Over the past 30 years, a wide variety of radiopharmaceuticals have been proposed for the scintigraphic detection of inflammatory and infectious disease. All radiopharmaceuticals yield a functional image of a process placed somewhere in the cascade of reactions in inflammation, this being the common pathway of response to tissue injury. This paper discusses relevant aspects of the biodistribution, in vivo kinetics and mechanisms of uptake of both clinically used and experimental radiopharmaceuticals that have been proposed for the scintigraphic detection of focal inflammation and infection.