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G蛋白偶联受体/G蛋白
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/ 5-羟色胺受体 / Tropisetron

托烷司琼 /Tropisetron {[allProObj[0].p_purity_real_show]}

货号：A545212 同义名： SDZ-ICS-930 free base;ICS 205-930

Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

Tropisetron 化学结构 CAS号：89565-68-4
Tropisetron 化学结构
CAS号：89565-68-4
Tropisetron 3D分子结构
CAS号：89565-68-4
Tropisetron 化学结构 CAS号：89565-68-4
Tropisetron 3D分子结构 CAS号：89565-68-4
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Tropisetron 纯度/质量文件 产品仅供科研

货号：A545212 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

 		98%
Venlafaxine ✔ 98%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 98%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 98%
Fluoxetine HCl ✔ 99.5%
Paroxetine hydrochloride ✔ AChR 97%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		98%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

 		99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

 		99%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

 		99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

 		98%
Tropisetron ✔ 99%
Palonosetron ✔ 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron hydrochloride dihydrate ✔ 98%
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

 		99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

 		98%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

 		++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1B, pKi: 6.1

5-HT1D, pKi: 6

 		++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tropisetron 生物活性

靶点

  • 5-HT3
描述 Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. Tropisetron specifically inhibited both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibited both the binding to DNA and the transcriptional activity of NFAT and AP-1[3]. Tropisetron (from 0.6 to 2.4 mg/kg/infusion) attenuated compulsive behavior of rats when pressing of the seeking lever potentially led to footshock[4]. Tropisetron ameliorated renal damage due to diabetic nephropathy possibly by suppressing oxidative stress and alteration of SIRT1, FOXO3a, and claudin-1 levels[5]. Tropisetron exhibited significant inhibitory effects IL-6, CK-MB(creatine kinase isoenzyme), sST2 (soluble growth stimulating gene 2 protein) and IgE (immunoglobulin E) expression levels, and inductive effects on atrial ventricular action potential in the sepsis group[6]. Two different doses of tropisetron (5 and 10 mg/kg) or vehicle were administered intraperitoneally 30 min before pMCAO(permanent middle cerebral artery occlusion). Animals receiving tropisetron showed a significant increase (p < 0.05) in neurological deficits and mortality rate. [7].

Tropisetron 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02007798 Brain Neoplasms ... 展开 >> Surgery 收起 << Not Applicable Unknown December 2014 China, Liaoning ... 展开 >> Yue Yun Recruiting Shenyang, Liaoning, China, 110001 Contact: Yue Yun, Master    008613889168717    crazy_mouse0707@hotmail.com    Principal Investigator: Ling Pei, Ph.D. 收起 <<
NCT02479581 Valvular Heart Disease Phase 2 Completed - China, Hunan ... 展开 >> Xiangya Hospital of Central South University Changsha, Hunan, China, 410078 收起 <<
NCT03071185 Elective Reconstructive Surger... 展开 >>y Pain, Post Operative 收起 << Not Applicable Recruiting April 30, 2017 China, Liaoning ... 展开 >> School & Hospital of Stomatology, China Medical University Recruiting Shenyang, Liaoning, China, 110002 Contact: xia zhang 收起 <<

Tropisetron 参考文献

[1]Vega Lde L, Munoz E, et al. The 5-HT3 receptor antagonist tropisetron inhibits T cell activation by targeting the calcineurin pathway. Biochem Pharmacol. 2005 Aug 1;70(3):369-80.

[2]Macor JE, Gurley D, et al. The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist. Bioorg Med Chem Lett. 2001 Feb 12;11(3):319-21.

[3]Vega Lde L, Muñoz E, Calzado MA, Lieb K, Candelario-Jalil E, Gschaidmeir H, Färber L, Mueller W, Stratz T, Fiebich BL. The 5-HT3 receptor antagonist tropisetron inhibits T cell activation by targeting the calcineurin pathway. Biochem Pharmacol. 2005 Aug 1;70(3):369-80

[4]Zhou YQ, Zhang LY, Yu ZP, Zhang XQ, Shi J, Shen HW. Tropisetron Facilitates Footshock Suppression of Compulsive Cocaine Seeking. Int J Neuropsychopharmacol. 2019 Sep 1;22(9):574-584

[5]Samadi M, Aziz SG, Naderi R. The effect of tropisetron on oxidative stress, SIRT1, FOXO3a, and claudin-1 in the renal tissue of STZ-induced diabetic rats. Cell Stress Chaperones. 2021 Jan;26(1):217-227

[6]Liu Z, Zeng Z, Wu C, Liu H. Tropisetron inhibits sepsis by repressing hyper-inflammation and regulating the cardiac action potential in rat models. Biomed Pharmacother. 2019 Feb;110:380-388

[7]Candelario-Jalil E, Muñoz E, Fiebich BL. Detrimental effects of tropisetron on permanent ischemic stroke in the rat. BMC Neurosci. 2008 Feb 6;9:19

Tropisetron 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.58mL

3.52mL

1.76mL

35.17mL

7.03mL

3.52mL

Tropisetron 技术信息

CAS号89565-68-4
分子式C17H20N2O2
分子量 284.353
别名 SDZ-ICS-930 free base;ICS 205-930;ICF 205-930
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C
溶解度
动物实验配方

Tags: Tropisetron | 89565-68-4 | SDZ-ICS-930 | nAChR Agonist | GPCR/G Protein | Neuronal Signaling | Membrane Transporter/Ion Channel | 5-HT Receptor | nAChR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Tropisetron 纯度/质量文件 | Tropisetron 亚型比较 | Tropisetron 生物活性 | Tropisetron 临床数据 | Tropisetron 参考文献 | Tropisetron 实验方案 | Tropisetron 技术信息

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