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

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2004年 / 31卷 / 05期

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

页码：571 / 574

页数：4