The metabolism of 1-phenyl-2-(N-benzylamino)propane (benzphetamine) in vitro was studied using rat-liver microsomes. Five metabolites were isolated from the incubation mixture and identified as 1-phenyl-2-(N-benzylamino)propane (benzylamphetamine), (1-(p-hydroxyphenyl)-2-(N-methyl-N-benzylamino)propane, 1-(p-hydroxyphenyl)-2-(N-benzylamino)propane, methamphetamine and amphetamine. This metabolism in vitro was compared with that in vivo which was reported previously. The formation of all five metabolites were catalysed by liver microsomes supplemented with NADPH and O2, and inhibited by either SKF 525-A or CO. N-Demethylation was inhibited by either 2-methyl-1,2-bis-(3-pyridyl)-1-propanone (metyrapone) or n-octylamine, while aromatic hydroxylation was inhibited by 7,8-benzoflavone and N-debenzylation was depressed by all these inhibitors. N-Demethylation was enhanced by pretreatment of rats with phenobarbitone, while aromatic hydroxylation was induced by pretreatment with 3-methylcholanthrene, and N-debenzylation was Induced by pretreatment with either phenobarbitone or 3-methylcholanthrene. These data suggested that the metabolism of benzphetamine was mediated by three slightly different enzyme systems.