Serotonin and its various receptors are involved in numerous brain functions and neuropsychiatric disorders.
The 5-HT1A family is the best characterized subtype of the fourteen currently known 5-HT receptors. The 5-HT1A receptor
is closely involved in the pathogenesis of anxiety, depression, epilepsy and eating disorders and therefore is an important
target for drug therapy. The development in the 1980s of molecules specifically targeting this receptor was followed by
the rapid development of corresponding PET neuroimaging. Because this receptor represents a crucial target in neuroscience,
a large number of radioligands have been developed by academic and industry centers for visualization and quantification,
first in living animals and ultimately in humans. After a brief account of some of the structural and functional
characteristics of brain 5-HT1A receptors, this review focuses on the main lines of evolutionopened up by preclinical and
clinical 5-HT1A PET radiopharmaceuticals, illustrating the potential value of PET for clinical research and drug development.
Keywords: Agonist, antagonist, neurotransmission, positron emission tomography, radiopharmaceutical, 5-HT1A receptor.
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