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) significantly reduces IκB-α phosphorylation expression levels in LPS- and MCP-1-activated macrophage cell lines, specifically NR8383, as observed in Cell Viability Assays [1]. This treatment resulted in a noticeable decrease in the production of both TNF-α and IL-6 in these stimulated cells.

Acotiamide demonstrates a dose-dependent enhancement in postprandial gastric motility indices when administered either intravenously (0.3, 1, 3 mg/kg) or orally (3, 10, 30 mg/kg) [2]. A single intravenous dose (0.83 mg/kg) of acotiamide significantly inhibits acetylcholinesterase (AChE) activity in the rat stomach, with an IC 50 value of 1.79 μM, thereby potentially improving functional dyspepsia [3]. These findings were observed in experiments involving male mongrel dogs weighing 9-11 kg and male beagle dogs weighing 9.6-12.9 kg for the gastric motility study [2], and male Sprague-Dawley rats aged 6-7 weeks for the AChE inhibition study [3]. The results indicate acotiamide's effectiveness in increasing postprandial gastric motility and inhibiting AChE in the stomach, evidenced by detailed animal models and specific dosage administrations.