Synthesis and evaluation of a new fluorine-18 labeled rotenoid as a potential pet probe of mitochondrial complex I activity

Article abstract of DOI:10.1002/(SICI)1099-1344(199911)42:11<1039::AID-JLCR259>3.0.CO;2-1

Fluorine-18 labeled (6aS, 12aS, 5'R)-12-deoxo-6',7'-dihydro-7'-fluororotenone (F-DDRT), a new potential PET probe of mitochondrial complex I activity, was synthesized. [¹⁸F]-DDRT was prepared with good specific activity by nucleophilic displacement with an overall radiochemical yield of 25% (EOB). The uptake of [¹⁸F]-DDRT in rat brain and heart was compared with the uptake of another fluorine-18 labeled rotenoid: [¹⁸F]-DHRT. In comparison to [¹⁸F]-DHRT, the brain and heart retention of [¹⁸F]-DDRT were both lower at any point of the study (respectively 0.49 and 2.82% dose/g vs 0.34 and 1.24% dose/g at 60 min post injection).