260779-88-2
Chemical Structure
Cisapride monohydrate
Synonym(s): R 51619 monohydrate; (±)-Cisaprid monohydrate
- CAS No.: 260779-88-2
- Formula:C23H31ClFN3O5
- Molecular Weight:483.96
IUPAC Name: 4-amino-5-chloro-N-((3S,4R)-1-(3-(4-fluorophenoxy)propyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide hydrate
InChIKey: QBYYXIDJOFZORM-LBPAWUGGSA-N
SMILES: ClC1=C(N)C=C(OC)C(C(N[C@H]2[C@@H](OC)CN(CCCOC3=CC=C(F)C=C3)CC2)=O)=C1.O
Biological Activity: Cisapride (R 51619) monohydrate is an orally active, selective 5-HT4 receptor agonist with an EC50 of 140 nM. Cisapride monohydrate also acts as an hERG potassium channel blocker with an IC50 of 9.4 nM. Cisapride monohydrate exerts gastrointestinal prokinetic effects by activating 5-HT4 receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride monohydrate can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Cisapride monohydrate | 99.87% | Cisapride (R 51619) monohydrate is an orally active, selective 5-HT4 receptor agonist with an EC50 of 140 nM. Cisapride monohydrate also acts as an hERG potassium channel blocker with an IC50 of 9.4 nM. Cisapride monohydrate exerts gastrointestinal prokinetic effects by activating 5-HT4 receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride monohydrate can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis. | ||||||||||||||||||||
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References
- [1]. Kovler ML, et al. Toll-like receptor 4-mediated enteric glia loss is critical for the development of necrotizing enterocolitis. Science translational medicine. 2021 Sep 22;13(612):eabg3459.
- [2]. Keller N, et al. Cardiovascular effects of cisapride and prucalopride on human 5-HT receptors in transgenic mice. Naunyn-Schmiedeberg's archives of pharmacology. 2018 Sep;391(9):975-985.
- [3]. Sung KW, et al. Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells. Naunyn-Schmiedeberg's archives of pharmacology. 2013 Oct;386(10):905-16. [Content Brief]
- [4]. Motavallian, et al. Does Cisapride, as a 5HT4 Receptor Agonist, Aggravate the Severity of TNBS‐Induced Colitis in Rat?. Gastroenterology Research and Practice 2012.1 (2012): 362536.
- [5]. Toga T, et al. The 5-HT(4) agonists cisapride, mosapride, and CJ-033466, a Novel potent compound, exhibit different human ether-a-go-go-related gene (hERG)-blocking activities. J Pharmacol Sci. 2007 Oct;105(2):207-10. [Content Brief]
