锝-3SPboroxime：一种带正电荷的锝(III)放射性示踪剂，具有很高的心脏摄取率和较长的心肌滞留时间。
Tc-3SPboroxime: A neutral Tc(III) radiotracer with high heart uptake and long myocardial retention.
机构信息
Department of Nuclear Medicine, Fuwai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences and Peking Union Medical College, No. 167 North Lishi Road, Xicheng District, Beijing, 100037, China.
Nuclear Science and Engineering Institute, University of Missouri-Columbia, Columbia, MO, USA.
出版信息
J Nucl Cardiol. 2021 Dec;28(6):2687-2696. doi: 10.1007/s12350-020-02087-3. Epub 2020 Mar 16.
BACKGROUND
Tc-3SPboroxime is a Tc(III) complex with high initial heart uptake comparable to that of Tc-Teboroxime, but with significantly longer myocardial retention in Sprague-Dawley rats. This study was performed to demonstrate its feasibility on myocardial perfusion imaging and myocardial blood flow quantification in swine models.
METHODS
Dynamic single-photon emission computed tomography (SPECT) studies with Tc-3SPboroxime were performed in normal (with/without dipyridamole, n = 9) and acute myocardial infarction (AMI) swine (n = 3) in comparison with Tc-Teboroxime and Tc-Sestamibi. List-mode acquisitions were immediately started after injection and continued for 15 minutes. Regions of interest were drawn on heart (infarct and remote areas of AMI swine) and liver to generate time activity curves. Heart/liver and infarct/remote radioactivity ratios were calculated. One-tissue compartment model was implemented to obtain K and K values.
RESULTS
The initial heart uptake of Tc-3SPboroxime was close to that of Tc-Teboroxime, but higher than that of Tc-Sestamibi. Tc-3SPboroxime had a myocardial retention longer than that of Tc-Teboroxime. The heart/liver ratio of Tc-3SPboroxime was higher than that of Tc-Teboroxime at later stage (13-15 minutes post-injection). The K value of Tc-3SPboroxime was much higher than that of Tc-Sestamibi, and the K value was significantly lower than that of Tc-Teboroxime both at rest and dipyridamole stress (rest K: 0.63 ± 0.11 vs 0.40 ± 0.04 mL·min·g, P = 0.027; stress K: 0.89 ± 0.05 vs 0.54 ± 0.08 mL·min·g, P = 0.031; rest K: 0.22 ± 0.04 vs 0.33 ± 0.11 mL·min·g, P = 0.003; stress K: 0.31 ± 0.03 vs 0.60 ± 0.30 mL·min·g, P = 0.047). High quality SPECT images could be obtained in any of the 5 minutes windows over the first 15 minutes after injection of Tc-3SPboroxime in normal and AMI swine models. Apical and anterior perfusion defects were clearly visualized in AMI swine.
CONCLUSION
Tc-3SPboroxime is a promising radiotracer for future clinical translation considering its heart uptake, heart/liver ratio and SPECT image quality, as well as the advantage over Tc-Sestamibi in the definition of stress flow.
背景
Tc-3SPboroxime 是一种 Tc(III) 络合物，具有与 Tc-Teboroxime 相当的初始心脏摄取率，但心肌保留时间明显更长，在 Sprague-Dawley 大鼠中。本研究旨在证明其在猪模型中的心肌灌注成像和心肌血流定量中的可行性。
方法
在正常（有/无双嘧达莫，n=9）和急性心肌梗死（AMI）猪（n=3）中进行 Tc-3SPboroxime 的动态单光子发射计算机断层扫描（SPECT）研究，并与 Tc-Teboroxime 和 Tc-Sestamibi 进行比较。在注射后立即开始进行列表模式采集，并持续 15 分钟。在心脏（AMI 猪的梗死和远隔区域）和肝脏上绘制感兴趣区域以生成时间活动曲线。计算心脏/肝脏和梗死/远隔放射性比值。实施单室模型以获得 K 和 K 值。
结果
Tc-3SPboroxime 的初始心脏摄取率接近 Tc-Teboroxime，但高于 Tc-Sestamibi。Tc-3SPboroxime 的心肌保留时间长于 Tc-Teboroxime。Tc-3SPboroxime 的心脏/肝脏比值在后期（注射后 13-15 分钟）高于 Tc-Teboroxime。Tc-3SPboroxime 的 K 值远高于 Tc-Sestamibi，且在静息和双嘧达莫应激时均低于 Tc-Teboroxime（静息 K：0.63±0.11 比 0.40±0.04 mL·min·g，P=0.027；应激 K：0.89±0.05 比 0.54±0.08 mL·min·g，P=0.031；静息 K：0.22±0.04 比 0.33±0.11 mL·min·g，P=0.003；应激 K：0.31±0.03 比 0.60±0.30 mL·min·g，P=0.047）。在正常和 AMI 猪模型中，注射 Tc-3SPboroxime 后前 15 分钟内的任何 5 分钟窗口内都可以获得高质量的 SPECT 图像。AMI 猪的心尖和前壁灌注缺损清晰可见。
结论
考虑到 Tc-3SPboroxime 的心脏摄取率、心脏/肝脏比值和 SPECT 图像质量，以及在应激血流定义方面优于 Tc-Sestamibi 的优势，它是一种很有前途的用于未来临床转化的放射性示踪剂。
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