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

doi:10.1016/j.nucmedbio.2003.10.014

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

School of Medicine

Research output: Contribution to journal › Article › peer-review

24 Scopus citations

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 language	English (US)
Pages (from-to)	571-574
Number of pages	4
Journal	Nuclear Medicine and Biology
Volume	31
Issue number	5
DOIs	https://doi.org/10.1016/j.nucmedbio.2003.10.014
State	Published - Jul 2004

Keywords

AT
Angiotensin
Hypertension
KR31173
Mice
PET

ASJC Scopus subject areas

Molecular Medicine
Radiology Nuclear Medicine and imaging
Cancer Research

Access to Document

10.1016/j.nucmedbio.2003.10.014

Cite this

@article{cc7235e2b19f40688aacc21728b80e7b,

title = "A novel radioligand for imaging the AT1 angiotensin receptor with PET",

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.",

keywords = "AT, Angiotensin, Hypertension, KR31173, Mice, PET",

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

note = "Funding Information: The authors thank Mr. Robert C. Smoot for his assistance with cyclotron operation and radiosynthesis. We also thank Merck Research Laboratories for providing us with MK-996. This work was supported by National Institutes of Health research grant number DK50183.",

year = "2004",

month = jul,

doi = "10.1016/j.nucmedbio.2003.10.014",

language = "English (US)",

volume = "31",

pages = "571--574",

journal = "Nuclear Medicine and Biology",

issn = "0969-8051",

publisher = "Elsevier Inc.",

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T1 - A novel radioligand for imaging the AT1 angiotensin receptor with PET

AU - Mathews, William B.

AU - Yoo, Sung Eun

AU - Lee, Sung Hou

AU - Scheffel, Ursula

AU - Rauseo, Paige A.

AU - Zober, Tamas G.

AU - Gocco, Gerard

AU - Sandberg, Kathryn

AU - Ravert, Hayden T.

AU - Dannals, Robert F.

AU - Szabo, Zsolt

N1 - Funding Information: The authors thank Mr. Robert C. Smoot for his assistance with cyclotron operation and radiosynthesis. We also thank Merck Research Laboratories for providing us with MK-996. This work was supported by National Institutes of Health research grant number DK50183.

PY - 2004/7

Y1 - 2004/7

N2 - 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.

AB - 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.

KW - AT

KW - Angiotensin

KW - Hypertension

KW - KR31173

KW - Mice

KW - PET

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