Synthesis of radiolabeled protein disulfide isomerase (PDI) inhibitors as new potential PET agents for imaging of the enzyme PDI in neurological disorders and cancer.

Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine

PubMedID: 23376309

Gao M, Yang Q, Wang M, Miller KD, Sledge GW, Zheng QH. Synthesis of radiolabeled protein disulfide isomerase (PDI) inhibitors as new potential PET agents for imaging of the enzyme PDI in neurological disorders and cancer. Appl Radiat Isot. 2013;7461-9.
Carbon-11-labeled substituted ß-tetrahydrocarbolines were prepared from their corresponding phenolic hydroxyl precursors with [(11)C]CH3OTf through O-[(11)C]methylation and isolated by simplified SPE in 50-60% decay corrected radiochemical yields at EOB with 185-370GBq/µmol specific activity at EOS. A fluorine-18-labeled substituted ß-tetrahydrocarboline was prepared from its corresponding halo-precursors (X=Cl, Br, I) with K[(18)F]F/Kryptofix 2.2.2 via the nucleophilic substitution and isolated by HPLC combined with SPE in 25-40% decay corrected radiochemical yield with 37-222GBq/µmol specific activity at EOB.