The author presents a selective and integrative overview of current research examining acute effects of abused drugs on aspects of behavioral control in humans. The review discusses the concept of behavioral control and reviews research models that examine inhibitory influences as a central mechanism of control. Evidence for drug-induced impairment of inhibitory mechanisms is reviewed from current neuroanatomical, neuropharmacological, and behavioral perspectives. Model-based laboratory assessments of behavioral control are described in terms of their application to behavioral pharmacology and evidence for alcohol and psychostimulant effects on basic inhibitory mechanisms is reviewed. Drug effects on inhibitory mechanisms are also discussed in terms of their relevance to higher-order cognitive and behavioral functions, and in relation to impulsive behaviors, such as drug abuse. The review concludes by identifying important drug-related phenomenon (e.g., drug tolerance, cue reactivity) that might also be studied in behavioral control frameworks in future research.