PET Radiotracers for Molecular Imaging of Serotonin 5-HT_1A Receptors

Title:PET Radiotracers for Molecular Imaging of Serotonin 5-HT_1A Receptors

Volume: 21 Issue: 1

Author(s): T. Billard, D. Le Bars and L. Zimmer

Affiliation:

Keywords: Agonist, antagonist, neurotransmission, positron emission tomography, radiopharmaceutical, 5-HT_1A receptor.

Abstract: Serotonin and its various receptors are involved in numerous brain functions and neuropsychiatric disorders. The 5-HT_1A family is the best characterized subtype of the fourteen currently known 5-HT receptors. The 5-HT_1A 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-HT_1A receptors, this review focuses on the main lines of evolutionopened up by preclinical and clinical 5-HT_1A PET radiopharmaceuticals, illustrating the potential value of PET for clinical research and drug development.

Cite this article as:

Billard T., Bars Le D. and Zimmer L., PET Radiotracers for Molecular Imaging of Serotonin 5-HT_1A Receptors, Current Medicinal Chemistry 2014; 21 (1) . https://dx.doi.org/10.2174/09298673113209990215