A novel radioligand for imaging the AT1 angiotensin receptor with PET

  • Nucl Med Biol. 2004 Jul;31(5):571-4. doi: 10.1016/j.nucmedbio.2003.10.014.
William B Mathews  1 ,  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
Affiliations
  • 1. Department of Radiology, Room B1151 Nelson Building, Johns Hopkins Medical Institutions, 600 North Wolfe St., Baltimore, MD 21287, USA. [email protected]
PMID: 15219274 DOI: 10.1016/j.nucmedbio.2003.10.014
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 [(11)C] methyl iodide and removing the protecting group by acid hydrolysis. In mice, the highest uptake of [(11)C] 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.

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