生物活性

• 描述Mosapride citrate, frequently used in the treatment of gastrointestinal (GI) disorders requiring gastroprokinetic efficacy, is a novel 5-HT4 agonist and partial 5-HT3 antagonist^[3]. In vitro studies, mosapride citrate, co-applied with 5-HT, could competitively block the 5-HT3 receptor current amplitudes in cultured NCB-20 cells, probably by binding to the receptor in closed statePark YS, Sung KW. Gastroprokinetic agent, mosapride inhibits 5-HT3 receptor currents in NCB-20 cells. Korean J Physiol Pharmacol. 2019 Sep;23(5):419-426. doi: 10.4196/kjpp.2019.23.5.419. Epub 2019 Aug 26. PMID: 31496879; PMCID: PMC6717790.|https://pubmed.ncbi.nlm.nih.gov/31496879/}. Besides this, it was found that mosapride could also inhibit Kv4.3 by both accelerating the rate of inactivation and activation, and thereby decreasing the time to peak{{Sung KW, Hahn SJ. Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 2013 Oct;386(10):905-16. doi: 10.1007/s00210-013-0896-6. Epub 2013 Jun 22. PMID: 23793103.|https://pubmed.ncbi.nlm.nih.gov/23793103/. In vivo studies, mosapride citrate could contribute to the reduction of the acetic acid or zymosan-induced visceromotor response to colorectal distension in rat^[4]. In addition, mosapride citrate also had the ability of suppressing methionine-choline deficient (MCD) diet-induced nonalcoholic steatohepatitis development, by reducing serum lipopolysaccharide and increasing plasma glucagon^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02982668	Severe Stroke ... more >> Acute Stroke Dysphagia Collapse <<	Not Applicable	Recruiting	December 2022	China, Shaanxi ... more >> Xijing Hospital Recruiting Xi'an, Shaanxi, China, 710032 Contact: Fang Yuan, PhD    +86-29-84771319    yuanfang@fmmu.edu.cn    Principal Investigator: Wen Jiang, PhD          Tangdu Hospital Recruiting Xi'an, Shaanxi, China, 710038 Contact: Peng Guo       1443291624@qq.com    Principal Investigator: Wei Zhang, MD          The First Affiliated Hospital of Xi'an Jiaotong University, Recruiting Xi'an, Shaanxi, China, 710061 Contact: Kang Huo, MD       huokangster@qq.com    Principal Investigator: Kang Huo, MD          Yulin No.2 Hospital Not yet recruiting Yunlin, Shaanxi, China, 719000 Contact: Wenzong Wang, MD       wwz0938@126.com    Principal Investigator: Wenzong Wang, MD Collapse <<
  NCT03600974	-	-	Not yet recruiting	July 1, 2021	-
  NCT03225248	Functional Dyspepsia	Phase 3	Completed	-	-

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• 参考文献

• [1] Nonogaki K, Kaji T. Mosapride, a selective serotonin 5-HT4 receptor agonist, and alogliptin, a selective dipeptidyl peptidase-4 inhibitor, exert synergic effects on plasma active GLP-1 levels and glucose tolerance in mice. Diabetes Res Clin Pract. 2015 Dec;110(3):e18-21.

  [2] Yoshida N, Omoya H, et al. Pharmacological effects of the new gastroprokinetic agent mosapride citrate and its metabolites in experimental animals. Arzneimittelforschung. 1993 Oct;43(10):1078-83.

  [3] Park YS, Sung KW. Gastroprokinetic agent, mosapride inhibits 5-HT3 receptor currents in NCB-20 cells. Korean J Physiol Pharmacol. 2019 Sep;23(5):419-426. doi: 10.4196/kjpp.2019.23.5.419. Epub 2019 Aug 26. PMID: 31496879; PMCID: PMC6717790.

  [4] Lee JW, Sung KW, Lee OY, Lee SE, Sohn CI. The effects of 5-HT4 receptor agonist, mosapride citrate, on visceral hypersensitivity in a rat model. Dig Dis Sci. 2012 Jun;57(6):1517-24. doi: 10.1007/s10620-012-2101-z. Epub 2012 Mar 17. PMID: 22427128.

  [5] Okubo H, Nakatsu Y, Sakoda H, Kushiyama A, Fujishiro M, Fukushima T, Matsunaga Y, Ohno H, Yoneda M, Kamata H, Shinjo T, Iwashita M, Nishimura F, Asano T. Mosapride citrate improves nonalcoholic steatohepatitis with increased fecal lactic acid bacteria and plasma glucagon-like peptide-1 level in a rodent model. Am J Physiol Gastrointest Liver Physiol. 2015 Jan 15;308(2):G151-8. doi: 10.1152/ajpgi.00198.2014. Epub 2014 Nov 26. PMID: 25428903.

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