锝-99m标记edda -tricine- hyic - tyr³-奥曲肽的初步研究:诊断神经内分泌肿瘤的放射性药物开发

L. T. U. H. Melero, E. Muramoto, E. B. Araújo
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摘要

在闪烁成像中使用对器官或受体具有高特异性的标记分子可以产生良好的局部图像,并最大限度地减少其他器官的暴露。奥曲肽是第一个生长抑素合成类似物,用于临床应用于生长抑素受体(sstr)超表达肿瘤的定位。本文研究了99mTc对hyic - tyr3 -奥曲肽的标记及标记物在正常瑞士小鼠体内的生物分布。使用hynico - toc 20 μg、EDDA 10 mg、tricine 20 mg、SnCl2.2H2O 15 μg、pH 7.5、沸水浴10 min时,获得了较高的放化学产率。生物分布研究表明,标记肽的血液清除速度快,肾脏摄取和尿排泄量高。腹部低背景有利于神经内分泌肿瘤的诊断。
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Preliminary studies of EDDA-tricine-HYNIC-Tyr³-octreotide labelled with technetium-99m: radiopharmaceutical development for the diagnosis of neuroendocrine tumours
The use of labelled molecules with high specificity for an organ or receptor in scintigraphy generates good local images and minimises the exposure of other organs. Octreotide was the first somatostatin synthetic analogue introduced in clinical use in the localisation of tumours with superexpression of somatostatin receptor (sstr). This work studied the labelling of HYNIC-Tyr3-octreotide with 99mTc and the biodistribution of labelled compounds in normal Swiss mice. A high radiochemical yield was obtained when using 20 μg of HYNIC-TOC, 10 mg of EDDA, 20 mg of tricine, 15 μg of SnCl2.2H2O, pH 7.5 and 10 min of boiling water bath. Biodistribution studies showed fast blood clearance of the labelled peptide with high kidney uptake and urinary excretion. The low background in the abdominal region is favourable for the diagnosis of neuroendocrine tumours.
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