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26

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T28531 Facinicline hydrochloride

RG3487

5-HT Receptor; AChR GPCR/G Protein; Neuroscience
Facinicline hydrochloride (RG3487) 是一种口服有效的烟碱α7 receptor 部分激动剂,对人 nAChR 的 Ki 值为 6 nM。它可改善啮齿类动物的认知和感觉运动门控。它与5-HT3受体结合的 Ki 为 1.2 nM。
T8593 RU 24969

5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole

5-HT Receptor GPCR/G Protein; Neuroscience
RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole) 是 5-HT1A 和 5-HT1B 受体的选择性激动剂,Ki 值分别为 0.38 和 2.5 nM。它可减少液体消耗并增加向前运动。
T7350 Nelotanserin

1-[3-(4-溴-1-甲基-1H-吡唑-5-基)-4-甲氧基苯基]-3-(2,4-二氟苯基)脲,APD125

5-HT Receptor GPCR/G Protein; Neuroscience
Nelotanserin (APD125) 是5-HT2A 强完全逆向激动剂,5-HT2C 中等强度的部分反向激动剂和5-HT2B 的弱反向激动剂,IC50s 值分别为 1.7、79 和 791 nM。
T4266 LY334370

4-氟-N-(3-(1-甲基哌啶-4-基)-1H-吲哚-5-基)苯甲酰胺盐酸盐,LY 334370

5-HT Receptor GPCR/G Protein; Neuroscience
LY334370 是一种选择性5-HT1F 受体激动剂,Ki 值为 1.6 nM。
T7277 SB 242084

6 - 氯-2,3 - 二氢- 5 -甲基- N - [6 - [(2 - 甲基-3 - 吡啶基)氧] -3 - 吡啶基] - 1H -吲哚- 1 - 酰胺盐酸盐,SB 242084 dihydrochloride hydrate

5-HT Receptor GPCR/G Protein; Neuroscience
SB 242084 是5-HT2C 选择性抑制剂,pKi 值9.0,是一种精神活性药物和研究化学品。
T1042 Granisetron hydrochloride

盐酸格拉司琼,BRL 43694A,Granisetron HCl

5-HT Receptor GPCR/G Protein; Neuroscience
Granisetron hydrochloride (Granisetron HCl) 是一种5-HT3受体拮抗剂,可作为化疗后止吐剂。
T50011 (2-methylpropyl)({[3-(trifluoromethyl)phenyl]methyl})amine

Others Others
(2-methylpropyl)({[3-(trifluoromethyl)phenyl]methyl})amine 是一种选择性血清素受体激动剂,特异性靶向5-HT2A 和5-HT2C 受体,已被用于研究血清素在各种生理和病理条件下的作用。
T8441 Lerisetron

5-HT Receptor GPCR/G Protein; Neuroscience
Lerisetron 是5-HT3拮抗剂,与 5-HT3受体具有高亲和力(pKi:9.2)。它对尿烷麻醉大鼠的 5-HT 引发的反射性心率过缓具有抑制作用。
T1173 Tropisetron hydrochloride

SDZ-ICS 930,Tropisetron HCl,ICS 205-930,盐酸托烷司琼

5-HT Receptor GPCR/G Protein; Neuroscience
Tropisetron hydrochloride (Tropisetron HCl) 是5-HT3受体拮抗剂和α7-烟碱受体激动剂,具有抗恶心和止吐活性,对5-HT3受体的 IC50为70.1 nM。
T1478 Ondansetron hydrochloride dihydrate

盐酸昂丹司琼,SN 307,NSC 665799,GR 38032,Ondansetron hydrochloride

5-HT Receptor GPCR/G Protein; Neuroscience
Ondansetron hydrochloride dihydrate (GR 38032) 是5- HT3受体拮抗剂,可治疗化疗后的恶心和呕吐,有抗焦虑和抗精神病作用。
T50089 2-(5,7-dichloro-1H-indol-3-yl)ethan-1-amine

Others Others
2-(5,7-dichloro-1H-indol-3-yl)ethan-1-amine 是一种吲哚胺类化合物,在结构上与血清素相似。它是5-HT2A 受体的选择性激动剂,在神经科学领域具有潜在的应用。
T60330 Metapramine

