The development of radiotracers for imaging sigma (σ) receptors in the central nervous system (CNS) using positron emission tomography (PET)

Abstract

Sigma (σ) receptors are unique mammalian proteins, distributed in the central nervous system and elsewhere, which are increasingly implicated in the pathophysiology of virtually all major central nervous system disorders. The heterogeneous but wide distribution of σ1 in the brain has prompted the development of selective radiotracers for imaging these sites using positron emission tomography (PET). To date, some 50 carbon-11-labelled and fluorine-18-labelled candidate PET radioligands targeting σ receptors have been reported. The historical development of selective σ1 receptor ligands as potential PET imaging agents, as well as the radiochemistry and application of the most recently developed examples, is described herein.