Dopamine plays a predominant role in establishment and maintenance of addiction. The precise mechanism involved in this process however is unclear. An important reason for our lack of knowledge is difficulties associated with measurement of dopamine release in healthy human brain. To address this problem we recently developed a novel neurotransmitter imaging technique called the single scan dynamic molecular imaging technique. The technique allows us to detect, map and measure dopamine released acutely (phasic release) in the live human brain during performance of a cognitive or behavioral task. It can be used to detect dopamine released at rest (tonic release). The technique exploits the competition between endogenously released dopamine and dopamine receptor ligand for occupancy of the same receptor site. Using this technique we are currently studying dopamine neurotransmission in people with opiate addiction and compared it with those of non-addict healthy volunteers. This study has allowed us to characterize the nature of dysregulated dopamine neurotransmission in addiction. Results of this ongoing study and their possible use in development of novel therapeutic strategies for treatment of addictive disorders will be discussed.