Metapramine (19560 RP) 是一种三环类抗抑郁剂。Metapramine 抑制去甲肾上腺素 (norepinephrine) 的再摄取,而不影响血清素或多巴胺的再摄取。Metapramine 是 N-methyl-D-aspartic acid (NMDA) 受体复合物通道的低亲和力拮抗剂。
T50039 3-(2-aminopropyl)phenol hydrochloride

Others Others
3-(2-aminopropyl)phenol hydrochloride 是一种用作分子结构单元的苯乙胺类化合物。它是一种精神活性药物,是5-HT1A、5-HT1B 和5-HT2C 等几种血清素受体的部分激动剂,也是5-HT2A 受体的拮抗剂。
T71046 FK-1052

FK-1052 is a serotonin 3 & 4 dual receptor antagonist.
T71045 FK-1052 HCl

FK-1052 HCl is a serotonin 3 & 4 dual receptor antagonist.
T22340 Granisetron

Sustol,Granisetronum,格拉司琼,Sancuso,Kevatril

5-HT Receptor GPCR/G Protein; Neuroscience
Granisetron, a serotonin receptor (5HT-3 selective) antagonist, is used as an antinauseant and antiemetic for cancer chemotherapy.
T27675 JNJ-28583867

JNJ28583867

JNJ-28583867 is an inhibitor of histamine H(3) receptor antagonist and serotonin reuptake.
T27607 Indisetron Dihydrochloride

N3389T,Sinseron,N-3389T,N 3389T

Indisetron Dihydrochloride is a 5-HT(3) and 5-HT(4) receptor antagonist. Indisetron reduces 2-methyl-5-serotonin (HT)-induced bradycardia.
T70729 Indisetron

Indisetron is a 5-HT(3) and 5-HT(4) receptor antagonist. Indisetron reduces 2-methyl-5-serotonin (HT)-induced bradycardia.
T61011 Izuforant

Izuforant (JW1601) (Compound 24) 具有有效的抗炎和止痒活性。 Izuforant 对人血清素3受体 (h5-HT3R) 具有结合亲和力,IC50值为 9.1 μM。它也是组胺 H4 受体 (H4R) 的口服活性拮抗剂,对人 H4R 的IC50值为 36 nM。
T37246 Palonosetron N-oxide

Palonosetron N-oxide is a metabolite of the serotonin (5-HT) receptor subtype 5-HT3antagonist palonosetron .1It is also a potential impurity in palonosetron preparations.2Palonosetron N-oxide is a degradation product formed by exposure to oxidative stress. 1.Stoltz, R.A., Cyong, J.-C., Shah, A., et al.Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjectsJ. Clin. Pharmacol.44(5)520-531(2004) 2.Vishnu Murthy, M., S...
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...
T10294 AM9405

5-HT Receptor GPCR/G Protein; Neuroscience
AM9405是一种新型的外周活性大麻素1型 (CB1)和5-羟色胺3型受体激动剂。 AM9405抑制回肠和结肠的抽搐收缩,IC50分别为45.71 和 0.076 nM。AM9405 在生理条件下显着减缓小鼠肠道蠕动.
T83776 Dopamine D3 Receptor Agonist 13a

Dopamine D3 受体激动剂13a是一种Dopamine D3 受体激动剂。该化合物选择性地与Dopamine D3 受体结合,相较于Dopamine D1、D2和D4受体(Kis = 0.14、4,600、2.85和756 nM,分别)具有更高的亲和力,并且还能与血清素(5-HT)受体亚型5-HT1A、5-HT2A、5-HT2B和5-HT2C(Kis = 6、54、1.47和252 nM,分别)结合;然而,它是Dopamine D2受体的部分激动剂(EC50 = 2.26 nM,在G蛋白招募分析中)并且作为Dopamine D3受体的拮抗剂(IC50 = 4.62 nM)。在大鼠身上,当剂量为3 mg/kg时,Dopamine D3 受体激动剂13a能减少可卡因自我给药。
T36639 Donecopride (fumarate hydrate)

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value...
T38145 Eltoprazine

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of no...

