多巴胺D3受体拮抗剂：寻找一种潜在的选择性正电子发射断层扫描（PET）配体。第3部分：放射性合成与体内研究。
Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies.
作者信息
Bennacef Idriss, Salinas Cristian A, Bonasera Thomas A, Gunn Roger N, Audrain Hélène, Jakobsen Steen, Nabulsi Nabeel, Weinzimmer David, Carson Richard E, Huang Yiyun, Holmes Ian, Micheli Fabrizio, Heidbreder Christian, Gentile Gabriella, Rossi Tino, Laruelle Marc
机构信息
GlaxoSmithKline Clinical Imaging Centre, Imperial College London, Hammersmith Hospital, Du Cane Road, London, UK.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5056-9. doi: 10.1016/j.bmcl.2009.07.055. Epub 2009 Jul 25.
Compound 1 is a potent and selective antagonist of the dopamine D(3) receptor. With the aim of developing a carbon-11 labeled ligand for the dopamine D(3) receptor, 1 was selected as a potential PET probe. [(11)C]1 was obtained by palladium catalyzed cross coupling using [(11)C]cyanide and 4 with a specific activity of 55.5+/-25.9GBq/micromol (1.5+/-0.7Ci/micromol). [(11)C]1 was tested in porcine and non-human primate models to assess its potential as a radioligand for PET imaging of the dopamine D(3) receptor. We conclude that in both species and despite appropriate in vitro properties, [(11)C]1 does not show any specific signal for the dopamine D(3) receptor.
化合物1是一种强效且选择性的多巴胺D(3)受体拮抗剂。为了开发一种用于多巴胺D(3)受体的碳-11标记配体，1被选为潜在的正电子发射断层扫描（PET）探针。[(11)C]1通过钯催化的交叉偶联反应，使用[(11)C]氰化物和4制备得到，比活度为55.5±25.9GBq/微摩尔（1.5±0.7居里/微摩尔）。[(11)C]1在猪和非人类灵长类动物模型中进行了测试，以评估其作为多巴胺D(3)受体PET成像放射性配体的潜力。我们得出结论，在这两个物种中，尽管[(11)C]1在体外具有合适的性质，但它并未显示出任何针对多巴胺D(3)受体的特异性信号。
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