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Chemical Structure| 81098-60-4 Chemical Structure| 81098-60-4

Structure of Cisapride
CAS No.: 81098-60-4

Chemical Structure| 81098-60-4

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

Synonyms: (±)-Cisaprid; R 51619; Propulsid

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Product Details of Cisapride

CAS No. :81098-60-4
Formula : C23H29ClFN3O4
M.W : 465.95
SMILES Code : O=C(C1=CC(Cl)=C(C=C1OC)N)N[C@@H]2[C@@H](CN(CC2)CCCOC3=CC=C(C=C3)F)OC
Synonyms :
(±)-Cisaprid; R 51619; Propulsid
MDL No. :MFCD00869327

Safety of Cisapride

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H319
Precautionary Statements:P305+P351+P338

Related Pathways of Cisapride

GPCR

Isoform Comparison

Biological Activity

Description
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].

In Vitro:

Cell Line
Concentration Treated Time Description References
human liver microsomes 5 μM 30 min To investigate the metabolism pathways and major metabolites of cisapride. Results showed that cisapride is primarily metabolized by CYP3A4, forming the major metabolite norcisapride. Br J Pharmacol. 2000 Apr;129(8):1655-67
Rat proximal colon mucosa-submucosa or mucosa-only preparations 100 μM To investigate the effects of luminal 5-HT on colonic anion secretion, it was found that luminal 5-HT increased HCO3− secretion via 5-HT4 receptor activation, and was not affected by TTX or atropine. Br J Pharmacol. 2015 Oct;172(19):4655-70
HEK293 cells 19.5, 39.1, 156, 313, 625, 1250, 2500, 5000, 10000, 20000 nM Evaluate the inhibitory effect of Cisapride on hERG channels, IC50 value was 938 nM Br J Pharmacol. 2016 Oct;173(19):2819-32
HEK293 cells 0.1, 0.3, 1, 3, 10, 30, 100 nM Evaluate the inhibitory effect of Cisapride on hERG channels, IC50 value was 6.8 nM Br J Pharmacol. 2016 Oct;173(19):2819-32
iPSC-derived cardiomyocytes 0.1 μM, 1 μM, 10 μM, 100 μM 24 h To evaluate the effects of cisapride on calcium flux and QT prolongation in cardiomyocytes. Results showed that cisapride induced changes in calcium flux, manifested as QT prolongation, with some cells exhibiting Torsade's-like arrhythmias. ALTEX. 2018;35(4):441-452
Oocytes expressing HERG channels 0.133 µM To study the blocking effect of Cisapride on HERG channels, showing an IC50 of 0.133 µM. Proc Natl Acad Sci U S A. 2000 Oct 24;97(22):12329-33

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00699894 Postoperative Nausea and Vomit... More >>ing Less << Not Applicable Withdrawn(Logistical difficult... More >>ies running the study) Less << - United States, New York ... More >> Long Island Jewish Medical Center/Schneider's Children Hospital New Hyde Park, New York, United States, 11040 Less <<
NCT02524496 - Completed - -
NCT01281540 Gastroparesis Phase 4 Terminated(Sponsor request) - -
NCT01281566 Infant, Premature ... More >> Infant, Newborn Less << Phase 4 Terminated(Sponsor request) - -
NCT01281553 Gastroesophageal Reflux Phase 4 Terminated(Sponsor request) - -
NCT01286090 Gastroparesis ... More >> Diabetes Mellitus Less << Phase 4 Terminated(Sponsor request) - -

Protocol

Bio Calculators
Preparing Stock Solutions 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

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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