title: A simple and efficient in vitro method for metabolism studies of radiotracers.
abstract: In vitro metabolism of acetylcholinesterase inhibitors containing 3-[(18)F]fluoromethylbenzyl- ([(18)F]1) and 4-[(18)F]fluorobenzyl-piperidine moieties ([(18)F]2) was studied and compared with the in vivo metabolism. Defluorination of the [(18)F]1 mainly occurred to generate [(18)F]fluoride ion both in vitro and in vivo. In contrast, the [(18)F]2 was converted into an unknown polar metabolite in both metabolism methods and another metabolite, 4-[(18)F]fluorobenzoic acid in vitro. These results demonstrated that the in vitro method can be used to predict the in vivo metabolism of both radiotracers.
authors.affiliation: Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Center for Clinical Research, Samsung Biomedical Research Institute, 50 Ilwon-dong, Kangnam-ku, Seoul, South Korea.
authors.forename: S Y
authors.initials: SY
authors.lastname: Lee
authors.forename: Y S
authors.initials: YS
authors.lastname: Choe
authors.forename: D H
authors.initials: DH
authors.lastname: Kim
authors.forename: B N
authors.initials: BN
authors.lastname: Park
authors.forename: S E
authors.initials: SE
authors.lastname: Kim
authors.forename: Y
authors.initials: Y
authors.lastname: Choi
authors.forename: K H
authors.initials: KH
authors.lastname: Lee
authors.forename: J
authors.initials: J
authors.lastname: Lee
authors.forename: B T
authors.initials: BT
authors.lastname: Kim
mesh_terms: D000818:Animals; D001565:Benzoates / Q000138:chemical synthesis; D002130:Calcium Phosphates / Q000737:chemistry; D002800:Cholinesterase Inhibitors / Q000378:metabolism*; D017886:Durapatite / Q000737:chemistry; D005462:Fluorine Radioisotopes; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D001565:Benzoates; D002130:Calcium Phosphates; D002800:Cholinesterase Inhibitors; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; C022894:2-fluorobenzoic acid; D017886:Durapatite