Labeling of a serotoninergic ligand with 18F : [18F] setoperone

Setoperone has been labeled with 18F to visualize the serotoninergic receptors by positron emission tomography. The synthesis is carried out by a nucleophilic substitution from a nitro derivative of setoperone with 18F−. The synthesis of nitro‐derivative is described as well as the different trials of recovery of ion 18F− from neon or aqueous target. The considered technique of labeling allow to obtain from 7.4 GBq (200 mCi) 18F, 1.5 to 2 GBq (40–50 mCi) of [18F]setoperone, 110 minutes after the end of bombardment. The specific activity obtained from this quantity of radioactivity is about 37 GBq/μMol (1 Ci/μMol).