Cisapride | 西沙比利 | (±)-Cisaprid | 5-HT4 Agonist

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西沙必利 /Cisapride {[allProObj[0].p_purity_real_show]}

货号：A238567 同义名： 西沙比利 / (±)-Cisaprid;R 51619

Cisapride是一种 5-HT4 受体激动剂，IC50 为 9.4 nM，具有胃促动力作用，能刺激肠道释放乙酰胆碱。

Cisapride 化学结构
CAS号：81098-60-4

Cisapride 3D分子结构
CAS号：81098-60-4

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Cisapride 纯度/质量文件产品仅供科研

货号：A238567 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • ACS Appl. Nano Mater., 2025. Ambeed. [ A188026 ]; • Eur. J. Clin. Microbiol. Infect. Dis., 2025. Ambeed. [ A151161 ]; • JJC, 2025, 20(Special Issue)): 27-39. Ambeed. [ A713856 ]; • bioRxiv, 2025. Ambeed. [ A538667 , A714873 , A126729 , A126049 , A446054 ]; • Nature Communications, 2025, 16, 1871. Ambeed. [ A508148 ]; 更多 >

5-羟色胺受体亚型比较

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 (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM								98%
Venlafaxine	✔								99%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								99%
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	✔								97%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	99%
Fluoxetine HCl	✔								99.5%
Paroxetine HCl	✔							AChR	99%
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						95%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						99%
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						98%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	99%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pKi: 9.5 5-HT2B, pIC50: 10.4						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron HCl dihydrate				✔					98%
VUF10166				++++ 5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM					99%+
Azasetron HCl				++++ 5-HT3, IC50: 0.33 nM					99%
Asenapine maleate		+++ 5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6	++++ 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-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 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		95%
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。

Cisapride 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].

体内研究

Cisapride (0.1-1 mg/kg; i.v., once) enhances antral and colonic motility in conscious dogs^[3].

Cisapride (2 mg/kg (i.p.); 4 mg/kg, (oral administration); once) does not exhibit significant differences in macroscopic features, histopathological features, cytokine profile, or bodyweight changes compared to TNBS-treated rats^[4].

体外研究

Cisapride (1-100 nM) exhibits potent hERG blockade with an IC50 value of 9.4 nM^[1].

Cisapride (1-100 nM) demonstrates efficacy at the 5-HT4 receptor with an EC50 value of 140 nM^[1].

Cisapride demonstrates dose-dependent inhibition of Kv4.3 potassium channels expressing CHO cells, with an IC50 value of 9.8 μM, across concentrations of 0.3, 1, 3, 10, and 30 μM^[2].

Cisapride 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)	-	-

Cisapride 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.

Cisapride 实验方案

计算器

存储液制备

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

Cisapride 技术信息

CAS号	81098-60-4
分子式	C₂₃H₂₉ClFN₃O₄
分子量	465.945

别名	西沙比利 ;(±)-Cisaprid;R 51619;Propulsid;Pridesia;Presid;Prepulsid;Kinestase;Kaudalit
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

溶解方案

细胞实验：

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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

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

西沙必利 /Cisapride {[allProObj[0].p_purity_real_show]}

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Cisapride 参考文献

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