5-HT radioligands for human brain imaging with PET and SPECT

Research output: Contribution to journalReviewResearchpeer-review

The serotonergic system plays a key modulatory role in the brain and is the target for many drug treatments for brain disorders either through reuptake blockade or via interactions at the 14 subtypes of 5-HT receptors. This review provides the history and current status of radioligands used for positron emission tomography (PET) and single photon emission computerized tomography (SPECT) imaging of human brain serotonin (5-HT) receptors, the 5-HT transporter (SERT), and 5-HT synthesis rate. Currently available radioligands for in vivo brain imaging of the 5-HT system in humans include antagonists for the 5-HT(1A), 5-HT(1B), 5-HT(2A), and 5-HT(4) receptors, and for SERT. Here we describe the evolution of these radioligands, along with the attempts made to develop radioligands for additional serotonergic targets. We describe the properties needed for a radioligand to become successful and the main caveats. The success of a PET or SPECT radioligand can ultimately be assessed by its frequency of use, its utility in humans, and the number of research sites using it relative to its invention date, and so these aspects are also covered. In conclusion, the development of PET and SPECT radioligands to image serotonergic targets is of high interest, and successful evaluation in humans is leading to invaluable insight into normal and abnormal brain function, emphasizing the need for continued development of both SPECT and PET radioligands for human brain imaging.

Original languageEnglish
JournalMedicinal Research Reviews
Issue number1
Pages (from-to)54-111
Number of pages58
Publication statusPublished - Jan 2013

    Research areas

  • Brain/diagnostic imaging, Humans, Positron-Emission Tomography/methods, Radiopharmaceuticals/metabolism, Receptors, Serotonin/metabolism, Serotonin/chemistry, Serotonin Antagonists/metabolism, Serotonin Plasma Membrane Transport Proteins/metabolism, Tomography, Emission-Computed, Single-Photon/methods

ID: 196168856