In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11C]SNAP-7941 and [18F]FE@SNAP reveal specific uptake in the ventricular system

Abstract The MCHR1 is involved in the regulation of energy homeostasis and changes of the expression are linked to a variety of associated diseases, such as diabetes and adiposity. The study aimed at the in vitro and in vivo evaluation of [11C]SNAP-7941 and [18F]FE@SNAP as potential PET-tracers for...

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Autores principales:	Markus Zeilinger, Monika Dumanic, Florian Pichler, Lubos Budinsky, Wolfgang Wadsak, Katharina Pallitsch, Helmut Spreitzer, Rupert Lanzenberger, Marcus Hacker, Markus Mitterhauser, Cécile Philippe
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2017
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/364732e8168b420aa283221050bfc995
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spelling	oai:doaj.org-article:364732e8168b420aa283221050bfc9952021-12-02T16:06:16ZIn vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11C]SNAP-7941 and [18F]FE@SNAP reveal specific uptake in the ventricular system10.1038/s41598-017-08684-62045-2322https://doaj.org/article/364732e8168b420aa283221050bfc9952017-08-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-08684-6https://doaj.org/toc/2045-2322Abstract The MCHR1 is involved in the regulation of energy homeostasis and changes of the expression are linked to a variety of associated diseases, such as diabetes and adiposity. The study aimed at the in vitro and in vivo evaluation of [11C]SNAP-7941 and [18F]FE@SNAP as potential PET-tracers for the MCHR1. Competitive binding studies with non-radioactive derivatives and small-animal PET/CT and MRI brain studies were performed under baseline conditions and tracer displacement with the unlabelled MCHR1 antagonist (±)-SNAP-7941. Binding studies evinced high binding affinity of the non-radioactive derivatives. Small-animal imaging of [11C]SNAP-7941 and [18F]FE@SNAP evinced high tracer uptake in MCHR1-rich regions of the ventricular system. Quantitative analysis depicted a significant tracer reduction after displacement with (±)-SNAP-7941. Due to the high binding affinity of the non-labelled derivatives and the high specific tracer uptake of [11C]SNAP-7941 and [18F]FE@SNAP, there is strong evidence that both radiotracers may serve as highly suitable agents for specific MCHR1 imaging.Markus ZeilingerMonika DumanicFlorian PichlerLubos BudinskyWolfgang WadsakKatharina PallitschHelmut SpreitzerRupert LanzenbergerMarcus HackerMarkus MitterhauserCécile PhilippeNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-10 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Markus Zeilinger Monika Dumanic Florian Pichler Lubos Budinsky Wolfgang Wadsak Katharina Pallitsch Helmut Spreitzer Rupert Lanzenberger Marcus Hacker Markus Mitterhauser Cécile Philippe In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11C]SNAP-7941 and [18F]FE@SNAP reveal specific uptake in the ventricular system
description	Abstract The MCHR1 is involved in the regulation of energy homeostasis and changes of the expression are linked to a variety of associated diseases, such as diabetes and adiposity. The study aimed at the in vitro and in vivo evaluation of [11C]SNAP-7941 and [18F]FE@SNAP as potential PET-tracers for the MCHR1. Competitive binding studies with non-radioactive derivatives and small-animal PET/CT and MRI brain studies were performed under baseline conditions and tracer displacement with the unlabelled MCHR1 antagonist (±)-SNAP-7941. Binding studies evinced high binding affinity of the non-radioactive derivatives. Small-animal imaging of [11C]SNAP-7941 and [18F]FE@SNAP evinced high tracer uptake in MCHR1-rich regions of the ventricular system. Quantitative analysis depicted a significant tracer reduction after displacement with (±)-SNAP-7941. Due to the high binding affinity of the non-labelled derivatives and the high specific tracer uptake of [11C]SNAP-7941 and [18F]FE@SNAP, there is strong evidence that both radiotracers may serve as highly suitable agents for specific MCHR1 imaging.
format	article
author	Markus Zeilinger Monika Dumanic Florian Pichler Lubos Budinsky Wolfgang Wadsak Katharina Pallitsch Helmut Spreitzer Rupert Lanzenberger Marcus Hacker Markus Mitterhauser Cécile Philippe
author_facet	Markus Zeilinger Monika Dumanic Florian Pichler Lubos Budinsky Wolfgang Wadsak Katharina Pallitsch Helmut Spreitzer Rupert Lanzenberger Marcus Hacker Markus Mitterhauser Cécile Philippe
author_sort	Markus Zeilinger
title	In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11C]SNAP-7941 and [18F]FE@SNAP reveal specific uptake in the ventricular system
title_short	In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11C]SNAP-7941 and [18F]FE@SNAP reveal specific uptake in the ventricular system
title_full	In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11C]SNAP-7941 and [18F]FE@SNAP reveal specific uptake in the ventricular system
title_fullStr	In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11C]SNAP-7941 and [18F]FE@SNAP reveal specific uptake in the ventricular system
title_full_unstemmed	In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11C]SNAP-7941 and [18F]FE@SNAP reveal specific uptake in the ventricular system
title_sort	in vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11c]snap-7941 and [18f]fe@snap reveal specific uptake in the ventricular system
publisher	Nature Portfolio
publishDate	2017
url	https://doaj.org/article/364732e8168b420aa283221050bfc995
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In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [11C]SNAP-7941 and [18F]FE@SNAP reveal specific uptake in the ventricular system

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