In the present review, we provide a comprehensive summary of recent pharmacological studies on dopamine transporter (DAT) inhibitors, which are potential treatments for neurodegenerative and psychiatric disorders. Extensive structure-activity relationship studies have identified numerous tropane-based ligands with high affinity and selectivity for the DAT or with high affinity to the DAT and other monoamine transporters (dual and triple monoamine reuptake inhibitors). The review covers advances in the field in past fifteen years. Among the described compounds, many appear to be promising drug candidates, while other may serve as valuable tools for research or as prototypes for new classes of selective DAT inhibitors. Special attention is being paid to separation of the DAT inhibition from NET and SERT inhibition.