一种用于正电子发射断层扫描（PET）成像AT1血管紧张素受体的新型放射性配体。
A novel radioligand for imaging the AT1 angiotensin receptor with PET.
作者信息
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
机构信息
Department of Radiology, Room B1151 Nelson Building, Johns Hopkins Medical Institutions, 600 North Wolfe St., Baltimore, MD 21287, USA.
出版信息
Nucl Med Biol. 2004 Jul;31(5):571-4. doi: 10.1016/j.nucmedbio.2003.10.014.
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.
2-丁基-5-甲氧基甲基-6-(1-氧代吡啶-2-基)-3-[[2'-(1H-四氮唑-5-基)联苯-4-基]甲基]-3H-咪唑并[4,5-b]吡啶（KR31173）通过将四氮唑保护的羟基前体与[(11)C]碘甲烷偶联并通过酸水解去除保护基团进行放射性标记。在小鼠中，[(11)C]KR31173的最高摄取部位是肾上腺、肾脏和肝脏。组织与血液的比率通常大于10:1。给予1mg/kg剂量的KR31173或MK-996可阻断示踪剂在肾上腺、肾脏、肺和心脏中的摄取。
Zotero 插件