Abstract
Molecular imaging with PET and SPECT is a very promising methodology for the drug development because it can directly visualize the spatiotemporal distribution and interaction processes of drugs in human at the molecular level using an appropriate molecular probe. The molecular probes used in these studies include a drug radiolabeled isotopically, a dosage form incorporated a radionuclide, and a radiolabeled ligand interacted with a targeted molecule, such as receptors, transporters and enzymes. The development of these radiolabeled molecular probes requires a rational design based on the structure-biological activity-biodistribution relationship. This paper describes the concept and several examples of the drug design of molecular probes used for PET/SPECT molecular imaging for drug development research.
