Positron emission tomography (PET) is a non-invasive technology of nuclear medicine that has sensitivity for tracing low picomolar concentrations of radiolabeled molecules in the human body. Radiolabeling a new drug to high specific radioactivity facilitates a detailed mapping of its distribution to crucial organs in humans after the administration of a "microdose" (< 1 microg), for which limited toxicology documentation is required. For drugs directed at the CNS, this method is particularly useful for confirming exposure to the brain. A different approach is to develop suitable radioligands for quantitative PET studies of drug binding to target proteins and subsequently to correlate receptor occupancy with pharmacodynamic responses. To follow disease progression and to monitor the outcome of new treatments, PEt also facilitates longitudinal studies of biomarkers of pathophysiology such as amyloid plaque load in Alzheimer's disease. Finally, combining genomic knowledge with PET neuroreceptor imaging is expected to facilitate the search for genetic predictors of drug response.