Towards selective CNS PET Imaging of the 5-HT7 Receptor System: Past, Present and Future

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 - 2020/8/1

Y1 - 2020/8/1

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. This article is part of the special issue entitled ‘Serotonin Research: Crossing Scales and Boundaries’.

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. This article is part of the special issue entitled ‘Serotonin Research: Crossing Scales and Boundaries’.

U2 - 10.1016/j.neuropharm.2019.107830

DO - 10.1016/j.neuropharm.2019.107830

M3 - Review

C2 - 31669129

SN - 0028-3908

SP - 107830

JO - Neuropharmacology

JF - Neuropharmacology

ER -