| Title : Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[(18)F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-ben zene-1,3-diol ([(18)F]FEFE) for the in vivo visualisation and quantification of the beta2-adrenergic receptor status in lung - Schirrmacher_2003_Bioorg.Med.Chem.Lett_13_2687 |
| Author(s) : Schirrmacher E , Schirrmacher R , Thews O , Dillenburg W , Helisch A , Wessler I , Buhl R , Hohnemann S , Buchholz HG , Bartenstein P , Machulla HJ , Rosch F |
| Ref : Bioorganic & Medicinal Chemistry Lett , 13 :2687 , 2003 |
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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)-ben zene-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. |
| PubMedSearch : Schirrmacher_2003_Bioorg.Med.Chem.Lett_13_2687 |
| PubMedID: 12873495 |
Schirrmacher E, Schirrmacher R, Thews O, Dillenburg W, Helisch A, Wessler I, Buhl R, Hohnemann S, Buchholz HG, Bartenstein P, Machulla HJ, Rosch F (2003)
Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[(18)F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-ben zene-1,3-diol ([(18)F]FEFE) for the in vivo visualisation and quantification of the beta2-adrenergic receptor status in lung
Bioorganic & Medicinal Chemistry Lett
13 :2687
Schirrmacher E, Schirrmacher R, Thews O, Dillenburg W, Helisch A, Wessler I, Buhl R, Hohnemann S, Buchholz HG, Bartenstein P, Machulla HJ, Rosch F (2003)
Bioorganic & Medicinal Chemistry Lett
13 :2687