RT Journal Article SR Electronic T1 Metabolism of Selegiline in Humans JF Drug Metabolism and Disposition JO Drug Metab Dispos FD American Society for Pharmacology and Experimental Therapeutics SP 657 OP 662 VO 25 IS 6 A1 Ho-Sang Shin YR 1997 UL http://dmd.aspetjournals.org/content/25/6/657.abstract AB Nine urinary metabolites of selegiline hydrochloride [N-methyl-N-propargyl(2-phenyl-1-methyl)ethylammonium chloride], a monoamine oxidase inhibitor, after administration to humans were identified. Their identities were confirmed by comparison of the spectra from GC/MS of peaks with those of authentic compounds. The following metabolites and unchanged drug (selegiline) were detected in urine: (R)-desmethylselegiline, (R)-methamphetamine, (R)-amphetamine, (1S,2R)-norephedrine, (1R,2R)-norpseudoephedrine, (1S,2R)-ephedrine, (1R,2R)-pseudoephedrine, (R)-p-hydroxyamphetamine, and (R)-p-hydroxymethamphetamine. The metabolites excreted 2 days after administration of 2.5–10 mg of selegiline hydrochloride amounted to 44–58% of the dose. Selegiline was metabolized by three distinct pathways: N-dealkylation, β-carbon hydroxylation, and ring-hydroxylation. The major metabolite was (R)-methamphetamine. During metabolism, no racemic transformation occurred and β-carbon hydroxylation showed apparently product stereoselectivity. The American Society for Pharmacology and Experimental Therapeutics