Radiosynthesis, in vitro and preliminary in vivo evaluation of the novel glutamine derived PET tracers [18F]fluorophenylglutamine and [18F]fluorobiphenylglutamine

Baguet, Tristan; Verhoeven, Jeroen; Pauwelyn, Glenn; Hu, Jiyun; Lambe, Patricia; Lombaerde, Stef De; Piron, Sarah; Donche, Sam; Descamps, Benedicte; Goethals, Ingeborg; Vanhove, Christian; Vos, Filip De; Beyzavi, M. Hassan

doi:10.1016/j.nucmedbio.2020.03.006

Cited by 5 publications

(1 citation statement)

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“…In another study, two glutamine-derived PET tracers, [ 18 F] 7a ([ 18 F]fluorophenylglutamine) and [ 18 F] 7b ([ 18 F]fluorobiphenylglutamine), were also labeled and evaluated using the same method; however, both tracers had a low affinity toward the rat ASCT-2 transporter in vitro and low uptake in the F98 rat xenograft in vivo ( Figure 9 b). The authors concluded that they would optimize the substituents of the arene ring to obtain a high-quality, glutamine-based PET radiotracer [ 46 ].…”

Section: Ruthenium-catalyzed 18 F-aa Synthesismentioning

confidence: 99%

Recent Advances in 18F-Labeled Amino Acids Synthesis and Application

Wang

Lin²,

Yao³

2022

Pharmaceutics

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Radiolabeled amino acids are an important class of agents for positron emission tomography imaging that target amino acid transporters in many tumor types. Traditional 18F-labeled amino acid synthesis strategies are always based on nucleophilic aromatic substitution reactions with multistep radiosynthesis and low radiochemical yields. In recent years, new 18F-labeling methodologies such as metal-catalyzed radiofluorination and heteroatom (B, P, S, Si, etc.)-18F bond formation are being effectively used to synthesize radiopharmaceuticals. This review focuses on recent advances in the synthesis, radiolabeling, and application of a series of 18F-labeled amino acid analogs using new 18F-labeling strategies.

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Section: Ruthenium-catalyzed 18 F-aa Synthesismentioning

confidence: 99%