Dopamine (DA) is involved in drug reinforcement, but its role in drug addiction remains unclear. Positron emission tomography (PET) is the first technology used for the direct measurement of components of the dopaminergic system in the living human brain. In this article, we reviewed the major findings of PET imaging studies on the involvement of DA in drug addiction, especially in heroin addiction. Furthermore, we summarized PET radiotracers that have been used to study the role of DA in drug addiction. To investigate presynaptic function in drug addiction, PET tracers have been developed to measure DA synthesis and transport. For the investigation of postsynaptic function, several radioligands targeting dopamine one (D1) receptor and dopamine two (D2) receptor are extensively used in PET imaging studies. Moreover, we also summarized the PET imaging findings of heroin addiction studies, including heroin-induced DA increases and the reinforcement, role of DA in the long-term effects of heroin abuse, DA and vulnerability to heroin abuse and the treatment implications. PET imaging studies have corroborated the role of DA in drug addiction and increase our understanding the mechanism of drug addiction. Anat Rec, 295:722-733, 2012. V C 2012 Wiley Periodicals, Inc.Key words: positron emission tomography; dopamine; dopamine receptor; drug addiction; heroin BRAIN DOPAMINERGIC SYSTEM Dopamine (DA) is a catecholamine neurotransmitter in the nervous system that permits individual nerve fibers (neurons) to communicate with each other. DA has many functions in the brain, including important roles in behavior and cognition, voluntary movement, motivation, punishment and reward, sleep, mood, attention, working memory, and learning (Smythies, 2005).