In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1

Author(s)

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

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.

Organisation(s)

Department of Inorganic Chemistry, Department of Organic Chemistry

External organisation(s)

Medizinische Universität Wien

Journal

Scientific Reports

Volume

7

No. of pages

10

ISSN

2045-2322

DOI

https://doi.org/10.1038/s41598-017-08684-6

Publication date

08-2017

Peer reviewed

Yes

Austrian Fields of Science 2012

106002 Biochemistry, 106006 Biophysics

Keywords

Sustainable Development Goals

SDG 3 - Good Health and Well-being

Portal url

https://ucrisportal.univie.ac.at/en/publications/aea1aa52-4891-4683-8119-aee21b03858f