title: 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.
authors.affiliation: Brain and Mind Research Institute, The University of Sydney, NSW, 2050, Australia; School of Chemistry, The University of Sydney, NSW, 2006, Australia.
authors.forename: Samuel D
authors.initials: SD
authors.lastname: Banister
authors.forename: Miral
authors.initials: M
authors.lastname: Manoli
authors.forename: Michael
authors.initials: M
authors.lastname: Kassiou
mesh_terms: D000818:Animals; D002490:Central Nervous System / Q000000981:diagnostic imaging*; D006801:Humans; D007553:Isotope Labeling; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D017480:Receptors, sigma / Q000378:metabolism*
chemical_list: D019275:Radiopharmaceuticals; D017480:Receptors, sigma
keywords: CNS; carbon-11; fluorine-18; sigma receptors