Current status of positron emission tomography radiotracers for serotonin receptors in humans

L. Zimmer (1, 2) , D. Le Bars (1, 3)

1 CERMEP - imagerie du vivant - Centre d'Etude et de Recherche Multimodal Et Pluridisciplinaire en imagerie du vivant
2 CRNL - Centre de recherche en neurosciences de Lyon - Lyon Neuroscience Research Center
3 ICBMS - Institut de Chimie et Biochimie Moléculaires et Supramoléculaires

Serotonin (5-HT) neurotransmission plays a key modulatory role in the brain. This system is critical for pathophysiological processes and many drug treatments for brain disorders interact with its 14 subtypes of receptors. Positron emission tomography (PET) is a unique tool for the study of the living brain in translational studies from animal models to patients in neurology or psychiatry. This short review is intended to cover the current status of PET radioligands used for imaging human brain 5-HT receptors. Here, we describe the available PET radioligands for the 5-HT1A, 5-HT1B, 5-HT2A, 5-HT4 and 5-HT6 receptors. Finally, we highlight the future challenges for a functional PET imaging of serotonin receptors, including the research towards specific PET radiotracers for yet unexplored serotonin receptors, the need of radiotracers for endogenous serotonin level measurement and the contribution of agonist radiotracers for functional imaging of 5-HT neurotransmission.

L. Zimmer, D. Le Bars. Current status of positron emission tomography radiotracers for serotonin receptors in humans. Journal of Labelled Compounds and Radiopharmaceuticals, 2013, 56 (3-4), pp.105-113. ⟨10.1002/jlcr.3001⟩. ⟨hal-00828326⟩