产品说明书
Mosapride Citrate
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同义名 : | 莫沙必利柠檬酸盐 ;AS-4370 citrate;TAK-370 citrate;Mosapride (citrate);Gasmotin;AS-4370;TAK-370 |
| CAS号 : | 112885-42-4 | |
| 货号 : | A101355 | |
| 分子式 : | C27H33ClFN3O10 | |
| 纯度 : | 98% | |
| 分子量 : | 614.016 | |
| MDL号 : | MFCD01666680 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(171.01 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 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 ... 展开 >> Acute Stroke Dysphagia 收起 << | Not Applicable | Recruiting | December 2022 | China, Shaanxi ... 展开 >> 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 收起 << |
| NCT03600974 | - | Not yet recruiting | July 1, 2021 | - | |
| NCT03225248 | Functional Dyspepsia | Phase 3 | Completed | - | - |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.63mL 0.33mL 0.16mL |
8.14mL 1.63mL 0.81mL |
16.29mL 3.26mL 1.63mL |
| 参考文献 |
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