Mosapride(KOREA UNITED PHARM, Inc.)(Mosapride(KOREA UNITED PHARM, Inc.)) - 药物靶点：5-HT4 receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Gastin、Mosapride、Mosapride (INN)

+ [3]

靶点

5-HT4 receptor

作用方式

激动剂

作用机制

5-HT4 receptor激动剂(5-羟色胺受体4激动剂)

治疗领域

消化系统疾病

在研适应症-

非在研适应症

消化不良

原研机构

KOREA UNITED PHARM, Inc.

在研机构-

非在研机构

KOREA UNITED PHARM, Inc.

权益机构

Eisai Co., Ltd.

Sumitomo Pharma Co., Ltd.

最高研发阶段无进展临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C21H25ClFN3O3

InChIKeyYPELFRMCRYSPKZ-UHFFFAOYSA-N

CAS号112885-41-3

关联

12

项与 Mosapride(KOREA UNITED PHARM, Inc.) 相关的临床试验

TCTR20240715011

/ Not yet recruiting临床1期IIT

A Bioequivalence study of a randomized, open-label, single dose, two-way crossover design with two-period, two-treatment and two-sequence of Mosapride Citrate Tablet 5 mg relative to GASMOTIN Originator Mosapride Citrate Tablets 5 mg in healthy Thai volunteers under fasting condition

开始日期2025-01-17

申办/合作机构

Bio-innova Co., Ltd

NCT03600974

/ Unknown statusN/AIIT

A New System for Diagnosis and Treatment of Gastroesophageal Refulx Diseases : Based on Endoscopy, pH Parameter, Impedence Parameter, High Resolution Manometry and Psychology

This is a pilot study measuring a new diagnosis and treatment system "EAISMLP" in adult patients with gastroesophageal reflux disease (GERD).

开始日期2019-02-01

申办/合作机构

首都医科大学

NL-OMON26098

/ CompletedN/AIIT

Soundscape improvement with MoSART+ to reduce neuropsychiatric symptoms in nursing home patients withdementia: a randomized controlled trial and implementationevaluation.

开始日期2018-05-01

申办/合作机构-

100 项与 Mosapride(KOREA UNITED PHARM, Inc.) 相关的临床结果

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100 项与 Mosapride(KOREA UNITED PHARM, Inc.) 相关的转化医学

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100 项与 Mosapride(KOREA UNITED PHARM, Inc.) 相关的专利（医药）

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495

项与 Mosapride(KOREA UNITED PHARM, Inc.) 相关的文献（医药）

2025-02-01·Food Chemistry

Theaflavin-3,3′-digallate (TF3) attenuated constipation by promoting gastrointestinal motility and modulating the gut microbiota: A comparative study of TF3 and the anti-constipation drug mosapride in mice

Article

作者: Yang, Mingxue ; Wu, Tingbo ; Huang, Haitao ; Li, Bo ; Wu, Yuanyuan ; Liu, Junsheng ; Wan, Xiaochun ; Jin, Leyi ; Yu, Haonan ; Tu, Youying

TF3 is a functional pigment formed during the process of black tea. This study aims to explore the anti-constipation effects of TF3 and compare its efficacy with the anti-constipation drug mosapride. Result showed that both TF3 and mosapride increased fecal water content and promoted gastrointestinal (GI) motility, but TF3 was more effective in restoring excitatory neurotransmitters like gastrin (Gas), motilin (MTL), and substance P (SP). TF3 uniquely altered the gut microbiota profile and restored the bacterial community at the phylum level. TF3 targeted specific bacteria such as Alloprevotella, Bacteroides, and Parabacteroides, while mosapride affected different bacterial groups. Significant changes in Bacteroides and Prevotellaceae UCG-001 were linked to constipation improvement. Importantly, TF3 did not synergize with mosapride in alleviating constipation. These findings highlight TF3's unique role in modulating gut microbiota to relieve constipation and suggest great potential to develop functional foods with anti-constipation properties using tea-derived polyphenols.

