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

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, Douglas P. Zipes, Gary D. Hutchins, Timothy R. DeGrado

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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.

Original languageEnglish (US)
Pages (from-to)2220-2224
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number8
StatePublished - Apr 15 2007



  • [C]hemicholinium-3 ([C]HC-3)
  • [F]hemicholinium-3 ([F]HC-3)
  • Biodistribution
  • High-affinity choline transporter (CHT1)
  • Positron emission tomography (PET)

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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