Analysis of metabolism of 6FDG: a PET glucose transport tracer.
Analysis of metabolism of 6FDG: a PET glucose transport tracer.
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DOI：
10.1016/j.nucmedbio.2010.12.007
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发表时间：
2011-07
影响因子：
3.1
通讯作者：
Ismail-Beigi F
中科院分区：
文献类型：
--
作者：
Muzic RF Jr;Chandramouli V;Huang HM;Wu C;Wang Y;Ismail-Beigi F
我们正在开发18F标记的6-氟-6-脱氧-D-葡萄糖（[18F] 6 FDG）作为葡萄糖转运的示踪剂。作为该过程的一部分，重要的是表征和定量推定的代谢物。与普遍存在的PET示踪剂18 F-标记的2-氟-2-脱氧-D-葡萄糖（[18 F]2FDG）（其被磷酸化并被捕获在细胞内）相反，氟取代[18 F] 6 FDG中碳6处的羟基应阻止其磷酸化。因此，[18F] 6 FDG有可能追踪葡萄糖代谢的转运步骤，而不会受到磷酸化和后续代谢步骤的干扰。本文的重点是确定静脉注射后[18 F] 6 FDG是否保持不变以及保持不变的程度。生物分布研究使用6 FDG标记的18 F以及寿命较长的放射性核素3 H和14 C。在静脉给药后1、6和24 h收获组织，从组织中提取放射性，并使用离子交换柱、高效液相色谱和化学反应性的组合进行分析。在1 h时间点，肝脏、脑、心脏、骨骼肌和血液中的绝大多数放射性被鉴定为6 FDG。在6小时和24小时时间点，有证据表明存在少量放射性物质，可能是6-氟-6-脱氧-D-山梨醇和6-氟-6-脱氧-D-葡萄糖酸。在PET成像研究的典型时间尺度上，[18 F] 6 FDG的放射性代谢物可忽略不计。
We are developing 18F-labeled 6-fluoro-6-deoxy-D-glucose ([18F]6FDG) as a tracer of glucose transport. As part of this process it is important to characterize and quantify putative metabolites. In contrast to the ubiquitous PET tracer 18F-labeled 2-fluoro-2-deoxy-D-glucose ([18F]2FDG) which is phosphorylated and trapped intracellularly, the substitution of fluorine for a hydroxyl group at carbon 6 in [18F]6FDG should prevent its phosphorylation. Consequently, [18F]6FDG has the potential to trace the transport step of glucose metabolism without the confounding effects of phosphorylation and subsequent steps of metabolism. Herein the focus is to determine whether, and the degree to which, [18F]6FDG remains unchanged following intravenous injection. Biodistribution studies were performed using 6FDG labeled with 18F as well as the longer-lived radionuclides 3H and 14C. Tissues were harvested at 1, 6, and 24 h following intravenous administration and radioactivity was extracted from the tissues and analyzed using a combination of ion exchange columns, high-performance liquid chromatography, and chemical reactivity. At the 1 h time-point, the vast majority of radioactivity in the liver, brain, heart, skeletal muscle, and blood was identified as 6FDG. At the 6- and 24-h time-points there was evidence of a minor amount of radioactive materials that appeared to be 6-fluoro-6-deoxy-D-sorbitol and possibly 6-fluoro-6-deoxy-D-gluconic acid. On the time scale typical of PET imaging studies radioactive metabolites of [18F]6FDG are negligible.
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DOI：
10.1152/ajpendo.00598.2004
发表时间：
2006-06-01
影响因子：
5.1
作者：
Pencek, RR;Bertoldo, A;Kelley, DE
通讯作者：
Kelley, DE
DOI：
10.1152/ajpendo.2000.279.5.e1064
发表时间：
2000-11-01
影响因子：
5.1
作者：
Halseth, AE;Bracy, DP;Wasserman, DH
通讯作者：
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DOI：
10.1123/ijsnem.16.5.485
发表时间：
2006-10-01
影响因子：
2.5
作者：
Lang, James A.;Gisolfi, Carl V.;Lambert, G. Patrick
通讯作者：
Lambert, G. Patrick
影响因子：
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作者：
HALAMA, JR;GATLEY, SJ;HOLDEN, JE
通讯作者：
HOLDEN, JE
影响因子：
4.7
作者：
DIENEL, GA;CRUZ, NF;SOKOLOFF, L
通讯作者：
SOKOLOFF, L