Acotiamide is an orally active, selective and reversible acetylcholinesterase ( AChE ) inhibitor, with IC 50 of 1.79 μM. Acotiamide is a gastroprokinetic agent that enhances gastric contractility and accelerates delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory [1] [2] [3].

Acotiamide (10, 30, 100 μM; 1 hour) decreases expression levels of IκB-α phosphorylation in LPS- and MCP-1-stimulated macrophage cell lines [1]. Cell Viability Assay [1] Cell Line: NR8383, macrophage Concentration: 10, 30, 100 μM Incubation Time: 1 hour Result: Significantly reduced both TNF-α and IL-6 productions in LPS/MCP-1-stimulated NR8383 cells.

Acotiamide (0.3, 1, 3 mg/kg; i.v./3, 10, 30 mg/kg; p.o.) increases the index of postprandial gastric motility in a dose-dependent manner [2]. Acotiamide (0.83 mg/kg; i.v.; once) inhibits AChE in rat stomach with IC 50 of 1.79 μM [3]. Animal Model: Male mongrel dogs (9-11 kg), Male beagle dogs (9.6-12.9 kg) [2] Dosage: 0.3, 1, 3, 10, 30 mg/kg Administration: Intravenous injection; once Result: Increased the postprandial gastric motility. Animal Model: Male Sprague-Dawley rats (aged 6-7 weeks) [3] Dosage: 0.83 mg/kg Administration: Intravenous injection; once. Result: Effectively improved functional dyspepsia by inhibiting AChE in rat stomach.