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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 is a 5-HT4 agonist which can stimulate intestinal ACh release.

Cisapride 化学结构 CAS号：81098-60-4
Cisapride 化学结构
CAS号：81098-60-4
Cisapride 3D分子结构
CAS号：81098-60-4
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]}
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。

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

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
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

Tags: Cisapride | 81098-60-4 | R 51619 | (±)-Cisaprid | R51619 | R-51619 | 5-HT4 Agonist | GPCR/G Protein | Neuronal Signaling | Membrane Transporter/Ion Channel | 5-HT Receptor | Potassium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Cisapride 纯度/质量文件 | Cisapride 亚型比较 | Cisapride 生物活性 | Cisapride 临床数据 | Cisapride 参考文献 | Cisapride 实验方案 | Cisapride 技术信息

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