Towards selective CNS PET imaging of the 5-HT7 receptor system: Past, present and future

Elina T L'Estrade; Maria Erlandsson; Fraser G Edgar; Tomas Ohlsson; Gitte M Knudsen; Matthias M Herth

doi:10.1016/j.neuropharm.2019.107830

Towards selective CNS PET imaging of the 5-HT7 receptor system: Past, present and future

Elina T L'Estrade, Maria Erlandsson, Fraser G Edgar, Tomas Ohlsson, Gitte M Knudsen, Matthias M Herth

18 Citations (Scopus)

Abstract

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'.

Original language	English
Article number	107830
Journal	Neuropharmacology
Volume	172
Pages (from-to)	107830
ISSN	0028-3908
DOIs	https://doi.org/10.1016/j.neuropharm.2019.107830
Publication status	Published - 1 Aug 2020

Keywords

5-HT7R
Molecular imaging
PET
Serotonin

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10.1016/j.neuropharm.2019.107830

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title = "Towards selective CNS PET imaging of the 5-HT7 receptor system: Past, present and future",

abstract = "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'.",

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AU - L'Estrade, Elina T

AU - Erlandsson, Maria

AU - Edgar, Fraser G

AU - Ohlsson, Tomas

AU - Knudsen, Gitte M

AU - Herth, Matthias M

PY - 2020/8/1

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Towards selective CNS PET imaging of the 5-HT7 receptor system: Past, present and future

Abstract

Keywords

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