The application of imaging techniques to evaluate receptor binding and therapeutic drug-target occupancy in the living brain is a powerful tool in drug discovery. Here, we share an overview of the application of nuclear and functional imaging modalities to support translational studies to evaluate:

• Therapeutic compound CNS biodistribution applications for small and large candidate molecules.
• Current tools to evaluate dose-occupancy study applications in the CNS.
• Pharmacodynamic outcome measures in the absence of direct imaging measures.
• Considerations for a novel radioligand development pathway.