In Vivo Receptor Visualization and Evaluation of Receptor Occupancy with Positron Emission Tomography

Positron emission tomography (PET) is useful for noninvasive in vivo visualization of disease-related receptors, for evaluation of receptor occupancy to determine an appropriate drug dosage, and for proof-of-concept of drug candidates in translational research. For these purposes, the specificity of the PET tracer for the target receptor is critical. Here, we review work in this area, focusing on the chemical structures of reported PET tracers, their Ki/Kd values, and the physical properties relevant to target receptor selectivity. Among these physical properties, such as cLogP, cLogD, molecular weight, topological polar surface area, number of hydrogen bond donors, and pKa, we focus especially on LogD and LogP as important physical properties that can be easily compared across a range of studies. We discuss the success of PET tracers in evaluating receptor occupancy and consider likely future developments in the field.