VALIDATION OF 3-DEOXY-3-FLUORO-D-GLUCOSE AS A GLUCOSE-TRANSPORT ANALOG IN RAT-HEART
VALIDATION OF 3-DEOXY-3-FLUORO-D-GLUCOSE AS A GLUCOSE-TRANSPORT ANALOG IN RAT-HEART
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DOI：
10.1152/ajpheart.1984.247.5.h754
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发表时间：
1984-01-01
影响因子：
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通讯作者：
HOLDEN, JE
中科院分区：
文献类型：
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作者：
HALAMA, JR;GATLEY, SJ;HOLDEN, JE
从四个方面研究了3-脱氧-3-氟-D-葡萄糖(D-3FDG)的行为。大鼠静脉注射标记物在组织中的分布。比较[18F]D-3FDG与标记3-脱氧-3-氟-L-葡萄糖(L-3FDG)的给药情况。结果与生理D-异构体更大的分布体积以及肾脏的一定程度的重吸收是一致的。大脑中排除了L-3FDG，但不排除其D-异构体。D-3FDG竞争性抑制大鼠离体心对葡萄糖的摄取。抑制常数为12.8.+-。1.6毫米，6.1.+-。1.1 mm为3-O-甲基-D-葡萄糖。给离体心推注[18F]D-3FDG后得到的残留曲线表明，示踪剂的磷酸化速度低于2-脱氧-2-氟-D-葡萄糖，但随后的去磷酸化速度更快。对注射[18F]D-3FDG后残留在组织中的18F进行了层析分析，发现除了游离的D-3FDG外，还有其他3个峰。这些在碱性磷酸酶处理后消失，并被归类为磷酸盐。主要代谢产物与己糖激酶法制备的D-3FDG-6-磷酸具有相同的保留时间。在血液中没有检测到磷酸化代谢物。18F标记的D-3FDG可能是研究葡萄糖转运和代谢的一种有用的示踪剂。
Four aspects of the behavior of 3-deoxy-3-fluoro-D-glucose (D-3FDG) were studied. The distribution of label in rat tissues after i.v. 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 3 other peaks. These disappeared after treatment with alkaline phosphatase and were 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.