产品说明书

Tropisetron

Print
Chemical Structure| 89565-68-4 同义名 : SDZ-ICS-930 free base;ICS 205-930;ICF 205-930
CAS号 : 89565-68-4
货号 : A545212
分子式 : C17H20N2O2
纯度 : 99%
分子量 : 284.353
MDL号 : MFCD00864399
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
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].
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 <<
实验方案
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
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