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topride HCl

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Chemical Structure| 122892-31-3 同义名 : 盐酸伊托必利 ;HSR803;Itopride (hydrochloride);Ganaton;Itopride hydrochloride
CAS号 : 122892-31-3
货号 : A953061
分子式 : C20H27ClN2O4
纯度 : 98%
分子量 : 394.892
MDL号 : MFCD00881710
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(265.9 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

H2O: 50 mg/mL(126.62 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • AChE

    AChE, IC50:2.04 μM
描述 Itopride hydrochloride (itopride) inhibits acetylcholinesterase (AChE) and antagonizes dopamine D2 receptor, and has been used as a gastroprokinetic agent. In the ileum, itopride accelerated peristaltic velocity at higher dosage (10-10-10-6 M) and significantly shortened colonic transit[3]. Itopride 100 mg t.i.d. is effective on decreasing pathologic reflux in patient with GERD (gastro-esophageal reflux disease)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.66mL

2.53mL

1.27mL

25.32mL

5.06mL

2.53mL
参考文献

[1]Scarpellini E, Vos R, et al. The effects of itopride on oesophageal motility and lower oesophageal sphincter function in man. Aliment Pharmacol Ther. 2011 Jan;33(1):99-105.

[2]Iwanaga Y, Kimura T, et al. Characterization of acetylcholinesterase-inhibition by itopride. Jpn J Pharmacol. 1994 Nov;66(3):317-22.

[3]Lim HC, Kim YG, Lim JH, Kim HS, Park H. Effect of itopride hydrochloride on the ileal and colonic motility in guinea pig in vitro. Yonsei Med J. 2008 Jun 30;49(3):472-8.

[4]Kim YS, Kim TH, Choi CS, Shon YW, Kim SW, Seo GS, Nah YH, Choi MG, Choi SC. Effect of itopride, a new prokinetic, in patients with mild GERD: a pilot study. World J Gastroenterol. 2005 Jul 21;11(27):4210-4.