Positron emission tomography {PET) is a nuclear medicine imaging technique which exploits the unique physical characteristics of radionuclides that decay by positron emission. These characteristics allow for in vivo quantitative measurement of three-dimensional distributions of radioactivity with a spatial resolution of 5 mm using current detector technology. In addition to these physical advantages, PET is the only imaging technique that can use the short-lived positron emitting radionuclides of the so-called “organic” elements: carbon (C-11), nitrogen (N-13), and oxygen (0–15). These elements are the building blocks of physiological compounds and can be used to study most enzymes, receptors, and other metabolically important compounds and their associated reactions. PET allows for the study of a variety of physiological and biochemical processes through the application of particular radiopharmaceuticals. PET has also been used to study the interaction of receptor-specific ligands in several receptor systems including dopaminergic, adrenergic, serotinergic, and opiod. C-11 and F-18 labeled receptor ligands have been used to study receptor selectivity and receptor concentrations in vivo. Recently, PET has been used to measure the pharmacokinetics of several novel antibiotics in humans allowing the direct measurement of tissue concentrations and correlation with classical pharmacokinetic parameters. This review discusses some of the current applications of PET in more detail.