A novel radioligand for imaging the AT1 angiotensin receptor with PET

被引:24
作者
Mathews, WB
Yoo, SE
Scheffel, U
Rauseo, PA
Zober, TG
Gocco, G
Sandberg, K
Ravert, HT
Dannals, RF
Szabo, Z
机构
[1] Johns Hopkins Med Inst, Dept Radiol, Baltimore, MD 21287 USA
[2] Korea Res Inst Chem Technol, Taejon 305606, South Korea
[3] Georgetown Univ, Med Ctr, Dept Med, Washington, DC 20007 USA
[4] Georgetown Univ, Med Ctr, Dept Physiol, Washington, DC 20007 USA
关键词
angiotensin; AT(1); hypertension; KR31173; mice; PET;
D O I
10.1016/j.nucmedbio.2003.10.014
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
2-Butyl-5-methoxymethyl-6-(1-oxopyridin-2-yl)-3-[[2'-(1H-tetrazol-5-yl)bipheny1-4-yl]methyl]-3H-imidazo[4,5-b]pyridine (KR31173) was radiolabeled by coupling a tetrazole-protected hydroxy precursor with [C-11] methyl iodide and removing the protecting group by acid hydrolysis. In mice, the highest uptake of [C-11] 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. (C) 2004 Elsevier Inc. All rights reserved.
引用
收藏
页码:571 / 574
页数:4
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