Towards selective CNS PET Imaging of the 5-HT7 Receptor System: Past, Present and Future
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Towards selective CNS PET Imaging of the 5-HT7 Receptor System : Past, Present and Future. / L'Estrade, Elina T; Erlandsson, Maria; Edgar, Fraser G; Ohlsson, Tomas; Knudsen, Gitte M; Herth, Matthias M.
In: Neuropharmacology, Vol. 172, 107830, 2020.Research output: Contribution to journal › Review › Research › peer-review
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TY - JOUR
T1 - Towards selective CNS PET Imaging of the 5-HT7 Receptor System
T2 - Past, Present and Future
AU - L'Estrade, Elina T
AU - Erlandsson, Maria
AU - Edgar, Fraser G
AU - Ohlsson, Tomas
AU - Knudsen, Gitte M
AU - Herth, Matthias M
N1 - Copyright © 2019. Published by Elsevier Ltd.
PY - 2020
Y1 - 2020
N2 - Since its discovery in 1993, the serotonin receptor subtype 7 (5-HT7) has attracted significant attention as a potential drug target; due to its elucidated roles in conditions such as insomnia, schizophrenia, and more. Therefore, it is unsurprising that there has been relatively early efforts undertaken to develop a positron emission tomography (PET) imaging agent for said receptor system. PET can be clinically used to probe receptor systems in vivo, permitting information such as a drug's occupancy against this system to be investigated. This review focuses on the efforts towards the development of a 5-HT7R selective PET CNS tracer over the last 20 years, critically reflecting on applied strategies and commonly employed chemical frameworks and suggests future considerations that are needed to successfully develop a PET tracer for this clinically relevant target.
AB - Since its discovery in 1993, the serotonin receptor subtype 7 (5-HT7) has attracted significant attention as a potential drug target; due to its elucidated roles in conditions such as insomnia, schizophrenia, and more. Therefore, it is unsurprising that there has been relatively early efforts undertaken to develop a positron emission tomography (PET) imaging agent for said receptor system. PET can be clinically used to probe receptor systems in vivo, permitting information such as a drug's occupancy against this system to be investigated. This review focuses on the efforts towards the development of a 5-HT7R selective PET CNS tracer over the last 20 years, critically reflecting on applied strategies and commonly employed chemical frameworks and suggests future considerations that are needed to successfully develop a PET tracer for this clinically relevant target.
U2 - 10.1016/j.neuropharm.2019.107830
DO - 10.1016/j.neuropharm.2019.107830
M3 - Review
C2 - 31669129
VL - 172
JO - Neuropharmacology
JF - Neuropharmacology
SN - 0028-3908
M1 - 107830
ER -
ID: 231253285