title: Radioligand development for molecular imaging of the central nervous system with positron emission tomography.
abstract: Positron emission tomography (PET) is routinely used to support the development of drugs to treat neurological and psychiatric disorders. PET radioligands must not only be selective for the target of interest but must also possess a range of physicochemical and pharmacological characteristics that allow them to be radiolabelled with short-lived positron-emitting isotopes, safely administered to humans, and for the degree of target binding to be quantified in vivo. We review the ligand development process, including target selection, radioligand discovery (in vitro and preclinical evaluation), radiochemistry and evaluation in humans.
authors.affiliation: Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche, Grenzacherstrasse 124, CH-4070 Basel, Switzerland.
authors.forename: Michael
authors.initials: M
authors.lastname: Honer
authors.affiliation: Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche, Grenzacherstrasse 124, CH-4070 Basel, Switzerland.
authors.forename: Luca
authors.initials: L
authors.lastname: Gobbi
authors.affiliation: Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche, Grenzacherstrasse 124, CH-4070 Basel, Switzerland.
authors.forename: Laurent
authors.initials: L
authors.lastname: Martarello
authors.affiliation: Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche, Grenzacherstrasse 124, CH-4070 Basel, Switzerland. Electronic address: robert.comley@roche.com.
authors.forename: Robert A
authors.initials: RA
authors.lastname: Comley
mesh_terms: D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D055808:Drug Discovery; D006801:Humans; D007880:Legislation, Drug; D008024:Ligands; D057054:Molecular Imaging; D049268:Positron-Emission Tomography; D011868:Radioisotopes / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000737:chemistry
chemical_list: D008024:Ligands; D011868:Radioisotopes; D019275:Radiopharmaceuticals