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 2006

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Endothelin A Receptors
Lung
Myocardium
Papio
Ligands
Kidney
atrasentan
Liver
Brain

Keywords

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

ASJC Scopus subject areas

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

Cite this

Synthesis and in vivo evaluation of a PET radioligand for imaging the endothelin-A receptor. / Mathews, William B; Zober, Tamas G.; Ravert, Hayden T.; Scheffel, Ursula; Hilton, John; Sleep, Darryl; Dannals, Robert F; Szabo, Zsolt.

In: Nuclear Medicine and Biology, Vol. 33, No. 1, 01.2006, p. 15-19.

Research output: Contribution to journalArticle

Mathews, William B ; Zober, Tamas G. ; Ravert, Hayden T. ; Scheffel, Ursula ; Hilton, John ; Sleep, Darryl ; Dannals, Robert F ; Szabo, Zsolt. / Synthesis and in vivo evaluation of a PET radioligand for imaging the endothelin-A receptor. In: Nuclear Medicine and Biology. 2006 ; Vol. 33, No. 1. pp. 15-19.
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