Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors

J Med Chem. 2022 Aug 25;65(16):10755-10808. doi: 10.1021/acs.jmedchem.2c00633. Epub 2022 Aug 8.


Serotonin (5-hydroxytryptamine, 5-HT) and 5-HT receptors (5-HTRs) have crucial roles in various neuropsychiatric disorders and neurodegenerative diseases, making them attractive diagnostic and therapeutic targets. Positron emission tomography (PET) is a noninvasive nuclear molecular imaging technique and is an essential tool in clinical diagnosis and drug discovery. In this context, numerous PET ligands have been developed for "visualizing" 5-HTRs in the brain and translated into human use to study disease mechanisms and/or support drug development. Herein, we present a comprehensive repertoire of 5-HTR PET ligands by focusing on their chemotypes and performance in PET imaging studies. Furthermore, this Perspective summarizes recent 5-HTR-focused drug discovery, including biased agonists and allosteric modulators, which would stimulate the development of more potent and subtype-selective 5-HTR PET ligands and thus further our understanding of 5-HTR biology.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Brain / diagnostic imaging
  • Brain / metabolism
  • Humans
  • Ligands
  • Positron-Emission Tomography* / methods
  • Radiopharmaceuticals
  • Receptors, Serotonin* / metabolism


  • Ligands
  • Radiopharmaceuticals
  • Receptors, Serotonin