对β1肾上腺素能受体具有选择性的（18）F配体的合成与心脏成像
Synthesis and Cardiac Imaging of (18)F-Ligands Selective for β1-Adrenoreceptors.
作者信息
Radeke Heike S, Purohit Ajay, Harris Thomas D, Hanson Kelley, Jones Reinaldo, Hu Carol, Yalamanchili Padmaja, Hayes Megan, Yu Ming, Guaraldi Mary, Kagan Mikhail, Azure Michael, Cdebaca Michael, Robinson Simon, Casebier David
机构信息
Research and Development, Lantheus Medical Imaging , 331 Treble Cove Road, North Billerica, Massachusetts 01862, United States.
出版信息
ACS Med Chem Lett. 2011 Jul 22;2(9):650-5. doi: 10.1021/ml1002458. eCollection 2011 Sep 8.
Abstract
A series of potent and selective β1-adrenoreceptor ligands were identified (IC50 range, 0.04-0.25 nM; β1/β2 selectivity range, 65-450-fold), labeled with the PET radioisotope fluorine-18 and evaluated in normal Sprague-Dawley rats. Tissue distribution studies demonstrated uptake of each radiotracers from the blood pool into the myocardium (0.48-0.62% ID/g), lung (0.63-0.97% ID/g), and liver (1.03-1.14% ID/g). Dynamic μPET imaging confirmed the in vivo dissection studies.
摘要
一系列强效且选择性的β1-肾上腺素能受体配体被鉴定出来（IC50范围为0.04 - 0.25 nM；β1/β2选择性范围为65 - 450倍），用正电子发射断层扫描（PET）放射性同位素氟-18进行标记，并在正常的斯普拉格-道利大鼠中进行评估。组织分布研究表明，每种放射性示踪剂从血池摄取到心肌（0.48 - 0.62% ID/g）、肺（0.63 - 0.97% ID/g）和肝脏（1.03 - 1.14% ID/g）中。动态微型正电子发射断层扫描（μPET）成像证实了体内解剖研究。
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