Synthesis of [125I]iodoDPA-713: A new probe for imaging inflammation

Haofan Wang, Mrudula Pullambhatla, Tomas R. Guilarte, Ronnie C. Mease, Martin G. Pomper

Research output: Contribution to journalArticle

Abstract

[125I]IodoDPA-713 [125I]1, which targets the translocator protein (TSPO, 18 kDa), was synthesized in seven steps from methyl-4-methoxybenzoate as a tool for quantification of inflammation in preclinical models. Preliminary in vitro autoradiography and in vivo small animal imaging were performed using [125I]1 in a neurotoxicant-treated rat and in a murine model of lung inflammation, respectively. The radiochemical yield of [125I]1 was 44 ± 6% with a specific radioactivity of 51.8 GBq/μmol (1400 mCi/μmol) and >99% radiochemical purity. Preliminary studies showed that [125I]1 demonstrated increased specific binding to TSPO in a neurotoxicant-treated rat and increased radiopharmaceutical uptake in the lungs of an experimental inflammation model of lung inflammation. Compound [125I]1 is a new, convenient probe for preclinical studies of TSPO activity.

Original languageEnglish (US)
Pages (from-to)80-83
Number of pages4
JournalBiochemical and Biophysical Research Communications
Volume389
Issue number1
DOIs
StatePublished - Nov 6 2009

Keywords

  • Autoradiography
  • Peripheral benzodiazepine receptor
  • Pyrazolopyrimidine
  • Small animal imaging
  • Translocator protein

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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