Serotonin receptors (5-HTRs) are implicated in the pathophysiology of a variety of
neuropsychiatric and neurodegenerative disorders and are also targets for drug therapy. In the CNS, most of
these receptors are expressed in high abundance in specific brain regions reflecting their role in brain
functions. Quantifying binding to 5-HTRs in vivo may permit assessment of physiologic and pathologic
conditions, and monitoring disease progression, evaluating treatment response, and for investigating new treatment
modalities. Positron emission tomography (PET) molecular imaging has the sensitivity to quantify binding of 5-HTRs in
CNS disorders and to measure drug occupancy as part of a process of new drug development. Although research on PET
imaging of 5-HTRs have been performed more than two decades, the successful radiotracers so far developed for human
studies are limited to 5-HT1AR, 5-HT1BR, 5-HT2AR, 5-HT4R and 5-HT6R. Herein we review the development and
application of radioligands for PET imaging of 5-HTRs in living brain.
Keywords: Molecular imaging, PET, 5-HTR, radioligands, serotonin receptors.
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