The metabolic fate of 1-phenyl-2-(N-methyl-N-benzylamino)propane (benzphetamine) and 1-phenyl-2-(N-methyl-N-furfurylamino)propane (furfenorex) in healthy volunteers has been investigated. Nine metabolites with traces of the unchanged drug were detected in human urine after oral administration of benzphetamine, and five metabolites were found following administration of furfenorex. The major metabolites were 1-(p-hydroxyphenyl)-2-(N-benzylamino)propane for benzphetamine and 1-phenyl-2-(N-methyl-N-gamma-valerolactonylamino)propane for furfenorex. In both cases, methamphetamine, amphetamine and their hydroxylated metabolites were also excreted as minor metabolites. Identified metabolites excreted in three days after administration of benzphetamine accounted for 30-44% of the dose and those excreted after administration of furfenorex, 31-46%.