D-p-hydroxyphenylglycine-L-proline was attached to L-dopa as delivery tool for improving the oral absorption. This tripeptide prodrug 1 of dopamine was well absorbed in a perfusion study in rat intestine, devoid of dopamine-like side effects on isolated smooth muscles and significantly inhibited the (+) methamphetamine-induced rotation in nigrostriatal-lesioned rats, suggesting of anti-Parkinsonism effect.