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

Markus Zeilinger; Monika Dumanic; Florian Pichler; Lubos Budinsky; Wolfgang Wadsak; Katharina Pallitsch; Helmut Spreitzer; Marcus Hacker; Markus Mitterhauser; Cecile Philippe

doi:10.1038/s41598-017-08684-6

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

Markus Zeilinger, Monika Dumanic, Florian Pichler, Lubos Budinsky, Wolfgang Wadsak, Katharina Pallitsch, Helmut Spreitzer, Marcus Hacker, Markus Mitterhauser (Corresponding author), Cecile Philippe

Publications: Contribution to journal › Article › Peer Reviewed

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.

Original language	English
Article number	8054
Number of pages	10
Journal	Scientific Reports
Volume	7
DOIs	https://doi.org/10.1038/s41598-017-08684-6
Publication status	Published - 14 Aug 2017

Austrian Fields of Science 2012

106002 Biochemistry
106006 Biophysics

Keywords

PROTEIN-COUPLED RECEPTOR
1ST PET-TRACER
MCH RECEPTOR
IDENTIFICATION
BRAIN
MICE
INHIBITOR
LIGAND
CELLS
SLC-1

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1038/s41598-017-08684-6Licence: CC BY 4.0

http://phaidra.univie.ac.at/o:918382Licence: CC BY 4.0

Cite this

Zeilinger, M., Dumanic, M., Pichler, F., Budinsky, L., Wadsak, W., Pallitsch, K., Spreitzer, H., Hacker, M., Mitterhauser, M., & Philippe, C. (2017). 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. Scientific Reports, 7, Article 8054. https://doi.org/10.1038/s41598-017-08684-6

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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",

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. ",

keywords = "PROTEIN-COUPLED RECEPTOR, 1ST PET-TRACER, MCH RECEPTOR, IDENTIFICATION, BRAIN, MICE, INHIBITOR, LIGAND, CELLS, SLC-1",

author = "Markus Zeilinger and Monika Dumanic and Florian Pichler and Lubos Budinsky and Wolfgang Wadsak and Katharina Pallitsch and Helmut Spreitzer and Marcus Hacker and Markus Mitterhauser and Cecile Philippe",

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Zeilinger, M, Dumanic, M, Pichler, F, Budinsky, L, Wadsak, W, Pallitsch, K, Spreitzer, H, Hacker, M, Mitterhauser, M & Philippe, C 2017, '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', Scientific Reports, vol. 7, 8054. https://doi.org/10.1038/s41598-017-08684-6

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. / Zeilinger, Markus; Dumanic, Monika; Pichler, Florian et al.
In: Scientific Reports, Vol. 7, 8054, 14.08.2017.

Publications: Contribution to journal › Article › Peer Reviewed

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AU - Dumanic, Monika

AU - Pichler, Florian

AU - Budinsky, Lubos

AU - Wadsak, Wolfgang

AU - Pallitsch, Katharina

AU - Spreitzer, Helmut

AU - Hacker, Marcus

AU - Mitterhauser, Markus

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