Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [¹¹C]hemicholinium-3 and [¹⁸F]hemicholinium-3

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• 作者：Qi-Huang Zheng ; Mingzhang Gao ; Bruce H. Mock ; Shuyan Wang ; Toshihiko Hara ; Rachid Nazih ; Michael A. Miller ; Tim J. Receveur ; John C. Lopshire ; William J. Groh ; et al.
• 关键词：High-affinity choline transporter (CHT1) ; Positron emission tomography (PET) ; [¹¹C]hemicholinium-3 ([¹¹C]HC-3) ; [¹⁸F]hemicholinium-3 ([¹⁸F]HC-3) ; Biodistribution
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：15 April 2007
• 年：2007
• 卷：17
• 期：8
• 页码：2220-2224
• 全文大小：148 K

文摘

The high-affinity choline transporter (CHT1) system is an attractive target for the development of positron emission tomography (PET) biomarkers to probe brain, cardiac, and cancer diseases. An efficient and convenient synthesis of new radiolabeled CHT1 inhibitors [¹¹C]hemicholinium-3 and [¹⁸F]hemicholinium-3 by solid-phase extraction (SPE) technique using a cation-exchange CM Sep-Pak cartridge has been well developed. The preliminary evaluation of both tracers through biodistribution studies in 9L-glioma rats has been performed, and the uptakes in the heart and tumor were observed, while very low brain uptake was seen.