N-(3-Chloropropyl)phenylethylamine (CPPEA) was examined as a possible prodrug of the neuromodulator trace amine beta-phenylethylamine (PEA) in rat tissues. CPPEA produced sustained elevation of PEA levels in rat brain, blood and liver. Rat brain concentrations of noradrenaline, dopamine and 5-hydroxytryptamine were decreased by administration of CPPEA.