Radioiodination and preclinical evaluation of 4-benzyl-1-(3-[I]-iodobenzylsulfonyl)piperidine as a breast tumor imaging tracer in mouse.

Objective: 4-Benzyl-1-(3-iodobenzylsulfonyl)piperidine, 4-B-IBSP, has shown high-binding affinity to both sigma (σ) receptors in our previous work. In current study, radiolabeling and preclinical evaluation of 4-benzyl-1-(3-[I]-iodobenzylsulfonyl)piperidine, 4-B-[I]IBSP, in human ductal breast carcinoma (T47D) cells and in breast adenocarcinoma-bearing BALB/c mice are described.

Methods: Radioiodination of this new σ ligand was performed by a palladium-catalyzed stannylation approach followed by oxidative iododestannylation reaction using Iodo-Gen.