Piperine (1), an alkaloid of blade and long peppers, inhibited gastric empt
ying (GE) of solids/liquids in rats and gastrointestinal transit (GT) in mi
ce in a dose and time dependent manner. Compound 1 significantly inhibited
GE of solids and GT at the doses extrapolated from humans (1 mg/kg and 1.3
mg/kg p.o. in rats and mice, respectively). However, at the same dose the e
ffect was insignificant for GE of liquids, One week oral treatment of 1 mg/
kg and 1.3 mg/kg in rats and mice, respectively, did not produce a signific
ant change in activity as compared to single dose administration. GE inhibi
tory activity of 1 is independent of gastric acid and pepsin secretion.