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18F标记嘧啶的研究。II. 大鼠体内18F-5-氟尿嘧啶、18F-5-氟-2'-脱氧尿苷和18F-5-氟尿苷的代谢研究。

Studies on 18F-labeled pyrimidines. II. Metabolic investigation of 18F-5-fluorouracil, 18F-5-fluoro-2'-deoxyuridine and 18F-5-fluorouridine in rats.

作者信息

Ishiwata K, Ido T, Kawashima K, Murakami M, Takahashi T

出版信息

Eur J Nucl Med. 1984;9(4):185-9. doi: 10.1007/BF00251469.

DOI:10.1007/BF00251469
PMID:6232143
Abstract

18F-labeled 5-fluorouracil(FUra), 5-fluoro-2'-deoxyuridine(FdUrd), and 5-fluorouridine ( FUrd ) were synthesized with high radiochemical purities. The 18F-labeled pyrimidines were injected into rats. The metabolites in serum, bile, and urine were analyzed up to 2 h after administration by radio-high performance liquid chromatography (HPLC). The blood clearance of three pyrimidines was very rapid. In the serum the nucleosides and base disappeared very rapidly with a biological half-life of about 2 min and most of them had disappeared by 60 min. The metabolites in the urine were similar to those in the serum. In the bile pyrimidine nucleosides and base were not detected. 18F- was found in the metabolites. Our results explain the high uptakes in the kidney and liver in biodistribution studies of the 18F-labeled pyrimidines.

摘要

合成了具有高放射化学纯度的18F标记的5-氟尿嘧啶(FUra)、5-氟-2'-脱氧尿苷(FdUrd)和5-氟尿苷(FUrd)。将18F标记的嘧啶注入大鼠体内。给药后2小时内,通过放射性高效液相色谱(HPLC)分析血清、胆汁和尿液中的代谢物。三种嘧啶的血液清除非常迅速。血清中的核苷和碱基消失得非常快,生物半衰期约为2分钟,大部分在60分钟内就已消失。尿液中的代谢物与血清中的相似。在胆汁中未检测到嘧啶核苷和碱基。在代谢物中发现了18F。我们的结果解释了在18F标记的嘧啶生物分布研究中肾脏和肝脏的高摄取情况。

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Studies on 18F-labeled pyrimidines III. Biochemical investigation of 18F-labeled pyrimidines and comparison with 3H-deoxythymidine in tumor-bearing rats and mice.18F 标记嘧啶的研究 III. 18F 标记嘧啶的生化研究以及在荷瘤大鼠和小鼠中与 3H-脱氧胸苷的比较。
Eur J Nucl Med. 1985;10(1-2):39-44. doi: 10.1007/BF00261761.
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Metabolic changes of glioma following chemotherapy: an experimental study using four PET tracers.化疗后胶质瘤的代谢变化:一项使用四种正电子发射断层显像剂的实验研究
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An improved synthesis of 18F-5-fluorouracil.18F - 5 - 氟尿嘧啶的改进合成方法。
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Metabolic trapping as a principle of oradiopharmaceutical design: some factors resposible for the biodistribution of [18F] 2-deoxy-2-fluoro-D-glucose.代谢捕获作为放射性药物设计的一项原则:影响[18F]2-脱氧-2-氟-D-葡萄糖生物分布的一些因素
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Distribution of 18F-5-fluorouracil in tumor-bearing mice and rats.18F - 5 - 氟尿嘧啶在荷瘤小鼠和大鼠体内的分布。
Int J Nucl Med Biol. 1978 Mar;5(1):19-28. doi: 10.1016/0047-0740(78)90086-4.