化合物

Facinicline hydrochloride
Cat.No: T28531
Synonym: RG3487
Target: 5-HT Receptor, AChR
RU 24969
Cat.No: T8593
Synonym: 5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole
Target: 5-HT Receptor
Nelotanserin
Cat.No: T7350
Synonym: 1-[3-(4-溴-1-甲基-1H-吡唑-5-基)-4-甲氧基苯基]-3-(2,4-二氟苯基)脲,APD125
Target: 5-HT Receptor
LY334370
Cat.No: T4266
Synonym: 4-氟-N-(3-(1-甲基哌啶-4-基)-1H-吲哚-5-基)苯甲酰胺盐酸盐,LY 334370
Target: 5-HT Receptor
SB 242084
Cat.No: T7277
Synonym: 6 - 氯-2,3 - 二氢- 5 -甲基- N - [6 - [(2 - 甲基-3 - 吡啶基)氧] -3 - 吡啶基] - 1H -吲哚- 1 - 酰胺盐酸盐,SB 242084 dihydrochloride hydrate
Target: 5-HT Receptor
Granisetron hydrochloride
Cat.No: T1042
Synonym: 盐酸格拉司琼,BRL 43694A,Granisetron HCl
Target: 5-HT Receptor
(2-methylpropyl)({[3-(trifluoromethyl)phenyl]methyl})amine
Cat.No: T50011
Synonym:
Target: Others
Lerisetron
Cat.No: T8441
Synonym:
Target: 5-HT Receptor
Tropisetron hydrochloride
Cat.No: T1173
Synonym: SDZ-ICS 930,Tropisetron HCl,ICS 205-930,盐酸托烷司琼
Target: 5-HT Receptor
Ondansetron hydrochloride dihydrate
Cat.No: T1478
Synonym: 盐酸昂丹司琼,SN 307,NSC 665799,GR 38032,Ondansetron hydrochloride
Target: 5-HT Receptor
2-(5,7-dichloro-1H-indol-3-yl)ethan-1-amine
Cat.No: T50089
Synonym:
Target: Others
Metapramine
Cat.No: T60330
Synonym:
Target:
3-(2-aminopropyl)phenol hydrochloride
Cat.No: T50039
Synonym:
Target: Others
FK-1052
Cat.No: T71046
Synonym:
Target:
FK-1052 HCl
Cat.No: T71045
Synonym:
Target:
Granisetron
Cat.No: T22340
Synonym: Sustol,Granisetronum,格拉司琼,Sancuso,Kevatril
Target: 5-HT Receptor
JNJ-28583867
Cat.No: T27675
Synonym: JNJ28583867
Target:
Indisetron Dihydrochloride
Cat.No: T27607
Synonym: N3389T,Sinseron,N-3389T,N 3389T
Target:
Indisetron
Cat.No: T70729
Synonym:
Target:
Izuforant
Cat.No: T61011
Synonym:
Target:
Palonosetron N-oxide
Cat.No: T37246
Synonym:
Target:
Maprotiline-d3 hydrochloride
Cat.No: T70960
Synonym:
Target:
AM9405
Cat.No: T10294
Synonym:
Target: 5-HT Receptor
Dopamine D3 Receptor Agonist 13a
Cat.No: T83776
Synonym:
Target:
Donecopride (fumarate hydrate)
Cat.No: T36639
Synonym:
Target:
Eltoprazine
Cat.No: T38145
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T4429 Rauwolscine hydrochloride

Corynanthidine hydrochloride,盐酸育亨宾碱,萝芙素盐酸盐,α-Yohimbine hydrochloride,Isoyohimbine hydrochloride

Adrenergic Receptor GPCR/G Protein; Neuroscience
Rauwolscine hydrochloride (Isoyohimbine hydrochloride) 是一种高选择性的 α2 adrenergic 受体拮抗剂,Ki=12 nM。
T6S1684 8-Gingerol

Antioxidant; Antibacterial; TRP/TRPV Channel Membrane transporter/Ion channel; Microbiology/Virology; oxidation-reduction
8-Gingerol 分离自姜的根状茎,是口服有效的 TRPV1激活剂,EC50值为5.0 µM。8-Gingerol 抑制 COX-2,还能抑制体外 H. pylori 的生长。

天然产物

Rauwolscine hydrochloride
Cat.No: T4429
Synonym: Corynanthidine hydrochloride,盐酸育亨宾碱,萝芙素盐酸盐,α-Yohimbine hydrochloride,Isoyohimbine hydrochloride
Target: Adrenergic Receptor
8-Gingerol
Cat.No: T6S1684
Synonym:
Target: Antioxidant, Antibacterial, TRP/TRPV Channel
TargetMol Loading
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