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RESEARCH PRODUCT
Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol ([18F]FEFE) for the in vivo visualisation and quantification of the β2-adrenergic receptor status in lung
Ralf SchirrmacherHans Georg BuchholzFrank RöschIgnatz WesslerWolfgang DillenburgRoland BuhlOliver ThewsEsther SchirrmacherAndreas HelischS. HöhnemannHans Jürgen MachullaPeter Bartensteinsubject
Fluorine RadioisotopesBiodistributionSwineStereochemistryClinical BiochemistryDiolPharmaceutical ScienceIn Vitro TechniquesBiochemistryChemical synthesisGuinea pigchemistry.chemical_compoundIn vivoDrug DiscoverymedicineAnimalsTissue DistributionLungMolecular BiologyFenoterolFenoterolOrganic ChemistryLigand (biochemistry)Models ChemicalchemistryMolecular MedicineReceptors Adrenergic beta-2RadiopharmaceuticalsEx vivoTomography Emission-Computedmedicine.drugdescription
The 18 F-labeled b2-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 radio- chemical yield of 20% after 65 min with a radiochemical purity higher than 98%. The specific activity was in the range of 50-60 GBq/mmol. In vitro testing of the non-radioactive fluorinated fenoterol derivative with isolated guinea pig trachea was conducted to obtain an IC50 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 b2-receptor. # 2003 Elsevier Ltd. All rights reserved.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2003-07-23 | Bioorganic & Medicinal Chemistry Letters |