Cisapride_product_DataBase

Bioactivity

Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity[1][2][3][4].

Invitro

Cisapride (1-100 nM) 是一种有效的 hERG 阻断剂，IC50 值为 9.4 nM[1]。Cisapride (1-100 nM) 对 5-HT4 受体有效，EC50 值为 140 nM[1]。Cisapride (0.3，1，3，10 和 30 μM) 对 Kv4.3 的抑制作用呈剂量依赖性，IC50 值为 9.8 μM 在表达 Kv4.3 钾通道的 CHO 细胞[2]。

In Vivo

Cisapride (0.1-1 mg/kg；静脉注射，一次) 刺激清醒犬的胃窦和结肠运动[3]。Cisapride (2 mg/kg，(腹腔注射)；4 mg/kg，(口服)；一次) 与三硝基苯磺酸处理的大鼠在宏观特征、组织病理学特征、细胞因子谱和体重变化均无显著差异[4]。 Animal Model:

Name

Cisapride

CAS

81098-60-4

Formula

C23H29ClFN3O4

Molar Mass

465.95

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

Cisapride

CAS: 81098-60-4 F: C23H29ClFN3O4 W: 465.95