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Itopride hydrochloride

Catalog No.GC15895

AChE inhibitor

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Itopride hydrochloride Chemical Structure

Cas No.: 122892-31-3

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 122892-31-3 SDF
Chemical Name 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
Formula C20H27ClN2O4 M.Wt 394.89
Solubility DMF: 1 mg/ml,DMSO: 1 mg/ml,PBS (pH 7.2): 10 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 11 reference(s) in Google Scholar.)

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