Home Neuronal Signaling 5-HT Receptor agonist Cisapride hydrate For research use only.

Cisapride hydrate

Synonyms: Propulsid, Alimix, Propulsin, Enteropride, Kinestase

Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.

Cisapride hydrate Chemical Structure

Cisapride hydrate Chemical Structure

CAS No. 260779-88-2

Purity & Quality Control

Cisapride hydrate Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells Function assay Inhibition of human ERG in MCF7 cells, IC50=0.00646 μM 19110341
HEK293 cells Function assay Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method, IC50=0.01 μM 19260734
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.03981 μM 18448342
Click to View More Cell Line Experimental Data

Biological Activity

Description Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.
Targets
5-HT4 receptor [1]
(Cell-free assay)		 hERG [1]
(Cell-free assay)
0.483 μM <1 μM
In vitro
In vitro Cisapride inhibits vascular Kv current independently of serotonin 5-HT4-receptor activation[2]. As HERG channel blocker, cisapride, can inhibit the growth of gastric cancer cells by altering distribution of cell cycle and inducing apoptosis so as to be of potential value in the treatment of gastric cancer. Cisapride could inhibit the growth and clonogenicity of human gastric cancer lines by specific blockage of HERG channel in a time- and dose-dependent manner while has little effects on GES cells[3].
Cell Research Cell lines The human gastric cancer SGC7901, AGS, MGC803 and MKN45 cell lines and human immortalized gastric epithelial GES cell line
Concentrations 0, 12.5, 25, 50, 100 or 200 nM
Incubation Time 1, 3, 5 and 7 day
Method Cells in the logarithmic growth phase are harvested and seeded in 96-well plates. The cell number is diluted to 5000/well in 200 microliters of RPMI1640 medium. In vitro experiments are carried out on the gastric cancer cell lines and GES cell line, using an MTT proliferation assay. MTT stains live cells, and the optical density absorbance at 490nm wavelength correlates with the cell number. Cisapride is added to the cells at concentrations of 0, 12.5, 25, 50, 100 or 200 nM and equivalent volume of ethanol is added as control in order to eliminate the effects of solvent. Twenty microliters of MTT is added to each well of the cell culture 4 h before termination of the culture at 37˚C. One hundred and fifty microliters of dimethyl sulfoxide is added to each well at the end of the culture and the plate is agitated for 10 minutes. The absorbency at 490 nm is read by a BIOHIT BP800 plate reader. Growth curve is drawn according to MTT colorimetry. The inhibition rate is calculated.
In Vivo
In vivo Cisapride is widely prescribed for the treatment of gastrointestinal motility dysfunctions, such as gastroesophageal reflux disorder (GERD), chronic intestinal pseudo-obstruction, and slow-transit constipation gastroparesis. Although cisapride is a beneficial prokinetic agent, several common side effects, such as abdominal pain, nausea, diarrhea, and increased frequency of urination, have been reported[2]. In rat, the PK profile indicate the T1/2 for cisapride is 1.48 h[1].
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 5 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 483.96 Formula

C23H29ClFN3O4.H2O
CAS No. 260779-88-2 SDF Download Cisapride hydrate SDF
Smiles COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F.O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 96 mg/mL ( (198.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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