Abstract
The critical role of serotonin (5-hydroxytryptamine; 5-HT) and its receptors (5-HTRs) in the pathophysiology of diverse neuropsychiatric and neurodegenerative disorders render them attractive diagnostic and therapeutic targets for brain disorders. Therefore, the in vivo assessment of binding of 5-HT receptor ligands under a multitude of physiologic and pathologic scenarios may support more-accurate identification of disease and its progression and the patient's response to therapy as well as the screening of novel therapeutic strategies. The present Review aims to focus on the current status of radioligands used for positron-emission tomography (PET) and single-photon-emission computerized tomography (SPECT) imaging of human brain serotonin receptors. We further elaborate upon and emphasize the attributes that qualify a radioligand for theranostics on the basis of its frequency of use in clinics, its benefit to risk assessment in humans, and its continuous evolution, along with the major limitations.
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