Home Neuronal Signaling 5-HT Receptor agonist Mosapride

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Mosapride 5-HT Receptor agonist

Cat.No.S4839

Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
Mosapride 5-HT Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 421.89

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Quality Control

Batch: S483901 DMSO]84 mg/mL]false]]]false]]]false Purity: 98%
98

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (199.1 mM)
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Chemical Information, Storage & Stability

Molecular Weight 421.89 Formula

C21H25ClFN3O3

 Storage (From the date of receipt)
CAS No. 112885-41-3 -- Storage of Stock Solutions

Synonyms N/A Smiles CCOC1=CC(=C(C=C1C(=O)NCC2CN(CCO2)CC3=CC=C(C=C3)F)Cl)N

Mechanism of Action

Targets/IC50/Ki
5HT4
In vitro
Mosapride facilitates acetylcholine release from the enteric cholinergic neurons. It does not block K+ channels or D2 dopaminergic receptors. This compound is a selective 5-HT4 receptor agonist with no affinity for 5-HT1, 5-HT2, adrenalineα1, adrenalineα2 or dopamine D2 receptors.
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 this compound 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 this chemical administered as single or multiple doses. It 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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