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Cisapride

Cat. No. M5130
Cisapride Structure
Synonym:

R 51619; (±)-Cisaprid

Size Price Availability Quantity
5mg USD 40  USD40 In stock
10mg USD 55  USD55 In stock
50mg USD 75  USD75 In stock
100mg USD 135  USD135 In stock
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Quality Control & Documentation
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 (for reference only)
Cell Experiment
Cell lines Chinese hamster ovary cells
Preparation method The effects of mosapride and cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Mosapride and cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 and 9.8 μM, respectively.
Concentrations 9.8 μM
Incubation time
Animal Experiment
Animal models Dogs
Formulation 10% gelatin solution
Dosages 1mg/kg, 3mg/kg
Administration p.o.
Chemical Information
Molecular Weight 465.95
Formula C23H29ClFN3O4
CAS Number 81098-60-4
Solubility (25°C) 20 mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Kempf J, et al. Am J Vet Res. High-resolution manometric evaluation of the effects of cisapride and metoclopramide hydrochloride administered orally on lower esophageal sphincter pressure in awake dogs.

[2] Matsunaga Y, et.al. J Pharmacol Exp Ther. Acotiamide hydrochloride (Z-338), a new selective acetylcholinesterase inhibitor, enhances gastric motility without prolonging QT interval in dogs: comparison with cisapride, itopride, and mosapride.

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


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