Cisapride

Catalog No.S5253 Synonyms: Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid

Cisapride Chemical Structure

Molecular Weight(MW): 465.95

Cisapride is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.

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Biological Activity

Description Cisapride is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.
Targets
hERG channel [1]
()
5-HT4 receptor [1]
()
9.4 nM 140 nM(EC50)
In vitro

Cisapride is a 5-HT4 receptor agonist, also a hERG blockers[1]. It is widely used for the treatment of gastrointestinal motility dysfunctions, such as gastroesophageal reflux disorder (GERD), chronic intestinal pseudo-obstruction, and slow-transit constipation gastroparesis. Cisapride works by promoting gastrointestinal motility through stimulating the release of intestinal acetylcholine from muscarinic receptors. Cisapride inhibits Kv 4.3 channels that are stably expressed in Chinese hamster ovary (CEO) cells as well as the current in L-type Ca2+ channels of ventricular myocytes. Cisapride inhibited Kv channel current in a concentration-dependent manner independent of its own function as a selective serotonin 5-HT4-receptor agonist[2].

Protocol

Solubility (25°C)

In vitro DMSO 93 mg/mL (199.59 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 465.95
Formula

C23H29ClFN3O4

CAS No. 81098-60-4
Storage powder
in solvent
Synonyms Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01281553 Terminated Gastroesophageal Reflux Johnson & Johnson Pharmaceutical Research & Development L.L.C. September 2003 Phase 4
NCT01281553 Terminated Gastroesophageal Reflux Johnson & Johnson Pharmaceutical Research & Development L.L.C. September 2003 Phase 4
NCT01286090 Terminated Gastroparesis|Diabetes Mellitus Johnson & Johnson Pharmaceutical Research & Development L.L.C. July 2003 Phase 4
NCT01286090 Terminated Gastroparesis|Diabetes Mellitus Johnson & Johnson Pharmaceutical Research & Development L.L.C. July 2003 Phase 4
NCT01281540 Terminated Gastroparesis Johnson & Johnson Pharmaceutical Research & Development L.L.C. May 2003 Phase 4
NCT01281540 Terminated Gastroparesis Johnson & Johnson Pharmaceutical Research & Development L.L.C. May 2003 Phase 4

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID