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In this study, we synthesized 17-[4-(2-[¹⁸F]fluoroethyl)−1H-1,2,3-triazol-1-yl]-6-thia-heptadecanoic acid ([¹⁸F]1), a PET radiotracer for the evaluation of fatty acid metabolism. [¹⁸F]1 was synthesized in 20−26% decay-corrected radiochemical yields from 17-azido 6-thia-heptadecanoic acid (9) and 4-[¹⁸F]fluoro-1-butyne using click chemistry. The tissue distribution of [¹⁸F]1 in mice showed high radioactivity accumulation in heart (3.70%ID/g at 1 min, 3.28%ID/g at 10 min, and 3.01%ID/g at 60 min postinjection), a prolonged myocardial elimination half-life (>60 min), and a maximal heart-to-blood uptake ratio at 5 min postinjection (5.55). Pretreatment with etomoxir, a carnitine palmitoyl transferase (CPT) I inhibitor, reduced myocardial radioactivity uptake at 30 min postinjection by 53%, suggesting that [¹⁸F]1 was transported into the mitochondria. Analyses of heart tissue samples showed that most of the radioactivity …