Abstract: AimTo investigate the metabolic pathways of dipfluzine in rats. MethodsAfter an oral dose of dipfluzine (80 mg·kg^-1) to rats, urine was collected for 12 h. The metabolites of dipfluzine in urine were chromatographed and identified by LC/DAD/MS methods. ResultsIn the rat urine, there were 1-(4-fluorophenyl)-4-piperazinylbutanone and its glucuronide, 4-hydroxybenzophenone and its glucuronide, 4-fluoro-γ-hydroxybenzenebutanoic acid and its glucuronide and sulfate, diphenylmethanol and its glucuronide, dipfluzine, and benzophenone. ConclusionIn rats, dipfluzine was mainly metabolized in the pathways of N-desalkylation at 1- and 4-positions of piperazine ring. Some of metabolites were further conjugated with glucuronic acid and/or sulfuric acid.