2024-10-21·Angewandte Chemie

Rapid Aminations of Functionalized Aryl Fluorosulfates in Water

作者: Saunders, John M. ; Aue, Donald H ; Lammert, Robert M. ; Lipshutz, Bruce H. ; Yirak, Jordan ; Saunders, John Michael ; Dismuke Rodriguez, Kylee B. ; Iyer, Karthik ; Lipshutz, Bruce Howard ; Kavthe, Rahul D. ; Aue, Donald H. ; Kavthe, Rahul ; Lammert, Robert ; Iyer, Karthik S. ; Dismuke Rodriguez, Kylee ; Yirak, Jordan R.

AbstractAryl fluorosulfates of varying complexities have been used in amination reactions in water using a new Pd oxidative addition complex (OAC‐1) developed specifically to match the needs of the fine chemicals industry, not only in terms of functional group tolerance, but also reflecting time considerations associated with these important C−N couplings. Also especially noteworthy is that they replace both PFAS‐related triflates and nonaflates, which are today out of favor due to recent government regulations. The new complex based on the BippyPhos ligand is used at low loadings and under aqueous micellar conditions. Moreover, it is easily prepared and stable to long term storage. DFT calculations on the OAC precatalyst compare well with the X‐ray structure of the crystals with π‐complexation to the aromatic system of the ligand and also confirm the NMR data showing a mixture of conformers in solution that differ from the X‐ray structure in rotation of the phenyl and t‐butyl ligand substituents. An extensive variety of coupling partners, including pharmaceutically relevant APIs, readily participate under mild and environmentally responsible reaction conditions.

2024-09-01·Naunyn-Schmiedeberg's Archives of Pharmacology

Mosapride stimulates human 5-HT4-serotonin receptors in the heart

Article

作者: Hesse, Christin ; Gergs, Ulrich ; Neumann, Joachim ; Hofmann, Britt

AbstractMosapride (4-amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl) methyl]-2-morpholinyl]-methyl] benzamide) is a potent agonist at gastrointestinal 5-HT4 receptors. Mosapride is an approved drug to treat several gastric diseases. We tested the hypothesis that mosapride also stimulates 5-HT4 receptors in the heart. Mosapride increased the force of contraction and beating rate in isolated atrial preparations from mice with cardiac overexpression of human 5-HT4-serotonin receptors (5-HT4-TG). However, it is inactive in wild-type mouse hearts (WT). Mosapride was less effective and potent than serotonin in raising the force of contraction or the beating rate in 5-HT4-TG. Only in the presence of cilostamide (1 μM), a phosphodiesterase III inhibitor, mosapride, and its primary metabolite time dependently raised the force of contraction under isometric conditions in isolated paced human right atrial preparations (HAP, obtained during open heart surgery). In HAP, mosapride (10 μM) reduced serotonin-induced increases in the force of contraction. Mosapride (10 µM) shifted the concentration–response curves to serotonin in HAP to the right. These data suggest that mosapride is a partial agonist at 5-HT4-serotonin receptors in HAP.

100 项与 Mosapride(KOREA UNITED PHARM, Inc.) 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D08236	Mosapride(KOREA UNITED PHARM, Inc.)	-	DB11675

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
消化不良	临床3期	-	KOREA UNITED PHARM, Inc.	2014-11-05

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


UEGW2022	N/A	胃食管反流	-	Mosapride citrate + Esomeprazole 40mg	遞鏇獵壓獵鬱鑰鹹鏇壓(窪艱觸觸膚餘膚蓋糧襯) = 鹹製蓋範淵願範網鬱築蓋衊築願夢鏇鏇構構餘 (襯遞鹽獵製窪鹹膚製積 )	积极	2022-10-09
DDW2022	N/A	消化不良 hydrogen \| methane	-	Mosapride 15mg/day	餘衊鏇製艱膚製憲選壓(糧願選夢齋網夢鏇願積) = 鏇艱構觸選獵膚鹽餘積構膚顧構範齋齋齋艱蓋 (繭蓋艱糧窪蓋夢鹹選夢 )	不佳	2022-05-22
DDW2022	N/A	消化不良 hydrogen \| methane	-	Rifaximin 1200mg/day	餘衊鏇製艱膚製憲選壓(糧願選夢齋網夢鏇願積) = 憲遞鑰艱觸窪網繭鑰壓構膚顧構範齋齋齋艱蓋 (繭蓋艱糧窪蓋夢鹹選夢 )	不佳	2022-05-22