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Acotiamide monohydrochloride trihydrate

CAS: 773092-05-0 F: C21H37ClN4O8S W: 541.06

Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibi
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Bioactivity Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory [1][2][3].
Invitro Acotiamide monohydrochloride trihydrate (10, 30, 100 μM; 1 hour) reduces expression levels of IκB-α phosphorylation in LPS- and MCP-1-stimulated macrophage cell lines[1]. Cell Viability Assay[1] Cell Line:
In Vivo Acotiamide monohydrochloride trihydrate (0.3, 1, 3 mg/kg; i.v./3, 10, 30 mg/kg; p.o.) increases the postprandial gastric motility index in a dose-dependent manner[2].Acotiamide monohydrochloride trihydrate (0.83 mg/kg; i.v.; once) inhibits AChE in rat stomach with IC50 of 1.79 μM[3]. Animal Model:
Name Acotiamide monohydrochloride trihydrate
CAS 773092-05-0
Formula C21H37ClN4O8S
Molar Mass 541.06
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Reference [1]. Hiroshi Yamawaki, et al. Acotiamide attenuates central urocortin 2-induced intestinal inflammatory responses, and urocortin 2 treatment reduces TNF-α productions in LPS-stimulated macrophage cell lines. Neurogastroenterol Motil. 2020 Aug;32(8):e13813. [2]. Matsunaga Y, et al. Acotiamide hydrochloride (Z-338), a new selective acetylcholinesterase inhibitor, enhances gastric motility without prolonging QT interval in dogs: comparison with cisapride, itopride, and mosapride. J Pharmacol Exp Ther. 2011 Mar;336(3):791-800. [3]. Kazuyoshi Y oshii, et al. Physiologically-Based Pharmacokinetic and Pharmacodynamic Modeling for the Inhibition of Acetylcholinesterase by Acotiamide, A Novel Gastroprokinetic Agent for the Treatment of Functional Dyspepsia, in Rat Stomach. Pharmaceutical Research, 33(2), 292–300.