Details
Stereochemistry | RACEMIC |
Molecular Formula | C21H25ClFN3O3.C6H8O7 |
Molecular Weight | 614.016 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CC(O)(CC(O)=O)C(O)=O.CCOC1=CC(N)=C(Cl)C=C1C(=O)NCC2CN(CC3=CC=C(F)C=C3)CCO2
InChI
InChIKey=HUZTYZBFZKRPFG-UHFFFAOYSA-N
InChI=1S/C21H25ClFN3O3.C6H8O7/c1-2-28-20-10-19(24)18(22)9-17(20)21(27)25-11-16-13-26(7-8-29-16)12-14-3-5-15(23)6-4-14;7-3(8)1-6(13,5(11)12)2-4(9)10/h3-6,9-10,16H,2,7-8,11-13,24H2,1H3,(H,25,27);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)
Mosapride is a gastroprokinetic agent, a 5-HT4 receptor agonist and 5-HT3 receptor antagonist exhibiting no activity at dopamine D2, 5-HT1 and 5-HT2 receptors. Mosapride stimulates serotonin receptor in the digestive tract and increases acetylcholine release to promote upper digestive tract (stomach and duodenum) and lower digestive tract (colon) motility.
It is usually used to treat heartburn, nausea and vomiting caused by chronic gastritis. Mosapride is approved and marketed in the countires of Asia and Latin America.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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6.2 null [pKi] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | MOSAPRIDE CITRATE TABLETS 2.5mg "DSEP" Approved UseMOSAPRIDE CITRATE TABLETS 2.5mg "DSEP" are usually used to treat heartburn, nausea and vomiting caused by chronic gastritis. |
PubMed
Title | Date | PubMed |
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[Comparative study on treatment of diabetic gastroparesis by acupuncture and Western medicine]. | 2005 Apr |
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Effects of mosapride, a 5-hydroxytryptamine 4 receptor agonist, on electrical activity of the small intestine and cecum in horses. | 2005 Aug |
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Increased gastric motility during 5-HT4 agonist therapy reduces response fluctuations in Parkinson's disease. | 2005 Dec |
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Clinical outcomes and management of mechanism-based inhibition of cytochrome P450 3A4. | 2005 Mar |
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Simultaneous quantification of fexofenadine and pseudoephedrine in human plasma by liquid chromatography/tandem mass spectrometry with electrospray ionization: method development, validation and application to a clinical study. | 2006 |
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The effect of mosapride on esophageal motility and bolus transit in asymptomatic volunteers. | 2006 Apr |
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[Serotonin 5- HT4 receptor agonist (mosapride citrate)]. | 2006 Aug |
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Simultaneous quantification of cilostazol and its primary metabolite 3,4-dehydrocilostazol in human plasma by rapid liquid chromatography/tandem mass spectrometry. | 2006 Feb |
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Effects of mosapride citrate on patients after vagal nerve preserving distal gastrectomy reconstructed by interposition of a jejunal J pouch with a jejunal conduit for early gastric cancer. | 2006 Feb |
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Enantioselective determination of a gastroprokinetic drug using amylose tris-(3,5-dimethylphenylcarbamate) as a stationary phase by HPLC. | 2006 Feb 13 |
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Mosapride improves food intake, while not worsening glycemic control and obesity, in ob/ob obese mice with decreased gastric emptying. | 2006 Jan-Feb |
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Acid regurgitation associated with persistent cough after pulmonary resection: an observational study. | 2006 Nov 14 |
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[Effects of acute hypobaric hypoxia on gastric emptying and intestinal propulsion: experiment with rats]. | 2006 Sep 12 |
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[Determination of mosapride in human plasma by high performance liquid chromatography tandem mass spectrometry]. | 2007 Aug |
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Meta-analysis of the effects of prokinetic agents in patients with functional dyspepsia. | 2007 Mar |
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Quantification of pseudoephedrine in human plasma by LC-MS/MS using mosapride as internal standard. | 2007 Mar |
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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. | 2007 Oct |
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Treatment of functional dyspepsia with serotonin agonists: a meta-analysis of randomized controlled trials. | 2007 Oct |
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Effect of mosapride on gastrointestinal transit time and diagnostic yield of capsule endoscopy. | 2007 Oct |
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Liquid chromatography-tandem mass spectrometric method for determination of mosapride citrate in equine tissues. | 2007 Oct 15 |
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Thermal care of functional dyspepsia based on bicarbonate-sulphate-calcium water: a sequential clinical trial. | 2007 Sep |
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Prokinetics influence the pharmacokinetics of rabeprazole. | 2008 |
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Efficacy of prokinetic agents in improving bowel preparation for colonoscopy. | 2008 |
