Impact of boronate capping groups on biological characteristics of novel (99m)Tc(III) complexes [(99m)TcCl(CDO)(CDOH)2B-R] (CDOH2 = cyclohexanedione dioxime).
Impact of boronate capping groups on biological characteristics of novel (99m)Tc(III) complexes [(99m)TcCl(CDO)(CDOH)2B-R] (CDOH2 = cyclohexanedione dioxime).
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硼酸酯封端基团对新型 (99m)Tc(III) 配合物 [(99m)TcCl(CDO)(CDOH)2B-R]（CDOH2 = 环己二酮二肟）生物学特性的影响。
DOI：
10.1021/bc500583k
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发表时间：
2015-01
期刊：
影响因子：
--
通讯作者：
Liu Shuang
中科院分区：
文献类型：
--
作者：
Yang Yong;Zheng Yumin;Tomaselli Elena;Fang Wei;Liu Shuang
本研究旨在探讨硼酸盐组对新型（99m）Tc（III）复合物[(99m)TcCl(CDO)(CDOH)2B-R] (（99m)Tc-异硼肟：R =异恶唑-4-yl (IS)）的心脏摄取和心肌保留的影响；（99m） tc - mpbor肟：R = n -甲基吡啶（MP）；（99m）Tc-PAboroxime: R = pyrazol-3-yl (PA)；（99m） tc - pybor肟：R = pyridin-3-yl (PY)；（99m） tc - 5ubor肟：R =尿嘧啶-5-基（5U）)。五种新的（99m）Tc（III）放射性示踪剂均以高产率和高放射化学纯度（RCP = 90-98%）制备，并在试剂盒混合物中保持稳定bbb6 h。使用SD大鼠进行生物分布和成像（平面和SPECT）研究。平面图像定量比较两组心肌保留和肝脏清除动力学。心脏保留和肝脏清除率曲线最符合双指数衰减函数。注射后0-1 min的初始心脏摄取顺序为（99m） tc - isboroxme(4.98±1.05%ID) ~ (99m) tc - teboroxme(4.56±0.91%ID) ~ (99m) tc - pboroxme(4.03±1.23%ID) ~ (99m) tc - pyboroxme(4.07±0.80%ID) > (99m) tc - 5uboroxme(3.24±0.67%ID) > (99m) tc - mpboroxme（2.53±0.65%ID）。快相心肌保留时间一般为（99m） tc - paboroxme(3.21±0.29 min) > (99m) tc - teboroxme(1.63±0.40 min) ~ (99m) tc - pyboroxme(1.57±0.29 min) ~ (99m) tc - isboroxme(1.55±0.32 min) > (99m) tc - mpboroxme(0.68±0.16 min) > (99m) tc - 5uboroxme（0.33±0.11 min）。（99m） tc - paboroxme（3.05±1.10%ID/g）和（99m） tc - isboroxme（3.75±0.68%ID/g）的2 min初始心脏摄取与（99m） tc - teboroxme（3.30±0.50%ID/g）非常接近。但（99m） tc - pboroxme的心肌保留时间明显长于（99m） tc - isboroxme和（99m） tc - teboroxme。尽管获取SPECT图像的最佳时间窗为0-5分钟，但在SD大鼠注射（99m） tc - paboroxme后的前30分钟内可以获得高质量的SPECT图像。这一说法得到了正常猪的SPECT/CT研究的支持。根据本研究结果，我们得出结论，硼酸盐组对（99m）Tc（III）复合物[(99m)TcCl(CDO)(CDOH)2B-R]的心脏摄取、心肌保留和肝脏清除动力学有显著影响。高初始心脏摄取与较长的心肌保留相结合，使得在前30分钟内使用标准和专用心脏SPECT相机使用（99m） tc - paboroxme对心脏进行成像成为可能。
This study sought to explore the impact of boronate groups on the heart uptake and myocardial retention of novel (99m)Tc(III) complexes [(99m)TcCl(CDO)(CDOH)2B-R] ((99m)Tc-ISboroxime: R = isoxazol-4-yl (IS); (99m)Tc-MPboroxime: R = N-methylpyridinium (MP); (99m)Tc-PAboroxime: R = pyrazol-3-yl (PA); (99m)Tc-PYboroxime: R = pyridin-3-yl (PY); and (99m)Tc-5Uboroxime: R = uracil-5-yl (5U)). All five new (99m)Tc(III) radiotracers were prepared in high yield and high radiochemical purity (RCP = 90-98%), and they remained stable in the kit mixture for >6 h. Biodistribution and imaging (planar and SPECT) studies were carried out using Sprague-Dawley (SD) rats. Planar image quantification was performed to compare their myocardial retention and liver clearance kinetics. It was found that their heart