Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies.
Idriss Bennacef, Cristian A Salinas, Thomas A Bonasera, Roger N Gunn, Hélène Audrain, Steen Jakobsen, Nabeel Nabulsi, David Weinzimmer, Richard E Carson, Yiyun Huang, Ian Holmes, Fabrizio Micheli, Christian Heidbreder, Gabriella Gentile, Tino Rossi, Marc Laruelle
文献索引：Bioorg. Med. Chem. Lett. 19 , 5056-5059, (2009)
全文：HTML全文
摘要
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.
相关化合物
相关文献：
Synthesis of tetrachloroisophthalo-[14C]-nitrile. Davies PE.
[J. Labelled Comp. Radiopharm. 21(3) , 285-292, (1984)]
Synthesis of Chiral Amino Acid Anilides by Ligand-Free Copper-Catalyzed Selective N-Arylation of Amino Acid Amides Dong J, et al.
[Adv. Synth. Catal. 355(4) , 692-696, (2013)]
Thermodynamic and aromaticity studies for the assessment of the halogen? cyano interactions on Iodobenzonitrile. Rocha IM, et al.
[J. Chem. Thermodyn. 65 , 204-212., (2013)]