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在一名志愿者身上首次评估锝-99m二巯基丙酰白蛋白作为脑室造影可能的示踪剂。

First evaluation of technetium-99m dimercaptopropionyl albumin as a possible tracer agent for ventriculography in a volunteer.

作者信息

Verbeke K A, Vanhecke W B, Mortelmans L A, Verbruggen A M

机构信息

Laboratory of Radiopharmaceutical Chemistry, F.F.W., K.U. Leuven, Belgium.

出版信息

Eur J Nucl Med. 1994 Sep;21(9):906-12. doi: 10.1007/BF00238113.

Abstract

Technetium-99m labelled red blood cells (99mTc-RBCs) are the standard radiopharmaceutical for radionuclide ventriculography but suffer from some practical disadvantages such as risk of viral contamination and lengthy preparation (in vitro labelling) or poor labelling efficiency due to patient medication interactions (in vivo labelling). 99mTc-labelled human serum albumin (HSA) is not really a valuable alternative as the activity diffuses too rapidly out of the vascular space due to the weak binding of the radionuclide. We have modified HSA by reaction with N-hydroxysuccinimidyl 2,3-di(S-acetylmercapto)propionate (SAMP) to introduce a varying number of 2,3-dimercaptopropionyl (DMP) side chains. The resulting DMP-HSA can be rapidly labelled with 99mTc at room temperature by simple addition of stannous ions and eluate of a 99mTc generator. After evaluation in mice and rabbits, two different 99mTc-DMP-HSA preparations - obtained after reaction of SAMP with albumin in a molar ratio of, respectively, 8:1 and 16:1 - were tested in a volunteer and compared to 99mTc-RBCs. The blood time-activity curves of the three preparations were quite similar but both 99mTc-DMP-HSA preparations were excreted much less into the urine than 99mTc-RBCs. Ventriculography was performed with the three tracer agents, each time with a 1-week interval. In the three studies, the heart was clearly visualized and the left and right ventricle could be easily delineated. The ejection fractions obtained after administration of the three preparations were similar. With both 99mTc-DMP-HSA preparations the low activity in the spleen was a distinct advantage and facilitated delineation of the left ventricle.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

锝-99m标记的红细胞(99mTc-RBCs)是放射性核素心室造影的标准放射性药物,但存在一些实际缺点,如病毒污染风险和制备过程冗长(体外标记),或因患者药物相互作用导致标记效率低下(体内标记)。99mTc标记的人血清白蛋白(HSA)并非真正有价值的替代物,因为由于放射性核素的弱结合,其活性从血管空间扩散得太快。我们通过与N-羟基琥珀酰亚胺2,3-二(S-乙酰巯基)丙酸酯(SAMP)反应对HSA进行了修饰,以引入不同数量的2,3-二巯基丙酰(DMP)侧链。所得的DMP-HSA可通过简单添加亚锡离子和99mTc发生器洗脱液在室温下快速用99mTc标记。在小鼠和兔子中进行评估后,将SAMP与白蛋白分别以8:1和16:1的摩尔比反应得到的两种不同的99mTc-DMP-HSA制剂在一名志愿者身上进行了测试,并与99mTc-RBCs进行了比较。三种制剂的血液时间-活性曲线非常相似,但两种99mTc-DMP-HSA制剂比99mTc-RBCs向尿液中的排泄量要少得多。用这三种示踪剂进行心室造影,每次间隔1周。在这三项研究中,心脏均清晰可见,左、右心室易于勾勒。给予三种制剂后获得的射血分数相似。两种99mTc-DMP-HSA制剂在脾脏中的低活性是一个明显的优势,有助于左心室的勾勒。(摘要截断于250字)

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