Steen Jakobsen

Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Research output: Contribution to journal/Conference contribution in journal/Contribution to newspaperJournal articleResearchpeer-review

  • 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
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.
Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Pages (from-to)5056-9
Number of pages4
Publication statusPublished - 2009

    Research areas

  • Animals, Carbon Radioisotopes, Haplorhini, Humans, Imidazolidines, Ligands, Piperidines, Positron-Emission Tomography, Radiopharmaceuticals, Rats, Receptors, Dopamine D3, Swine

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