Radiosynthesis and biological evaluation of a promising σ2-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer

Zhude Tu, Jinbin Xu, Lynne A. Jones, Shihong Li, Dexing Zeng, Mei Ping Kung, Hank F. Kung, Robert H. Mach

Research output: Contribution to journalArticlepeer-review

22 Scopus citations

Abstract

Sigma-2 receptors represent an endogenous marker for proliferation in solid tumors. The high affinity, high selectivity σ2 receptor ligand N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2-(2-fluoroethoxy)-5-iodo-3-methoxybenzamide (3) was separately radiolabeled with F-18 and I-125. The radiolabeling yield was 30% and 70% for [18F]3 and [125I]3, respectively. Studies of [125I]3 using murine 66 breast tumor membrane homogenates and evaluation of [18F]3 and [125I]3 in 66 tumor-bearing mice indicate that this ligand has potential as a PET or a SPECT probe for imaging σ2 receptors in breast cancer.

Original languageEnglish (US)
Pages (from-to)2268-2273
Number of pages6
JournalApplied Radiation and Isotopes
Volume68
Issue number12
DOIs
StatePublished - Dec 2010
Externally publishedYes

Keywords

  • Breast cancer
  • F-18
  • I-125
  • Molecular imaging
  • Sigma receptor

ASJC Scopus subject areas

  • Radiation

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