Schirrmacher Esther, Schirrmacher Ralf, Thews Oliver, Dillenburg Wolfgang, Helisch Andreas, Wessler Ignatz, Buhl Roland, Höhnemann Sabine, Buchholz Hans Georg, Bartenstein Peter, Machulla Hans Jürgen, Rösch Frank
Institute of Nuclear Chemistry, University of Mainz, Fritz Strassmann-Weg 2, D-55128, Mainz, Germany.
Bioorg Med Chem Lett. 2003 Aug 18;13(16):2687-92. doi: 10.1016/s0960-894x(03)00538-9.
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.
（18）F标记的β2-肾上腺素能受体配体（R，R）（S，S）5-（2-（2-[4-（2-[（18）F]氟乙氧基）苯基]-1-甲基乙氨基）-1-羟乙基）-苯-1,3-二醇，是原始高选择性外消旋非诺特罗的衍生物，在65分钟后以20%的总放射化学产率合成，放射化学纯度高于98%。比活度在50-60GBq/微摩尔范围内。用分离的豚鼠气管对非放射性氟化非诺特罗衍生物进行体外测试，以获得60nM的半数抑制浓度（IC50）值。对豚鼠进行了初步的离体器官分布和正电子发射断层扫描（PET）体内实验，以研究生物分布以及放射性示踪剂的置换，从而证明与β2受体的特异性结合。
