کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1363702 | 981520 | 2009 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies](/preview/png/1363702.png)
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.
Radiosynthesis and in vivo testing for a potential Dopamine D3 PET ligand are reported.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 17, 1 September 2009, Pages 5056–5059