PET imaging is a non-invasive technic of medical imaging. This requires the synthesis of specific ligands, radiolabeled with a PET-isotopes, mainly carbon-11 or fluorine-18.

First [18F] PET radioligands of 5-HT6 receptors.


The 5-HT6 receptor is one of the most recently discovered of the serotonin family of receptors. Even if the role of the 5-HT6 receptor in the brain was not yet clearly understood, its specific brain localization, particularly in the basal ganglia and limbic regions, and the high affinity shown by several atypical antipsychotics suggested involvement in the serotonergic control of motor function, mood-dependent behavior, and related diseases. Recent studies identified 5-HT6 receptors as promising targets for cognitive improvement in psychiatric or neurodegenerative diseases (Alzheimer diseases) and for antiobesity drugs.
To well understand the role of this 5-HT6 receptor, we have developed a selective and specific radioligands labelled with fluorine-18.

Ligands syntheses & 5-HT6R affinities

Image20

Radiolabeling of selected tracer: [18F]2FNQ1P

Image21

 

In vivo PET imaging with [18F]2FNQ1P

Image22