Small Molecule Receptor Ligands for PET Studies of the Central Nervous System-Focus on G Protein Coupled Receptors

G protein-coupled receptors (GPRCs) are a class of proteins that are expressed in high abundance and are responsible for numerous signal transduction pathways in the central nervous system. Consequently, alterations in GPRC function have been associated with a wide variety of neurologic and neuropsychiatric disorders. The development of PET probes for imaging GPRCs has served as a major emphasis of PET radiotracer development and PET imaging studies over the past 30 years. In this review, a basic description of the biology of G proteins and GPRCs is provided. This includes recent evidence of the existence of dimeric and multimeric species of GPRCs that have been termed “receptor mosaics,” with an emphasis on the different GPRCs that form complexes with the dopamine D2 receptor. An overview of the different PET radiotracers for imaging the component GPRC within these different multimeric complexes of the D2 receptor is also provided.