A novel radioligand for imaging the AT1 angiotensin receptor with PET

William B. Mathews, Sung Eun Yoo, Sung Hou Lee, Ursula Scheffel, Paige A. Rauseo, Tamas G. Zober, Gerard Gocco, Kathryn Sandberg, Hayden T. Ravert, Robert F. Dannals, Zsolt Szabo

Research output: Contribution to journalArticlepeer-review

Abstract

2-Butyl-5-methoxymethyl-6-(1-oxopyridin-2-yl)-3-[[2′-(1H-tetrazol-5- yl)biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine (KR31173) was radiolabeled by coupling a tetrazole-protected hydroxy precursor with [11C] methyl iodide and removing the protecting group by acid hydrolysis. In mice, the highest uptake of [11C] KR31173 was in the adrenal glands, kidneys, and liver. Tissue to blood ratios were generally greater than 10:1. Uptake of the tracer in the adrenal glands, kidneys, lungs, and heart was blocked with a 1 mg/kg dose of KR31173 or MK-996.

Original languageEnglish (US)
Pages (from-to)571-574
Number of pages4
JournalNuclear Medicine and Biology
Volume31
Issue number5
DOIs
StatePublished - Jul 2004

Keywords

  • AT
  • Angiotensin
  • Hypertension
  • KR31173
  • Mice
  • PET

ASJC Scopus subject areas

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

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