Efficient one-pot radiosynthesis of the ¹¹C-labeled aquaporin-4 inhibitor TGN-020.

ABSTRACT:

Background

[¹¹C]TGN-020 has been developed as a positron emission tomography (PET) tracer for imaging aquaporin-4 (AQP4) in the brain and used in clinical studies. Previously, [¹¹C]TGN-020 was synthesized through the acylation of [¹¹C]nicotinic acid, produced by the reaction of 3-bromopyridine and n-butyllithium with [¹¹C]CO₂, with 2-amino-1,3,4-thiadiazole. In this study, to enhance the automated radiosynthesis efficiency of [¹¹C]TGN-020, we optimized its radiosynthesis procedure using our in-house developed ¹¹C-labeling synthesizer.

Results

[¹¹C]TGN-020 was synthesized via direct [¹¹C]CO₂ fixation using n-butyllithium and 3-bromopyridine in tetrahydrofuran, followe

SUBMITTER: Kawamura K 

PROVIDER: S-EPMC11972257 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature