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

Research output: Contribution to journalArticle

30 Citations (Scopus)

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
Pages (from-to)2220-2224
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number8
DOIs
StatePublished - Apr 15 2007

Fingerprint

Hemicholinium 3
Heart Neoplasms
Brain
Positron emission tomography
Solid Phase Extraction
Biomarkers
Brain Neoplasms
Glioma
Positron-Emission Tomography
Cations
Rats
Tumors
Heart Diseases
Ion exchange
choline transporter

Keywords

  • [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

Cite this

Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3. / Zheng, Qi-Huang; Gao, Mingzhang; Mock, Bruce H.; Wang, Shuyan; Hara, Toshihiko; Nazih, Rachid; Miller, Michael A.; Receveur, Tim J.; Lopshire, John C.; Groh, William; Zipes, Douglas P.; Hutchins, Gary; DeGrado, Timothy R.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 8, 15.04.2007, p. 2220-2224.

Research output: Contribution to journalArticle

Zheng, Qi-Huang ; Gao, Mingzhang ; Mock, Bruce H. ; Wang, Shuyan ; Hara, Toshihiko ; Nazih, Rachid ; Miller, Michael A. ; Receveur, Tim J. ; Lopshire, John C. ; Groh, William ; Zipes, Douglas P. ; Hutchins, Gary ; DeGrado, Timothy R. / Synthesis and biodistribution of new radiolabeled high-affinity choline transporter inhibitors [11C]hemicholinium-3 and [18F]hemicholinium-3. In: Bioorganic and Medicinal Chemistry Letters. 2007 ; Vol. 17, No. 8. pp. 2220-2224.
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