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抑制剂/激动剂
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/ Mosapride Citrate

枸橼酸莫沙比利 /Mosapride Citrate {[allProObj[0].p_purity_real_show]}

货号：A101355 同义名： 莫沙必利柠檬酸盐 / AS-4370 citrate;TAK-370 citrate

Mosapride Citrate是选择性 5HT4 激动剂，又是 5HT3 拮抗剂，用作胃动力药。

Mosapride Citrate 化学结构 CAS号：112885-42-4
Mosapride Citrate 化学结构
CAS号：112885-42-4
Mosapride Citrate 3D分子结构
CAS号：112885-42-4
Mosapride Citrate 化学结构 CAS号：112885-42-4
Mosapride Citrate 3D分子结构 CAS号：112885-42-4
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Mosapride Citrate 纯度/质量文件 产品仅供科研

货号：A101355 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 5-HT ↓ 5-HT1 ↓ 5-HT2 ↓ 5-HT3 ↓ 5-HT5 ↓ 5-HT6 ↓ 5-HT7 ↓ 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

 		98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

 		98%
Venlafaxine ✔ 99%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 99%
Ziprasidone HCl ✔ 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

 		98%
Dapoxetine HCl ✔ 97%
Trazodone ✔ 98+%
Clomipramine HCl ✔ 98%
Mirtazapine ✔ 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

 		97%
Duloxetine ✔ 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 99%
Fluoxetine HCl ✔ 99.5%
Paroxetine HCl ✔ AChR 99%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		95%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

 		99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

 		98%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

 		98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

 		99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

 		98%
Tropisetron ✔ 99%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron HCl dihydrate ✔ 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

 		99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

 		99%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

5-HT5A, pKi: 8.84

 		++++

5-HT6, pKi: 9.6

 		++++

5-HT7, pKi: 9.94

 		97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

 		++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

 		+

5-HT5A, Ki: 206 nM

 		++

5-HT7, Ki: 6.6 nM

 		98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

 		99%+
Intepirdine ++++

5-HT6, pKi: 9.63

 		99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

 		98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

 		++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

 		+

5-HT6, pKi: 5.9

 		+

5-HT7, pKi: 6.3

 		95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Mosapride Citrate 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].

Mosapride Citrate 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 - -

Mosapride Citrate 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.

Mosapride Citrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.63mL

0.33mL

0.16mL

8.14mL

1.63mL

0.81mL

16.29mL

3.26mL

1.63mL

Mosapride Citrate 技术信息

CAS号112885-42-4
分子式C27H33ClFN3O10
分子量 614.016
别名 莫沙必利柠檬酸盐 ;AS-4370 citrate;TAK-370 citrate;Mosapride (citrate);Gasmotin;AS-4370;TAK-370
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Inert atmosphere,Room temperature
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方

Tags: Mosapride | 112885-42-4 | TAK-370 | AS-4370 | TAK370 | TAK 370 | AS4370 | AS 4370 | 5HT4 Agonist | GPCR/G Protein | Neuronal Signaling | Membrane Transporter/Ion Channel | Metabolic Enzyme/Protease | 5-HT Receptor | Potassium Channel | Cytochrome P450 | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Mosapride Citrate 纯度/质量文件 | Mosapride Citrate 亚型比较 | Mosapride Citrate 生物活性 | Mosapride Citrate 临床数据 | Mosapride Citrate 参考文献 | Mosapride Citrate 实验方案 | Mosapride Citrate 技术信息

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