮
Target: Adrenergic Receptor
FFN 102 mesylate
Cat.No: T41194
Synonym:
Target: Others
MPP+ iodide
Cat.No: T9169
Synonym:
Target: Mitochondrial Metabolism, Autophagy
m-Chlorophenylbiguanide hydrochloride
Cat.No: T22959
Synonym: 1-(3-Chlorophenyl)biguanidehydrochloride,1-(3-氯苯基)双胍
Target: 5-HT Receptor
Clomipramine hydrochloride
Cat.No: T0255
Synonym: Clomipramine HCl,Anafranil,盐酸氯米帕明
Target: Dopamine Receptor, 5-HT Receptor, Serotonin Transporter, Norepinephrine, GST
Atomoxetine hydrochloride
Cat.No: T0869
Synonym: Tomoxetine hydrochloride,(R)-Tomoxetine hydrochloride,盐酸托莫西汀,LY 139603,Atomoxetine HCl,LY 139603 HCl
Target: Dopamine Receptor, 5-HT Receptor, Norepinephrine
Vanoxerine
Cat.No: T23501
Synonym:
Target: Others
Altropane
Cat.No: T29920
Synonym:
Target:
Centanafadine
Cat.No: T10758
Synonym: EB-1020
Target: Others
Rimcazole
Cat.No: T24712
Synonym:
Target:
RTI 336
Cat.No: T26145
Synonym: RTI336,RTI-336
Target:
CL-216303 HCl
Cat.No: T27036
Synonym: DOV-216303,DOV216303,CL 216303,CL-216303,DOV 216303,CL216303
Target:
Niaprazine
Cat.No: T36949
Synonym:
Target: 5-HT Receptor, Adrenergic Receptor, Histamine Receptor
Clomipramine D3
Cat.No: T10842
Synonym: 氯米帕明 D3
Target: Others
Clomipramine D3 hydrochloride
Cat.No: T10842L
Synonym:
Target: Others
(18F)LBT 999
Cat.No: T24956
Synonym: (18F)LBT999,LBT999 18F,LBT 999 18F,LBT-999 18F,(18F)LBT-999
Target:
Fecnt F-18
Cat.No: T31758
Synonym: J2.661.350G,18F-Fecnt,(18F)-Fecnt
Target:
Org 24598
Cat.No: T37699
Synonym:
Target:
JNJ-7925476 HCl
Cat.No: T27689
Synonym: JNJ-7925476,JNJ7925476,JNJ 7925476
Target:
TAS-303
Cat.No: T70615
Synonym:
Target:
Z1078601926
Cat.No: T79264
Synonym:
Target:
Bicifadine free base
Cat.No: T71772
Synonym:
Target:
GBR-12935 maleate
Cat.No: T70914
Synonym:
Target:
Maprotiline-d3 hydrochloride
Cat.No: T70960
Synonym:
Target:
(S)-5-hydroxy-6-methoxy Duloxetine maleate
Cat.No: T83888
Synonym:
Target:
PF-04449613
Cat.No: T37800
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN6552 5,7-Dimethoxyluteolin

Dopamine Receptor GPCR/G Protein; Neuroscience
5,7-Dimethoxyluteolin 是 5,7-二甲基木犀草素的一种衍生物,可以活化多巴胺转运蛋白,EC50为 3.417 μM。

天然产物

5,7-Dimethoxyluteolin
Cat.No: TN6552
Synonym:
Target: Dopamine Receptor
TargetMol Loading
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