Assessment of Cu-ETS as a PET radiopharmaceutical for evaluation of regional renal perfusion
Assessment of Cu-ETS as a PET radiopharmaceutical for evaluation of regional renal perfusion
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DOI：
10.1016/j.nucmedbio.2007.01.002
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发表时间：
2007-04-01
影响因子：
3.1
通讯作者：
Hutchins, Gary D.
中科院分区：
文献类型：
--
作者：
Green, Mark A.;Mathias, Carla J.;Hutchins, Gary D.
乙乙二醛双（缩氨基硫脲）（Cu-ETS）的铜（II）配合物作为正电子发射断层扫描（PET）放射性药物进行评价，用于评估区域肾灌注。研究方法：在四个未成熟的农场猪使用共同注射的Sc-46-和Co-57-微球给药到左心室的一致性肾流量估计得到了证实，与11和15 μ m的微球。使用未成熟的农场猪（n=3）和成熟的哥廷根小型猪（n = 6），将静脉内[Cu-64] Cu-ETS给药后的局部肾放射性铜摄取与肾灌注的微球测量进行比较。通过肾脏PET成像进一步研究[Cu-64] Cu-ETS的分布和动力学。在体外评价血液对[Cu-64] Cu-ETS的分解速率，采用辛醇萃取法回收完整的[Cu-64]Cu-ETS。结果：共注射的11和15 μ m微球提供了相似的肾流量估计。静脉注射[（64）Cu]Cu-ETS的肾摄取与使用微球测量的局部肾灌注之间观察到线性关系。[Cu-64]Cu-ETS提供了高质量的PET肾脏图像，证明了从高流量外皮质到低流量髓质的预期计数梯度。当孵育与派血在体外在37摄氏度，[Cu-64] Cu-ETS放射性药物被观察到分解的半衰期为2.8分钟。结论：Cu-ETS出现适合作为PET放射性药物用于评价区域肾灌注，提供肾摄取的放射性铜，微球灌注测量线性变化。用[Cu-60，Cu-61.62.64]Cu-ETS定量肾灌注（ml min（-1）g（-）1（））将需要校正动脉输入函数，以获得作为完整Cu-ETS放射性药物存在的血液放射性铜的分数，因为Cu-ETS螯合物在血液中具有有限的化学稳定性。血液样本的快速辛醇提取似乎适合作为捕获[Cu-60/61/62/64] Cu-ETS实际血液浓度的方法。(c)2007年爱思唯尔公司All rights reserved.
The copper(II) complex of ethylglyoxal bis(thiosemicarbazone) (Cu-ETS) was evaluated as a positron emission tomography (PET) radiopharmaceutical for assessment of regional renal perfusion. Methods: The concordance of renal flow estimates obtained with 11- and 15-mu m microspheres was confirmed in four immature farm pigs using co-injected Sc-46- and Co-57-microspheres administered into the left ventricle. With the use of both immature farm pigs (n=3) and mature Gottingen minipigs (n = 6), regional renal radiocopper uptake following intravenous [Cu-64] Cu-ETS administration was compared to microsphere measurements of renal perfusion. The distribution and kinetics of [Cu-64] Cu-ETS were further studied by PET imaging of the kidneys. The rate of [Cu-64]Cu-ETS decomposition by blood was evaluated in vitro, employing octanol extraction to recover intact [Cu-64]Cu-ETS. Results: The co-injected 11- and 15-mu m microspheres provided similar estimates of renal flow. A linear relationship was observed between the renal uptake of intravenous [(64) Cu]Cu-ETS and regional renal perfusion measured using microspheres. [Cu-64]Cu-ETS provided high-quality PET kidney images demonstrating the expected count gradient from high-flow outer cortex to low-flow medulla. When incubated with pie blood in vitro at 37 degrees C, the [Cu-64] Cu-ETS radiopharmaceutical was observed to decompose with a half-time of 2.8 min. Conclusion: Cu-ETS appears suitable for use as a PET radiopharmaceutical for evaluation of regional renal perfusion, affording renal uptake of radiocopper that varies linearly with microsphere perfusion measurements. Quantification of renal perfusion (in ml min(-1) g(-)1()) with [Cu-60,Cu-61.62.64]Cu-ETS will require correcting the arterial input function for the fraction of blood radiocopper remaining present as the intact Cu-ETS radiopharmaceutical, since the Cu-ETS chelate has limited chemical stability in blood. Rapid octanol extraction of blood samples appears suitable as an approach to capturing the actual blood concentration of [Cu-60/61/62/64] Cu-ETS. (c) 2007 Elsevier Inc. All rights reserved.