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Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies |
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| Authors: | 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 |
| Affiliation: | 1. GlaxoSmithKline Clinical Imaging Centre, Imperial College London, Hammersmith Hospital, Du Cane Road, London, UK;2. Aarhus PET Centre, Aarhus University Hospital, Aarhus, Denmark;3. PET Centre, Yale University School of Medicine, New Haven CT, USA;4. Cancer Therapeutics, Melbourne, Australia;5. GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, Verona, Italy;6. Division of Neurosciences and Mental Health, Imperial College London, Neuroscience Laboratories, Burlington Danes Building, Hammersmith Hospital, UK;7. Altria Client Service, Richmond VA, USA |
| Abstract: | Compound 1 is a potent and selective antagonist of the dopamine D3 receptor. With the aim of developing a carbon-11 labeled ligand for the dopamine D3 receptor, 1 was selected as a potential PET probe. [11C]1 was obtained by palladium catalyzed cross coupling using [11C]cyanide and 4 with a specific activity of 55.5 ± 25.9 GBq/μmol (1.5 ± 0.7 Ci/μmol). [11C]1 was tested in porcine and non-human primate models to assess its potential as a radioligand for PET imaging of the dopamine D3 receptor. We conclude that in both species and despite appropriate in vitro properties, [11C]1 does not show any specific signal for the dopamine D3 receptor. |
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