Dopamine D-3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

作者：Bennacef Idriss; Salinas Cristian A; Bonasera Thomas A; Gunn Roger N; Audrain Helene; Jakobsen Steen; Nabulsi Nabeel; Weinzimmer David; Carson Richard E; Huang Yiyun; Holmes Ian; Micheli Fabrizio^*; Heidbreder Christian; Gentile Gabriella; Rossi Tino; Laruelle Marc

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(17): 5056-5059.

DOI：10.1016/j.bmcl.2009.07.055

• Dopamine D-3
• Antagonist
• PET
• Ligand

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. [C-11]1 was obtained by palladium catalyzed cross coupling using [11C] cyanide and 4 with a specific activity of 55.5 /- 25.9 GBq/mu mol (1.5 /- 0.7 Ci/mu mol). [C-11]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, [C-11]1 does not show any specific signal for the dopamine D-3 receptor.

• 出版日期2009-9-1