Radiosynthesis of novel carbon-11-labeled triaryl ligands for cannabinoid-type 2 receptor

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• 作者：Masayuki Fujinaga ; Katsushi Kumata ; Kazuhiko Yanamoto ; Kazunori Kawamura ; Tomoteru Yamasaki ; Joji Yui ; Akiko Hatori ; Masanao Ogawa ; Yuichiro Yoshida ; Nobuki Nengaki ; Jun Maeda ; Ming-Rong Zhang
• 关键词：Cannabinoid subtype-2 ; PET ; Triaryl ligands ; Brain uptake ; Radiosynthesis
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 March 2010
• 年：2010
• 卷：20
• 期：5
• 页码：1565-1568
• 全文大小：243 K

文摘

Two novel triaryl ligands 2 and 5 with potent in vitro binding affinities for the cannabinoid subtype-2 (CB2) receptor were labeled with a positron-emitting radioactive nuclide ¹¹C. Radioligands [¹¹C]2, [¹¹C]5, and their analogs [¹¹C]3 and [¹¹C]4 were synthesized by O-[¹¹C]methylation of their corresponding phenol precursors with [¹¹C]CH₃I. [¹¹C]2–5 had relatively high uptakes (>1.2 % injected dose/g tissue) in mouse brains.