Department of Nuclear Medicine, Aarhus University Hospital, Aarhus Sygehus, Denmark.
Scand J Clin Lab Invest. 2010 Apr 19;70(3):209-16. doi: 10.3109/00365511003663648.
The aim of this study was to establish a radio synthesis of (99m)Tc-HYNIC-lactadherin for in vivo studies and to perform biodistribution analysis studies in mice, comparing (99m)Tc-HYNIC-lactadherin to (99m)Tc-HYNIC-annexin V.
The radiochemical purity of (99m)Tc-HYNIC-lactadherin was optimized by varying the amount of SnCl(2) in the synthesis. Furthermore, the need for bovine serum albumin (BSA) as a stabilizing agent was evaluated by following the stability by radiochemical purity measurement with and without the addition of BSA. A total of 24 mice were assigned to groups of 15 and nine mice, respectively. The animals were sacrificed at different time points; 10 min, 60 min, and 180 min.
The synthesis of (99m)Tc-HYNIC-lactadherin for in vivo studies has been optimized to give a stable product without addition of BSA and with a radiochemical purity of more than 95%. Approximately 60% of the injected dose of (99m)Tc-HYNIC-lactadherin was found in the liver and 4-5% could be assigned to kidneys. In contrast, (99m)Tc-HYNIC-annexin V distributes with around 13% and 45% of the injected dose in liver and kidneys, respectively. Over the experimental period (10-180 min) only small distributional changes were observed for both probes.
In conclusion, the biodistribution of (99m)Tc-HYNIC-lactadherin, a potential new tracer for in vivo quantification of apoptosis, was evaluated. The small renal uptake of (99m)Tc-HYNIC-lactadherin makes it possible to image apoptosis in the kidneys, but the high liver clearance may be a disadvantage during myocardial perfusion.
本研究的目的是建立(99m)Tc-HYNIC-乳凝集素的放射性合成方法,用于体内研究,并通过比较(99m)Tc-HYNIC-乳凝集素与(99m)Tc-HYNIC-膜联蛋白 V 的体内分布分析来进行研究。
通过改变合成中 SnCl2 的量来优化(99m)Tc-HYNIC-乳凝集素的放射化学纯度。此外,通过添加和不添加牛血清白蛋白(BSA)时的放射化学纯度测量来评估 BSA 作为稳定剂的必要性。总共将 24 只小鼠分为 15 只一组和 9 只一组。动物在不同的时间点处死,分别为 10 分钟、60 分钟和 180 分钟。
(99m)Tc-HYNIC-乳凝集素的体内研究合成已得到优化,无需添加 BSA 即可得到稳定的产物,且放射化学纯度大于 95%。约 60%的注射剂量的(99m)Tc-HYNIC-乳凝集素在肝脏中发现,4-5%可归属于肾脏。相比之下,(99m)Tc-HYNIC-膜联蛋白 V 在肝脏和肾脏中的分布剂量分别约为 13%和 45%。在整个实验期间(10-180 分钟),两种探针的分布变化都很小。
总之,评估了潜在的用于体内定量检测细胞凋亡的新示踪剂(99m)Tc-HYNIC-乳凝集素的体内分布。(99m)Tc-HYNIC-乳凝集素的肾脏摄取量小,使得可以对肾脏中的细胞凋亡进行成像,但肝脏清除率高可能是心肌灌注期间的一个缺点。