Synthesis and in vivo evaluation of a PET radioligand for imaging the endothelin-A receptor

William B. Mathews, Tamas G. Zober, Hayden T. Ravert, Ursula Scheffel, John Hilton, Darryl Sleep, Robert F. Dannals, Zsolt Szabo

Research output: Contribution to journalArticle

Abstract

The endothelin-A receptor ligand Atrasentan (ABT-627) was radiolabeled by 11C-methylaton of the desmethyl precursor in phenolate form. In mice, the highest uptake of [11C]ABT-627 was in the liver, kidneys and lungs. No significant binding was observed in mouse brain or heart. PET studies in a baboon, however, showed accumulation in the myocardium and lungs with a tissue/blood equilibrium reached at 40 min postinjection. Between 35 and 75 min, the heart/blood and lung/blood ratios were 1.72 and 1.31, respectively. Pretreatment with a 0.39 mg/kg dose of unlabeled ABT-627 inhibited the uptake of the tracer by 53-54% in both the myocardium and lungs at 65 min.

Original languageEnglish (US)
Pages (from-to)15-19
Number of pages5
JournalNuclear Medicine and Biology
Volume33
Issue number1
DOIs
StatePublished - Jan 1 2006

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Keywords

  • ABT-627
  • Atrasentan
  • Baboon
  • Endothelin
  • PET

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

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