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Biodistribution of 99Tcm-labelled 5-thio-D-glucose.

机译:99Tcm标记的5-硫代-D-葡萄糖的生物分布。

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We studied the biodistribution and tumour localization of 99Tcm-labelled-5-thio-D-glucose (99Tcm-TG). 5-Thio-D-glucose was labelled with 99Tcm by direct stannous ion reduction. The biodistribution of 99Tcm-TG was investigated in normal rabbits and in mice bearing experimental tumours. In rabbits, the plasma and clearance of 99Tcm-TG was 14.5 +/- 2.0 and 11.3 +/- 3.0 ml.min-1 respectively. Urinary excretion at 1 h was 53 +/- 5%. 99Tcm-TG was injected intravenously in mice bearing MC26 colon carcinoma and tissue samples were analysed by gamma scintillation counting at various times. Uptake of 99Tcm-TG in tumour at 1 and 3 h was 1.6 +/- 0.3% and 1.2 +/- 0.3%; the tumour to muscle ratios were 2.7:1 and 4:1 respectively. The autoradiographic biodistribution of 99Tcm-TG in MX-1 human breast xenografted nude mice showed more persistent tumour uptake of 99Tcm-TG than 14C-2-deoxyglucose (14C-DG). 99Tcm-TG accumulated in the centre of the tumours; 14C-DG was decreased in this central region probably because of zones of infarction on necrosis. The discordance between the tumour uptake of 99Tcm-TG and 14C-DG indicates that 99Tcm-TG does not act like a glucose analog, suggesting 99Tcm-TG avidity for zones of infarction or necrosis. The further study of 99Tcm-TG in tumours and ischaemic injury is warranted.
机译:我们研究了99Tcm标记的5-thio-D-葡萄糖(99Tcm-TG)的生物分布和肿瘤定位。通过直接亚锡离子还原,用99Tcm标记5-Th-D-葡萄糖。研究了99Tcm-TG在正常兔和患有实验性肿瘤的小鼠中的生物分布。在兔中,99Tcm-TG的血浆和清除率分别为14.5 +/- 2.0和11.3 +/- 3.0 ml.min-1。 1小时尿排泄为53 +/- 5%。向患有MC26结肠癌的小鼠静脉内注射99Tcm-TG,并在不同时间通过伽玛闪烁计数分析组织样本。在第1和第3小时,肿瘤中99Tcm-TG的摄取为1.6 +/- 0.3%和1.2 +/- 0.3%;肿瘤与肌肉的比例分别为2.7:1和4:1。在MX-1人乳房异种移植裸鼠中99Tcm-TG的放射自显影生物分布显示,与14C-2-脱氧葡萄糖(14C-DG)相比,99Tcm-TG具有更高的持久性肿瘤吸收能力。 99Tcm-TG积累在肿瘤中心;在该中心区域14C-DG下降可能是由于坏死性梗死区。肿瘤摄取99Tcm-TG与14C-DG之间的差异表明99Tcm-TG不像葡萄糖类似物那样起作用,表明99Tcm-TG对于梗死或坏死区域具有亲和力。有必要对99Tcm-TG在肿瘤和缺血性损伤中进行进一步研究。

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