Haradahira T, Tanaka A, Maeda M, Kanazawa Y, Ichiya Y I, Masuda K
Research Development Corporation of Japan, Kawaguchi, Japan.
Nucl Med Biol. 1995 Aug;22(6):719-25. doi: 10.1016/0969-8051(95)00018-s.
Fluorine-18 labeled analog of D-fructose, 1-deoxy-1-[18F]fluoro-D- fructose (1-[18F]FDFrc), was synthesized by nucleophilic substitution of [18F]fluoride ion and the effect of the fluorine substitution on its in vivo metabolism was investigated. The tissue distributions of 1-[18F]FDFrc in rats and tumor bearing mice showed initial high uptake and subsequent rapid washout of the radioactivity in the principal sites of D-fructose metabolism (kidneys, liver and small intestine). The uptakes in the brain and tumor (fibrosarcoma) were the lowest and moderate, respectively, but tended to increase with time. The in vivo metabolic studies of 1-[18F]FDFrc and nonradioactive 1-FDFrc in mouse brain and tumor showed that the fluorinated analog remained unmetabolized in these tissues, indicating that the substitution of fluorine at the C-1 position produces a nonmetabolizable analog of D-fructose. Thus, 1-[18F]FDFrc had no features of a metabolic trapping tracer without showing any appreciable organ or tumor specific localization.
通过亲核取代[¹⁸F]氟离子合成了D-果糖的氟-18标记类似物1-脱氧-1-[¹⁸F]氟-D-果糖（1-[¹⁸F]FDFrc），并研究了氟取代对其体内代谢的影响。1-[¹⁸F]FDFrc在大鼠和荷瘤小鼠体内的组织分布显示，在D-果糖代谢的主要部位（肾脏、肝脏和小肠），放射性最初摄取较高，随后迅速清除。在大脑和肿瘤（纤维肉瘤）中的摄取分别最低和中等，但随时间有增加趋势。对1-[¹⁸F]FDFrc和非放射性1-FDFrc在小鼠脑和肿瘤中的体内代谢研究表明，氟化类似物在这些组织中未代谢，这表明在C-1位取代氟产生了一种不可代谢的D-果糖类似物。因此，1-[¹⁸F]FDFrc没有代谢捕获示踪剂的特征，也未显示出任何明显的器官或肿瘤特异性定位。
