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

Research output: Contribution to journalArticle

31 Scopus citations

Abstract

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
Volume17
Issue number8
DOIs
StatePublished - Apr 15 2007

Keywords

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

ASJC Scopus subject areas

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

Fingerprint Dive into the research topics of 'Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [<sup>11</sup>C]hemicholinium-3 and [<sup>18</sup>F]hemicholinium-3'. Together they form a unique fingerprint.

  • Cite this

    Zheng, Q. H., Gao, M., Mock, B. H., Wang, S., Hara, T., Nazih, R., Miller, M. A., Receveur, T. J., Lopshire, J. C., Groh, W. J., Zipes, D. P., Hutchins, G. D., & DeGrado, T. R. (2007). Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3. Bioorganic and Medicinal Chemistry Letters, 17(8), 2220-2224. https://doi.org/10.1016/j.bmcl.2007.01.105