Cisapride
- CAS No.
- 81098-60-4
- Chemical Name:
- Cisapride
- Synonyms
- Alimix;T 1341;r51619;CIPRIL;Risamal;Risamol;ACENALIN;Kaudalit;Pridesia;Propulsin
- CBNumber:
- CB9121489
- Molecular Formula:
- C23H29ClFN3O4
- Molecular Weight:
- 465.95
- MOL File:
- 81098-60-4.mol
- Modify Date:
- 2024/7/25 20:04:51
Melting point | 109.8 °C |
---|---|
Boiling point | 605.4±55.0 °C(Predicted) |
Density | 1.29±0.1 g/cm3(Predicted) |
storage temp. | Keep in dark place,Inert atmosphere,Room temperature |
solubility | DMSO: ~30 mg/mL |
form | solid |
pka | 13.01±0.40(Predicted) |
color | white |
Water Solubility | 9.319mg/L(30 ºC) |
CAS DataBase Reference | 81098-60-4(CAS DataBase Reference) |
Cisapride Chemical Properties,Uses,Production
Description
Cisapride is a gastroprokinetic useful in the treatment of reflux esophagitis, constipation, and a variety of gastro-intestinal motility disorders. Its novel mechanism of action is thought to involve the enhancement of acetylcholine release in the mysenteric plexus of the gut. It is reportedly devoid of CNS and cardiac side-effects.
Chemical Properties
White Solid
Uses
Cisapride Monohydrate is a cardioactive drug that causes prolongation of cardiac repolarization in human; selective serotonin 5-HT4 receptor agonist.
Indications
Cisapride (Propulsid) is serotonin-4 (5-HT4) receptor agonists that stimulate GI motility. Cisapride appears to act by facilitating the release of acetylcholine from the myenteric plexus. It has no antiadrenergic, antidopaminergic, or cholinergic side effects. Following oral administration, peak plasma levels occur in 1.5 to 2 hours; the drug’s half-life is 10 hours.
Definition
ChEBI: The amide resulting from formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with cis-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-amine. It has been used (as its monohydrate or as its tartrate) for the treatment of gastro-oeso hageal reflux disease and for non-ulcer dyspepsia, but its propensity to cause cardiac arrhythmias resulted in its complete withdrawal from many countries, including the U.K., and restrictions on its use elsewhere.
Biological Activity
5-HT 4 receptor agonist and gastrokinetic agent. Stimulates intestinal acetylcholine release, possibly via 5-HT 4 receptor-dependent and -independent mechanisms, leading to increased intestinal motility.
Clinical Use
Cisapride has been successfully used to treat gastroparesis and mild gastroesophageal reflux disease.
Side effects
The most frequent side effect has been diarrhea. A few patients had seizure activity that was reversible after medication was discontinued. Cisapride was pulled from the U. S. market after deaths from drug-associated cardiac arrhythmias, including ventricular tachycardia, ventricular fibrillation, torsades de pointes, and QT prolongation.
Metabolic pathway
Cisapride 14C labeled at the carbonyl carbon and 3H labeled at the fluorophenyl moiety or at the piperidine ring is investigated using some animals. N- Dealkylation at the nitrogen of the piperidine ring, resulting in the main urinary metabolite norcisapride, and aromatic hydroxylation of the fluorinated phenyl ring are the major metabolic pathways in dogs and humans. Norcisapride excretion accounts for 14% of the dose in dogs and 41-45% in humans. Minor metabolic pathways are O-dearylation of the 4- fluorophenyl group and oxidation on the piperidine ring (rat, rabbits and dogs: Lavrijsen et al. (1986)15).
Cisapride Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
OCEAN TRADING CORPORATION | +91(22) 24921669 | New Delhi, India | 6211 | 58 | Inquiry |
Euroasia Trans Continental | +91 22 56349035-36 | New Delhi, India | 519 | 47 | Inquiry |
VASUDHA PHARMA CHEM LTD | + 91-40-4476 3666 | Hyderabad, India | 26 | 58 | Inquiry |
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
Hebei Guanlang Biotechnology Co,.LTD | +86-19930503253; +8619930503252 | China | 5835 | 58 | Inquiry |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | China | 29798 | 60 | Inquiry |
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