Cisapride

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Chemical Structure| 81098-60-4 同义名 : 西沙比利 ;(±)-Cisaprid;R 51619;Propulsid;Pridesia;Presid;Prepulsid;Kinestase;Kaudalit
CAS号 : 81098-60-4
货号 : A238567
分子式 : C23H29ClFN3O4
纯度 : 98%
分子量 : 465.945
MDL号 : MFCD00869327
存储条件:

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(225.35 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

生物活性
描述 Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is also an hERG blocker with an IC50 value of 9.4 nM. It functions as a gastroprokinetic agent, stimulating gastrointestinal motor activity[1][2][3][4].
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
NCT00699894 Postoperative Nausea and Vomit... 展开 >>ing 收起 << Not Applicable Withdrawn(Logistical difficult... 展开 >>ies running the study) 收起 << - United States, New York ... 展开 >> Long Island Jewish Medical Center/Schneider's Children Hospital New Hyde Park, New York, United States, 11040 收起 <<
NCT02524496 - Completed - -
NCT01281540 Gastroparesis Phase 4 Terminated(Sponsor request) - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.73mL

2.15mL

1.07mL

21.46mL

4.29mL

2.15mL

参考文献

[1]Toga, T., Y. Kohmura, and R. Kawatsu, The 5-HT(4) agonists cisapride, mosapride, and CJ-033466, a Novel potent compound, exhibit different human ether-a-go-go-related gene (hERG)-blocking activities. J Pharmacol Sci, 2007. 105(2): p. 207-10.

[2]Sung, K.W. and S.J. Hahn, Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells. Naunyn Schmiedebergs Arch Pharmacol, 2013. 386(10): p. 905-16.

[3]Mine, Y, et al. Comparison of effect of mosapride citrate and existing 5-HT4 receptor agonists on gastrointestinal motility in vivo and in vitro. J Pharmacol Exp Ther, 1997. 283(3): p. 1000-8.

[4]Motavallian, A, et al., Does Cisapride, as a 5HT(4) Receptor Agonist, Aggravate the Severity of TNBS-Induced Colitis in Rat. Gastroenterol Res Pract, 2012. 2012: p. 362536.