retention and liver clearance curves were best fitted to the biexponential decay function. The initial heart uptake at 0-1 min after injection followed the general ranking order of (99m)Tc-ISboroxime (4.98 ± 1.05%ID) ∼ (99m)Tc-Teboroxime (4.56 ± 0.91%ID) ∼ (99m)Tc-PAboroxime (4.03 ± 1.23%ID) ∼ (99m)Tc-PYboroxime (4.07 ± 0.80%ID) > (99m)Tc-5Uboroxime (3.24 ± 0.67%ID) > (99m)Tc-MPboroxime (2.53 ± 0.65%ID). The fast-phase myocardial retention time followed the general order of (99m)Tc-PAboroxime (3.21 ± 0.29 min) > (99m)Tc-Teboroxime (1.63 ± 0.40 min) ∼ (99m)Tc-PYboroxime (1.57 ± 0.29 min) ∼ (99m)Tc-ISboroxime (1.55 ± 0.32 min) > (99m)Tc-MPboroxime (0.68 ± 0.16 min) > (99m)Tc-5Uboroxime (0.33 ± 0.11 min). (99m)Tc-PAboroxime (3.05 ± 1.10%ID/g) and (99m)Tc-ISboroxime (3.75 ± 0.68%ID/g) had the 2 min initial heart uptake very close to that of (99m)Tc-Teboroxime (3.30 ± 0.50%ID/g). However, the myocardial retention time of (99m)Tc-PAboroxime was significantly longer than that of (99m)Tc-ISboroxime and (99m)Tc-Teboroxime. Even though the best time window is 0-5 min for SPECT image acquisition, high quality SPECT images could be obtained during the first 30 min postinjection of (99m)Tc-PAboroxime in SD rats. This statement was supported by the SPECT/CT studies in normal pigs. On the basis of results from this study, it was concluded that boronate groups had significant impact on the heart uptake, myocardial retention, and liver clearance kinetics of (99m)Tc(III) complexes [(99m)TcCl(CDO)(CDOH)2B-R]. The combination of high initial heart uptake with longer myocardial retention makes it possible to image the heart with (99m)Tc-PAboroxime during the first 30 min using both standard and specialized cardiac SPECT cameras.
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DOI：
10.1007/s00259-011-1877-y
发表时间：
2011-11-01
影响因子：
9.1
作者：
Fiechter, Michael;Ghadri, Jelena R.;Kaufmann, Philipp A.
通讯作者：
Kaufmann, Philipp A.
DOI：
--
发表时间：
1989-03
期刊：
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子：
--
作者：
D. W. Seldin;Lynne L. Johnson;D. K. Blood;Michael J. Muschel;Kevin F. Smith;R. M. Wall;Paul J. Cannon
通讯作者：
D. W. Seldin;Lynne L. Johnson;D. K. Blood;Michael J. Muschel;Kevin F. Smith;R. M. Wall;Paul J. Cannon
DOI：
--
发表时间：
1990
期刊：
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子：
--
作者：
J. Leppo;D. J. Meerdink
通讯作者：
J. Leppo;D. J. Meerdink
影响因子：
2.4
作者：
Yu, Ming;Guaraldi, Mary T.;Robinson, Simon P.
通讯作者：
Robinson, Simon P.
DOI：
10.1016/j.apradiso.2005.09.003
发表时间：
2006-03
期刊：
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine
影响因子：
--
作者：
Madhava B. Mallia;A. Mathur;S. Subramanian;S. Banerjee;K. Kothari;S. P. Koiry;H. D. Sarma;M. Venkatesh
通讯作者：
Madhava B. Mallia;A. Mathur;S. Subramanian;S. Banerjee;K. Kothari;S. P. Koiry;H. D. Sarma;M. Venkatesh