New fluoro-diphenylchalcogen derivatives to explore the serotonin transporter by PET

A series of fluorinated diphenylchalcogen derivatives, possessing a sulfur or an oxygen bridge, has been prepared with the aim to get a suitable radiotracer to image the SERT in vivo using positron emission tomography (PET). The compounds were synthesized and assayed toward the serotonin (SERT), dopamine (DAT), and norepinephrine (NET) transporters. Among the developed series, five compounds display a high SERT affinity (Ki: 0.27–2.91 nM range) and can be labeled either with carbon-11 or fluorine-18.

Graphical abstractThe synthesis of highly potent fluorinated SERT tracers is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide