Mosapride

Catalog No.S4839

Mosapride Chemical Structure

Molecular Weight(MW): 421.89

Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

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Biological Activity

Description Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
Targets
5HT4 [1]
()
In vitro

Mosapride facilitates acetylcholine release from the enteric cholinergic neurons. It does not block K+ channels or D2 dopaminergic receptors[2]. Mosapride is a selective 5-HT4 receptor agonist with no affinity for 5-HT1, 5-HT2, adrenalineα1, adrenalineα2 or dopamine D2 receptors[3].

In vivo Mosapride augmented lower gastrointestinal motility in animal models and in patients with lower gastrointestinal disorders. It enhanced defecation responses in animal models. In human, after oral administration of single doses of mosapride 5-40 mg, peak mosapride concentrations (Cmax) were reached after about 1 hour. Both the Cmax and area under the concentration-time curve from time zero to infinity (AUC∞) increased in a dose-proportional manner. There were no significant differences in the pharmacokinetic profiles of mosapride administered as single or multiple doses. Mosapride is excreted in the urine and faeces. It is primarily metabolized in the liver by cytochrome P450 3A4 to the active metabolite, a des-4-fluorobenzyl compound[3].

Protocol

Animal Research:

[1]

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  • Animal Models: Male Hartley guinea pigs
  • Formulation: 0.5% tragacanth solution
  • Dosages: 3, 10 and 30 mg/kg
  • Administration: i.g.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (199.1 mM)

* 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 421.89
Formula

C21H25ClFN3O3

CAS No. 112885-41-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02056405 Unknown status Drug: Mosapride|Drug: Placebo Postoperative Ileus Hospital Italiano de Buenos Aires December 2015 Phase 4
NCT02106130 Completed Drug: Rebamipide|Drug: Mosapride citrate Healthy IlDong Pharmaceutical Co Ltd May 2013 Phase 1
NCT01284764 Completed Drug: Mosapride Foreign Body Left During Endoscopic Examination Inje University January 2011 Phase 3
NCT01094847 Completed Drug: DWJ1252 Bioequivalence Daewoong Pharmaceutical Co. LTD. April 2010 Phase 1

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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