title: Current status of positron emission tomography radiotracers for serotonin receptors in humans.
abstract: 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.
authors.affiliation: Hospices Civils de Lyon, CERMEP-Imaging Platform, Lyon, France; University of Lyon 1, INSERM, CNRS, Lyon Neuroscience Research Centre, Lyon, France.
authors.forename: Luc
authors.initials: L
authors.lastname: Zimmer
authors.forename: Didier
authors.initials: D
authors.lastname: Le Bars
mesh_terms: D001921:Brain / Q000000981:diagnostic imaging; D002250:Carbon Radioisotopes / Q000737:chemistry; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006801:Humans; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology
chemical_list: D002250:Carbon Radioisotopes; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists
keywords: PET; brain; radiopharmaceutical; receptor; serotonin