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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 |
| Institution: | 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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