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; Rupert Lanzenberger; Marcus Hacker; Markus Mitterhauser; Cécile Philippe

doi:10.1038/s41598-017-08684-6

Scientific Reports (Aug 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

Markus Zeilinger,
Monika Dumanic,
Florian Pichler,
Lubos Budinsky,
Wolfgang Wadsak,
Katharina Pallitsch,
Helmut Spreitzer,
Rupert Lanzenberger,
Marcus Hacker,
Markus Mitterhauser,
Cécile Philippe

Affiliations

Markus Zeilinger: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna
Monika Dumanic: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna
Florian Pichler: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna
Lubos Budinsky: Department of Biomedical Imaging and Image-guided Therapy, Division of Molecular and Gender Imaging, Medical University of Vienna
Wolfgang Wadsak: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna
Katharina Pallitsch: Department of Organic Chemistry, University of Vienna
Helmut Spreitzer: Department of Pharmaceutical Chemistry, University of Vienna
Rupert Lanzenberger: Department of Psychiatry and Psychotherapy, Medical University of Vienna
Marcus Hacker: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna
Markus Mitterhauser: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna
Cécile Philippe: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna

DOI: https://doi.org/10.1038/s41598-017-08684-6
Journal volume & issue: Vol. 7, no. 1
pp. 1 – 10

Abstract

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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.

Published in Scientific Reports

ISSN: 2045-2322 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Medicine; Science
Website: https://www.nature.com/srep/

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