The dopamine transporter has served as the primary molecular target fo
r the development of potential pharmacotherapeutic treatments for coca
ine-abuse. The evolution of structure-activity relationships, within v
arious classes of dopamine uptake inhibitors, has provided selective m
olecular probes to study the dopamine transporter. Ultimately, the elu
cidation of structure and function of this protein will undoubtedly pr
ovide new leads toward treatment of cocaine addiction.