A novel radioligand for imaging the AT1 angiotensin receptor with PET
A novel radioligand for imaging the AT1 angiotensin receptor with PET
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DOI：
10.1016/j.nucmedbio.2003.10.014
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发表时间：
2004-07-01
影响因子：
3.1
通讯作者：
Szabo, Z
中科院分区：
文献类型：
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作者：
Mathews, WB;Yoo, SE;Szabo, Z
通过将四唑保护的羟基前体与[C-11]碘甲烷偶联并通过酸水解除去保护基，对2-丁基-5-甲氧基甲基-6-（1-氧代吡啶-2-基）-3-[[2 '-（1H-四唑-5-基）联苯-4-基]甲基]-3H-咪唑并[4，5-B]吡啶（KR 31173）进行放射性标记。在小鼠中，[C-11] KR 31173的最高摄取位于肾上腺、肾脏和肝脏中。组织与血液的比例通常大于10：1。以1 mg/kg剂量的KR 31173或MK-996阻断肾上腺、肾脏、肺和心脏对示踪剂的摄取。(C)2004爱思唯尔公司All rights reserved.
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.