title: Exploration of the structure-activity relationship of a novel tetracyclic class of TSPO ligands-potential novel positron emitting tomography imaging agents.
abstract: A series of novel TSPO ligands based on the tetracyclic class of translocator protein (TSPO) ligands first described by Okubo et al. was synthesised and evaluated as potential positron emitting tomography (PET) ligands for imaging TPSO in vivo. Fluorine-18 labelling of the molecules was achieved using direct radiolabelling or synthon based labelling approaches. Several of the ligands prepared have promising profiles as potential TSPO PET imaging ligands.
authors.affiliation: GE Healthcare, The Grove Centre, White Lion Road, Amersham, Bucks HP7 9LL, UK.
authors.forename: Dennis
authors.initials: D
authors.lastname: O'Shea
authors.forename: Rabia
authors.initials: R
authors.lastname: Ahmad
authors.forename: Erik
authors.initials: E
authors.lastname: Årstad
authors.forename: Michelle
authors.initials: M
authors.lastname: Avory
authors.forename: Wai-Fung
authors.initials: WF
authors.lastname: Chau
authors.forename: Clare
authors.initials: C
authors.lastname: Durrant
authors.forename: Ella
authors.initials: E
authors.lastname: Hirani
authors.forename: Paul A
authors.initials: PA
authors.lastname: Jones
authors.forename: Imtiaz
authors.initials: I
authors.lastname: Khan
authors.forename: Sajinder K
authors.initials: SK
authors.lastname: Luthra
authors.forename: Dimitrios
authors.initials: D
authors.lastname: Mantzilas
authors.forename: Véronique
authors.initials: V
authors.lastname: Morisson-Iveson
authors.forename: Joanna
authors.initials: J
authors.lastname: Passmore
authors.forename: Edward G
authors.initials: EG
authors.lastname: Robins
authors.forename: Bo
authors.initials: B
authors.lastname: Shan
authors.forename: Harry
authors.initials: H
authors.lastname: Wadsworth
authors.forename: Sarah
authors.initials: S
authors.lastname: Walton
authors.forename: Yongjun
authors.initials: Y
authors.lastname: Zhao
authors.forename: William
authors.initials: W
authors.lastname: Trigg
mesh_terms: D000818:Animals; D005462:Fluorine Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling / Q000379:methods; D008024:Ligands; D049268:Positron-Emission Tomography / Q000379:methods*; D021381:Protein Transport; D051381:Rats; D018079:Receptors, GABA / Q000032:analysis* / Q000737:chemistry / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D005462:Fluorine Radioisotopes; D008024:Ligands; D018079:Receptors, GABA; C499229:TSPO protein, human