title: [¹⁸F]FE@SNAP-A new PET tracer for the melanin concentrating hormone receptor 1 (MCHR1): microfluidic and vessel-based approaches.
abstract: Changes in the expression of the melanin concentrating hormone receptor 1 (MCHR1) are involved in a variety of pathologies, especially obesity and anxiety disorders. To monitor these pathologies in-vivo positron emission tomography (PET) is a suitable method. After the successful radiosynthesis of [(11)C]SNAP-7941-the first PET-Tracer for the MCHR1, we aimed to synthesize its [(18)F]fluoroethylated analogue: [(18)F]FE@SNAP. Therefore, microfluidic and vessel-based approaches were tested. [(18)F]fluoroethylation was conducted via various [(18)F]fluoroalkylated synthons and direct [(18)F]fluorination. Only the direct [(18)F]fluorination of a tosylated precursor using a flow-through microreactor was successful, affording [(18)F]FE@SNAP in 44.3 ± 2.6%.
authors.affiliation: Radiochemistry and Biomarker Development Unit, Department of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, Vienna 1090, Austria.
authors.forename: Cécile
authors.initials: C
authors.lastname: Philippe
authors.forename: Johanna
authors.initials: J
authors.lastname: Ungersboeck
authors.forename: Eva
authors.initials: E
authors.lastname: Schirmer
authors.forename: Milica
authors.initials: M
authors.lastname: Zdravkovic
authors.forename: Lukas
authors.initials: L
authors.lastname: Nics
authors.forename: Markus
authors.initials: M
authors.lastname: Zeilinger
authors.forename: Karem
authors.initials: K
authors.lastname: Shanab
authors.forename: Rupert
authors.initials: R
authors.lastname: Lanzenberger
authors.forename: Georgios
authors.initials: G
authors.lastname: Karanikas
authors.forename: Helmut
authors.initials: H
authors.lastname: Spreitzer
authors.forename: Helmut
authors.initials: H
authors.lastname: Viernstein
authors.forename: Markus
authors.initials: M
authors.lastname: Mitterhauser
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Wadsak
mesh_terms: D005462:Fluorine Radioisotopes / Q000737:chemistry*; D006801:Humans; D044085:Microfluidics / Q000379:methods; D010880:Piperidines / Q000737:chemistry*; D049268:Positron-Emission Tomography / Q000379:methods; D011743:Pyrimidines / Q000737:chemistry*; D017481:Receptors, Somatostatin / Q000032:analysis*
chemical_list: D005462:Fluorine Radioisotopes; C103263:MCHR1 protein, human; D010880:Piperidines; D011743:Pyrimidines; D017481:Receptors, Somatostatin; C464854:SNAP7941