用于靶向β-淀粉样蛋白的¹⁸F标记苯乙烯基苯并恶唑衍生物的放射性合成及体内评价
Radiosynthesis and in vivo evaluation of a ¹⁸F-labelled styryl-benzoxazole derivative for β-amyloid targeting.
作者信息
Ribeiro Morais G, Gano L, Kniess T, Bergmann R, Abrunhosa A, Santos I, Paulo A
机构信息
Radiopharmaceutical Sciences Group, IST/ITN, Instituto Superior Técnico, Universidade Técnica de Lisboa, EN 10, 2686-953 Sacavem, Portugal.
出版信息
Appl Radiat Isot. 2013 Dec;82:100-4. doi: 10.1016/j.apradiso.2013.07.003. Epub 2013 Jul 13.
The formation of β-amyloid deposits is considered a histopathological feature of Alzheimer's disease (AD). In vivo molecular imaging by means of amyloid-avid radiotracers will allow for an early and conclusive diagnostic of AD. Herein, we describe the radiosynthesis of the radiofluorinated styryl benzoxazole derivative [¹⁸F]-[2-[N-methyl-N-(2'-fluoroethyl)-4'-aminostyryl]benzoxazole] ([¹⁸F]-1) and its pre-clinical evaluation, including metabolic and biodistribution studies in male Wistar rats. The in vivo biological evaluation of [¹⁸F]-1 showed that this new radiotracer has a moderate brain uptake with a slow brain washout and a poor in vivo stability.
β-淀粉样蛋白沉积物的形成被认为是阿尔茨海默病（AD）的组织病理学特征。通过淀粉样蛋白亲和放射性示踪剂进行的体内分子成像将有助于对AD进行早期和确定性诊断。在此，我们描述了放射性氟化苯乙烯基苯并恶唑衍生物[¹⁸F]-2-[N-甲基-N-(2'-氟乙基)-4'-氨基苯乙烯基]苯并恶唑的放射性合成及其临床前评估，包括在雄性Wistar大鼠中的代谢和生物分布研究。[¹⁸F]-1的体内生物学评估表明，这种新型放射性示踪剂具有适度的脑摄取、缓慢的脑清除和较差的体内稳定性。
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