title: Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[(18)F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol ([(18)F]FEFE) for the in vivo visualisation and quantification of the beta2-adrenergic receptor status in lung.
abstract: The (18)F-labeled beta2-adrenergic receptor ligand (R,R)(S,S) 5-(2-(2-[4-(2-[(18)F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol, a derivative of the original highly selective racemic fenoterol, was synthesized in an overall radiochemical yield of 20% after 65 min with a radiochemical purity higher than 98%. The specific activity was in the range of 50-60 GBq/micromol. In vitro testing of the non-radioactive fluorinated fenoterol derivative with isolated guinea pig trachea was conducted to obtain an IC(50) value of 60 nM. Preliminary ex vivo organ distribution and in vivo experiments with positron emission tomography (PET) on guinea pigs were performed to study the biodistribution as well as the displacement of the radiotracer to prove specific binding to the beta2-receptor.
authors.affiliation: Institute of Nuclear Chemistry, University of Mainz, Fritz Strassmann-Weg 2, D-55128, Mainz, Germany. frank.roesch@uni-mainz.de
authors.forename: Esther
authors.initials: E
authors.lastname: Schirrmacher
authors.forename: Ralf
authors.initials: R
authors.lastname: Schirrmacher
authors.forename: Oliver
authors.initials: O
authors.lastname: Thews
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Dillenburg
authors.forename: Andreas
authors.initials: A
authors.lastname: Helisch
authors.forename: Ignatz
authors.initials: I
authors.lastname: Wessler
authors.forename: Roland
authors.initials: R
authors.lastname: Buhl
authors.forename: Sabine
authors.initials: S
authors.lastname: Höhnemann
authors.forename: Hans Georg
authors.initials: HG
authors.lastname: Buchholz
authors.forename: Peter
authors.initials: P
authors.lastname: Bartenstein
authors.forename: Hans Jürgen
authors.initials: HJ
authors.lastname: Machulla
authors.forename: Frank
authors.initials: F
authors.lastname: Rösch
mesh_terms: D000818:Animals; D005280:Fenoterol / Q000031:analogs & derivatives* / Q000378:metabolism; D005462:Fluorine Radioisotopes; D066298:In Vitro Techniques; D008168:Lung / Q000000981:diagnostic imaging* / Q000378:metabolism; D008956:Models, Chemical; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D018343:Receptors, Adrenergic, beta-2 / Q000032:analysis / Q000378:metabolism*; D013552:Swine; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
chemical_list: D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D018343:Receptors, Adrenergic, beta-2; D005280:Fenoterol