Itopride hydrochloride
(Synonyms: 盐酸伊托必利; HSR803) 目录号 : GC15895
An AChE inhibitor and a prokinetic agent
Cas No.:122892-31-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 2.04 μM
Itopride is an acetylcholinesterase (AchE) inhibitor.
Acetylcholinesterase plays key roles in the termination of impulse transmission by rapidly hydrolyzing the neurotransmitter acetylcholine in varioius cholinergic pathways in both central and peripheral nervous systems.
In vitro: Itopride was found to inhibit both AChE and horse serum butyrylcholinesterase (BuChE). The itopride IC50 against AChE was, however, 100-fold less than that against BuChE. The recovery of AChE activity inhibited by low dose of neostigmine was partial, but that inhibited by itopride was complete. Double reciprocal plots showed that both Vmax and Km were affected by itopride, indicating a "mixed" type inhibition, although primarily being an uncompetitive one. In addition, the inhibitory effect of itopride on cholinesterase (ChE) activity in guinea pig gastrointestine was much weaker than that on pure AChE [1].
In vivo: Previoius animal study showed that in conscious dogs with implanted strain gauge force transducers, itopride could stimulate contractile activity in the gastrointestinal tract from stomach to colon. Whereas, mosapride was able to stimulate contractile activity only in the gastric antrum and ileum. Moreover, in rats s andguinea pig, itopride could accelerate colonic luminal transit, however, both mosapride and cisapride failed to enhance colonic transit. Such findings suggested that itopride had a stimulatory action on propelling colonic luminal contents, colonic peristalsis, which was quite different from mosapride and cisapride [2].
Clinical trial: Itopride hydrochloride has been clinically used as a gastroprokinetic agent in several countries including Japan, for the symptomatic treatment of functional dyspepsia [2].
References:
[1] Iwanaga Y,Kimura T,Miyashita N,Morikawa K,Nagata O,Itoh Z,Kondo Y. Characterization of acetylcholinesterase-inhibition by itopride. Jpn J Pharmacol.1994 Nov;66(3):317-22.
[2] Tsubouchi T,Saito T,Mizutani F,Yamauchi T,Iwanaga Y. Stimulatory action of itopride hydrochloride on colonic motor activity in vitro and in vivo. J Pharmacol Exp Ther.2003 Aug;306(2):787-93.
| Cas No. | 122892-31-3 | SDF | |
| 别名 | 盐酸伊托必利; HSR803 | ||
| 化学名 | N-(4-(2-(dimethylamino)ethoxy)benzyl)-3,4-dimethoxybenzamide hydrochloride | ||
| Canonical SMILES | CN(CCOC1=CC=C(CNC(C2=CC(OC)=C(OC)C=C2)=O)C=C1)C.Cl | ||
| 分子式 | C20H27ClN2O4 | 分子量 | 394.89 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 1 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5324 mL | 12.6618 mL | 25.3235 mL |
| 5 mM | 0.5065 mL | 2.5324 mL | 5.0647 mL |
| 10 mM | 0.2532 mL | 1.2662 mL | 2.5324 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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