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Cisapride

Cat. No. M5130
Cisapride Structure
Synonym:

R 51619; (±)-Cisaprid

Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 240 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50 of 9.4 × 10-9 M. Cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 9.8 uM In vivo: Cisapride (1 mg/kg i.v.), when administered 10 min after the start of GR113808 infusion, did not stimulate either antral or colonic motor activity under treatment with GR113808. The enhanced antral or colonic motor activity induced by these drugs was antagonized by treatment with GR113808 in dogs. Cisapride could not bring about more colitis damages through 5HT(4) receptors. Based on the present study further researches are required for investigating the exact roles of 5HT(4) receptors in the pathogenesis of ulcerative colitis.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Dogs
Formulation 10% gelatin solution
Dosages 1mg/kg, 3mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 465.95
Formula C23H29ClFN3O4
CAS Number 81098-60-4
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

High-resolution manometric evaluation of the effects of cisapride and metoclopramide hydrochloride administered orally on lower esophageal sphincter pressure in awake dogs.
Kempf J, et al. Am J Vet Res. 2014 Apr;75(4):361-6. PMID: 24669921.

Acotiamide hydrochloride (Z-338), a new selective acetylcholinesterase inhibitor, enhances gastric motility without prolonging QT interval in dogs: comparison with cisapride, itopride, and mosapride.
Matsunaga Y, et.al. J Pharmacol Exp Ther. 2011 Mar;336(3):791-800. PMID: 21123674.

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  Catalog
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Keywords: Cisapride, R 51619; (±)-Cisaprid supplier, 5-HT Receptor, inhibitors

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