A novel radioligand for imaging the AT1 angiotensin receptor with PET

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 hig...

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Bibliographic Details
Published in:Nuclear medicine and biology 2004-07, Vol.31 (5), p.571-574
Main Authors: Mathews, William B, Yoo, Sung-Eun, Lee, Sung-Hou, Scheffel, Ursula, Rauseo, Paige A, Zober, Tamas G, Gocco, Gerard, Sandberg, Kathryn, Ravert, Hayden T, Dannals, Robert F, Szabo, Zsolt
Format: Article
Language:English
Subjects:
Adrenal Glands - diagnostic imaging
Adrenal Glands - metabolism
Animals
Carbon Radioisotopes - pharmacokinetics
Imidazoles - pharmacokinetics
Kidney - diagnostic imaging
Kidney - metabolism
Ligands
Liver - diagnostic imaging
Liver - metabolism
Male
Mice
Organ Specificity
Positron-Emission Tomography - methods
Radiopharmaceuticals - pharmacokinetics
Receptor, Angiotensin, Type 1 - metabolism
Reproducibility of Results
Sensitivity and Specificity
Tetrazoles - pharmacokinetics
Tissue Distribution
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Summary: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.
ISSN:0969-8051
DOI:10.1016/j.nucmedbio.2003.10.014