Halama J R, Gatley S J, DeGrado T R, Bernstein D R, Ng C K, Holden J E
Am J Physiol. 1984 Nov;247(5 Pt 2):H754-9. doi: 10.1152/ajpheart.1984.247.5.H754.
Four aspects of the behavior of 3-deoxy-3-fluoro-D-glucose (D-3FDG) were studied. The distribution of label in rat tissues after intravenous administration of [18F]D-3FDG was compared with that seen with labeled 3-deoxy-3-fluoro-L-glucose (L-3FDG). Results were consistent with a larger volume of distribution for the physiological D-isomer coupled with some degree of reabsorption by the kidneys. L-3FDG, but not its D-isomer, was excluded from the brain. D-3FDG competitively inhibited uptake of glucose by isolated perfused rat hearts. The inhibition constant was 12.8 +/- 1.6 mM compared with 6.1 +/- 1.1 mM for 3-O-methyl-D-glucose. Residue curves obtained after bolus administration of [18F]D-3FDG to isolated hearts indicated phosphorylation of the tracer at a lower rate than for 2-deoxy-2-fluoro-D-glucose but with subsequent dephosphorylation at a faster rate. Chromatographic analysis of 18F remaining in tissues after administration of [18F]D-3FDG revealed in addition to free D-3FDG three other peaks. These disappeared after treatment with alkaline phosphatase and were thus assigned as phosphates. The principal metabolite had the same retention time as D-3FDG-6-phosphate prepared with hexokinase. No phosphorylated metabolites were detected in blood. D-3FDG labeled with 18F may be a useful tracer in studies of glucose transport and metabolism.
对3-脱氧-3-氟-D-葡萄糖（D-3FDG）的行为的四个方面进行了研究。静脉注射[¹⁸F]D-3FDG后大鼠组织中的标记物分布与用标记的3-脱氧-3-氟-L-葡萄糖（L-3FDG）观察到的分布进行了比较。结果与生理性D-异构体更大的分布容积以及肾脏一定程度的重吸收一致。L-3FDG被排除在脑外，但其D-异构体则不然。D-3FDG竞争性抑制离体灌注大鼠心脏对葡萄糖的摄取。抑制常数为12.8±1.6 mM，而3-O-甲基-D-葡萄糖的抑制常数为6.1±1.1 mM。向离体心脏推注[¹⁸F]D-3FDG后获得的残留曲线表明，示踪剂的磷酸化速率低于2-脱氧-2-氟-D-葡萄糖，但随后的去磷酸化速率更快。静脉注射[¹⁸F]D-3FDG后组织中剩余的¹⁸F的色谱分析显示，除了游离D-3FDG外还有其他三个峰。用碱性磷酸酶处理后这些峰消失，因此被确定为磷酸盐。主要代谢产物的保留时间与用己糖激酶制备的D-3FDG-6-磷酸相同。血液中未检测到磷酸化代谢产物。用¹⁸F标记的D-3FDG可能是葡萄糖转运和代谢研究中的一种有用示踪剂。
