One-step conjugation of glycylglycine with [18F]FDG and a pilot PET imaging study
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Date
2018
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Abstract
This study describes a single step conjugation of Glycylglycine (GlyGly) which is a small peptide, with [18F]FDG via oxime formation. Amiooxy-functionalization of GlyGly (AO-GlyGly) was accomplished through the reaction of Boc-aminooxy succinimide ester. Conjugation reaction was performed at 100 °C for 30 min in a vial containing AO-GlyGly and [18F]FDG solution. The radiolabeled product ([18F]FDG-GlyGly) was obtained with 98.65 ± 0.35% yield without any purification step which makes this method more attractive for 18F radiolabeling. The present study is concluded with an in vivo pilot animal PET study to assess biodistribution and kinetics of chemoselectively [18F]FDG tagged GlyGly in vivo. © 2018, Akadémiai Kiadó, Budapest, Hungary.
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fluorine glycylglycine fluorodeoxyglucose f 18 , fluorodeoxyglucose f 18 , glycylglycine , unclassified drug , animal experiment , Article , bladder , drug conjugation , high performance liquid chromatography , in vivo study , isotope labeling , kidney , male , molecular weight , nonhuman , pilot study , positron emission tomography , rat , retention time , tissue distribution , Wistar rat