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Mosapride in gastrointestinal disorders. | 2008 |
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A new possibility for repairing the anal dysfunction by promoting regeneration of the reflex pathways in the enteric nervous system. | 2008 Apr |
|
5-Amino-6-chloro-N-[(1-isobutylpiperidin-4-yl)methyl]-2-methylimidazo[1,2-alpha]pyridine-8-carboxamide (CJ-033,466), a novel and selective 5-hydroxytryptamine4 receptor partial agonist: pharmacological profile in vitro and gastroprokinetic effect in conscious dogs. | 2008 Apr |
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Quantitative determination of domperidone in human plasma by ultraperformance liquid chromatography with electrospray ionization tandem mass spectrometry. | 2008 Apr |
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Frequency scale symptoms for gastroesophageal reflux disease (Frequency Scale for Symptoms of GERD) predicts need for addition of prokinetics to proton pump inhibitor therapy. | 2008 Aug |
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Effects of milnacipran on binge eating - a pilot study. | 2008 Feb |
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The effect of mosapride citrate on proximal and distal colonic motor function in the guinea-pig in vitro. | 2008 Feb |
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Role of ion channel modifiers in reversal of morphine-induced gastrointestinal inertia by prokinetic agents in mice. | 2008 Jan |
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High-performance liquid chromatography and thin-layer chromatography for the simultaneous quantitation of rabeprazole and mosapride in pharmaceutical products. | 2008 Jan |
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The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. | 2008 Jul |
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The in vivo gastrointestinal activity of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. | 2008 Jul |
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Multiple system atrophy and impaired gallbladder emptying. | 2008 Jul 15 |
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The prokinetic effect of mosapride citrate on horse gastric emptying rates. | 2008 Jun |
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Effect of itopride hydrochloride on the ileal and colonic motility in guinea pig in vitro. | 2008 Jun 30 |
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Long-term Ultrasonographic Follow-up Study of Gastric Motility in Patients with Functional Dyspepsia. | 2008 Mar |
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Effects of mosapride citrate on patients after vagal nerve, lower esophageal sphincter, and pyloric sphincter-preserving nearly total gastrectomy reconstructed by jejunal J pouch interposition, and postoperative quality of life. | 2008 Mar-Apr |
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Frequency scale for symptoms of gastroesophageal reflux disease predicts the need for addition of prokinetics to proton pump inhibitor therapy. | 2008 May |
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Effect of mosapride on recovery of intestinal motility after hand-assisted laparoscopic colectomy for carcinoma. | 2008 Nov |
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Validation of 13C-acetic acid breath test by measuring effects of loperamide, morphine, mosapride, and itopride on gastric emptying in mice. | 2008 Oct |
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Choledochoscope manometry about different drugs on the Sphincter of Oddi. | 2008 Oct 14 |
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Acotiamide hydrochloride (Z-338), a novel prokinetic agent, restores delayed gastric emptying and feeding inhibition induced by restraint stress in rats. | 2008 Sep |
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Impaired gastric motility and its relationship to reflux symptoms in patients with nonerosive gastroesophageal reflux disease. | 2009 |
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Effectiveness of prokinetic agents against diseases external to the gastrointestinal tract. | 2009 Apr |
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Effects of mosapride citrate, metoclopramide hydrochloride, lidocaine hydrochloride, and cisapride citrate on equine gastric emptying, small intestinal and caecal motility. | 2009 Apr |
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Characterization of metabolic profile of mosapride citrate in rat and identification of two new metabolites: Mosapride N-oxide and morpholine ring-opened mosapride by UPLC-ESI-MS/MS. | 2009 Aug 15 |
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The plasticity of the defecation reflex pathway in the enteric nervous system of guinea pigs. | 2009 Feb |
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Rapid effect of mosapride citrate, 5-HT4 receptor agonist, on fasting blood glucose in Type 2 diabetes patients. | 2009 Jul-Aug |
Patents
Sample Use Guides
In general, for adults, take 2 tablets (5 mg of mosapride citrate) at a time, 3 times a day, before or after meal.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21333625
Mosapride (1-10 uM) enhanced differentiation of neural networks in ES gut-like organ from mouse ES cells.
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