A simple and efficient in vitro method for metabolism studies of radiotracers.
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.
Lee
S Y
SY
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.
Choe
Y S
YS
Kim
D H
DH
Park
B N
BN
Kim
S E
SE
Choi
Y
Y
Lee
K H
KH
Lee
J
J
Kim
B T
BT
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
D001565:Benzoates; D002130:Calcium Phosphates; D002800:Cholinesterase Inhibitors; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; C022894:2-fluorobenzoic acid; D017886:Durapatite