PET radioligands for dopamine receptors and re-uptake sites: Chemistry and biochemistry

This report, based on the past experience of European centres, offers practical guidance on the chemistry and biochemistry of PET radioligands used for the in vivo imaging of dopamine receptors and re-uptake sites. It mainly summarizes methods for the preparation of D1 and D2 receptor ligands labelled with positron-emitting radioisotopes. Some of these ligands (¹¹C-labelled SCH23390, raclopride and nomifensine, ¹⁸F-labelled butyrophenones, [⁷⁶Br]bromolisuride), which have been found useful in PET clinical investigations, have been emphasized. This report is intended as an introduction and guideline for new PET-groups who want to start research in the dopaminergic neurotransmission imaging field.