Progress and Challenges in the Development of PET Ligands to Aid CNS Drug Discovery

Positron emission tomography (PET) is a quantitative molecular imaging technology based on radiotracers typically labeled with 11C and 18F that can quantify biochemical processes within the living human brain. Over the last decade, PET imaging has been increasingly used to support neuroscience drug discovery by providing direct measurement of the drug–target interaction in the brain. This article will provide an overview of the available PET tracers for clinical studies and of the recent advances in the identification of novel PET tracers, will discuss some of the challenges and limits to develop new PET tracers, and will eventually suggest future areas of interest.