title: [¹⁸F]GE-180: a novel fluorine-18 labelled PET tracer for imaging Translocator protein 18 kDa (TSPO).
abstract: A series of tricyclic compounds have been synthesised and evaluated in vitro for affinity against Translocator protein 18 kDa (TSPO) and for preferred imaging properties. The most promising of the compounds were radiolabelled and evaluated in vivo to determine biodistribution and specificity for high expressing TSPO regions. Metabolite profiling in brain and plasma was also investigated. Evaluation in an autoradiography model of neuroinflammation was also carried out for the best compound, 12a ([(18)F]GE-180).
authors.affiliation: GE Healthcare, The Grove Centre, White Lion Road, Amersham, Bucks HP9 7LL, UK.
authors.forename: Harry
authors.initials: H
authors.lastname: Wadsworth
authors.forename: Paul A
authors.initials: PA
authors.lastname: Jones
authors.forename: Wai-Fung
authors.initials: WF
authors.lastname: Chau
authors.forename: Clare
authors.initials: C
authors.lastname: Durrant
authors.forename: Naghmeh
authors.initials: N
authors.lastname: Fouladi
authors.forename: Joanna
authors.initials: J
authors.lastname: Passmore
authors.forename: Dennis
authors.initials: D
authors.lastname: O'Shea
authors.forename: Duncan
authors.initials: D
authors.lastname: Wynn
authors.forename: Veronique
authors.initials: V
authors.lastname: Morisson-Iveson
authors.forename: Amanda
authors.initials: A
authors.lastname: Ewan
authors.forename: Mikkel
authors.initials: M
authors.lastname: Thaning
authors.forename: Dimitrios
authors.initials: D
authors.lastname: Mantzilas
authors.forename: Ingvil
authors.initials: I
authors.lastname: Gausemel
authors.forename: Imtiaz
authors.initials: I
authors.lastname: Khan
authors.forename: Andrew
authors.initials: A
authors.lastname: Black
authors.forename: Michelle
authors.initials: M
authors.lastname: Avory
authors.forename: William
authors.initials: W
authors.lastname: Trigg
mesh_terms: D000818:Animals; D002227:Carbazoles / Q000737:chemistry* / Q000378:metabolism; D005462:Fluorine Radioisotopes / Q000737:chemistry / Q000378:metabolism; D008024:Ligands; D015394:Molecular Structure; D009206:Myocardium / Q000378:metabolism; D049268:Positron-Emission Tomography; D051381:Rats; D017207:Rats, Sprague-Dawley; D018079:Receptors, GABA / Q000378:metabolism*
chemical_list: D002227:Carbazoles; D005462:Fluorine Radioisotopes; C571664:GE-180; D008024:Ligands; D018079:Receptors, GABA; C499229:TSPO protein, human