Classics in Neuroimaging: The Serotonergic 2A Receptor System-from Discovery to Modern Molecular Imaging
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Classics in Neuroimaging : The Serotonergic 2A Receptor System-from Discovery to Modern Molecular Imaging. / T L'Estrade, Elina; Hansen, Hanne D; Erlandsson, Maria; Ohlsson, Tomas G; Knudsen, Gitte M; Herth, Matthias M.
In: ACS Chemical Neuroscience, Vol. 9, No. 6, 20.06.2018, p. 1226-1229.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Classics in Neuroimaging
T2 - The Serotonergic 2A Receptor System-from Discovery to Modern Molecular Imaging
AU - T L'Estrade, Elina
AU - Hansen, Hanne D
AU - Erlandsson, Maria
AU - Ohlsson, Tomas G
AU - Knudsen, Gitte M
AU - Herth, Matthias M
PY - 2018/6/20
Y1 - 2018/6/20
N2 - Already in 1953, Woolley and Shaw speculated that serotonin could be involved in a range of central nervous system (CNS) disorders. Lysergic acid diethylamide (LSD) displayed an important role in this respect. It was used not only to antagonize biological effects of serotonin and to study the system itself, but also to identify serotonergic subtype receptors. The 5-HT2A receptor was discovered in the 1970s and identified as the responsible receptor mediating psychedelic effects of LSD. The development of positron emission tomography (PET) allowed to study this receptor system in vivo. Parameters such as abundance of 5-HT2A neuroreceptors or receptor occupancy can be determined using PET. As such, the development of 5-HT2A receptor tracers started immediately after the introduction of PET in the mid-1970s. In this Viewpoint, we provide a historical overview from the discovery of serotonin to the identification of the 5-HT2A receptor subtype and the subsequent development of 5-HT2A receptor subtype specific PET tracers over the last four decades. We emphasize the interplay between pharmacology, medicinal chemistry, radiochemistry, and nuclear medicine that is important while developing a PET tracer. Moreover, we highlight selected examples applying 5-HT2A receptor PET tracers within neurological diseases and drug occupancy studies.
AB - Already in 1953, Woolley and Shaw speculated that serotonin could be involved in a range of central nervous system (CNS) disorders. Lysergic acid diethylamide (LSD) displayed an important role in this respect. It was used not only to antagonize biological effects of serotonin and to study the system itself, but also to identify serotonergic subtype receptors. The 5-HT2A receptor was discovered in the 1970s and identified as the responsible receptor mediating psychedelic effects of LSD. The development of positron emission tomography (PET) allowed to study this receptor system in vivo. Parameters such as abundance of 5-HT2A neuroreceptors or receptor occupancy can be determined using PET. As such, the development of 5-HT2A receptor tracers started immediately after the introduction of PET in the mid-1970s. In this Viewpoint, we provide a historical overview from the discovery of serotonin to the identification of the 5-HT2A receptor subtype and the subsequent development of 5-HT2A receptor subtype specific PET tracers over the last four decades. We emphasize the interplay between pharmacology, medicinal chemistry, radiochemistry, and nuclear medicine that is important while developing a PET tracer. Moreover, we highlight selected examples applying 5-HT2A receptor PET tracers within neurological diseases and drug occupancy studies.
U2 - 10.1021/acschemneuro.8b00176
DO - 10.1021/acschemneuro.8b00176
M3 - Journal article
C2 - 29763291
VL - 9
SP - 1226
EP - 1229
JO - ACS Chemical Neuroscience
JF - ACS Chemical Neuroscience
SN - 1948-7193
IS - 6
ER -
ID: 199380441