This publication provides an overview of central nervous system (CNS) radiotracer development, discussing different aspects and stages of development. Non-invasive neuroimaging with radiotracers can provide functional information at the cellular level and contributes substantially to understanding the complex mechanisms of the functioning and pathophysiological processes in the human brain and is useful in certain diseases for patient stratification, treatment response monitoring and as an aided technique for drug development. The success of the development of clinically significant radiotracers depends on many factors such as the selected biological target, specificity and affinity of the radio ligand, pharmacokinetics of radiotracer and others. The information provided in the document will be useful to researchers, students and professionals engaged in the development and deployment of CNS radiotracers for clinical, research or drug development applications.