Effect of co-ligands on chemical and biological properties of (99m)Tc(III) complexes [(99m)Tc(L)(CDO)(CDOH)2BMe] (L=Cl, F, SCN and N3; CDOH2=cyclohexanedione dioxime).
Effect of co-ligands on chemical and biological properties of (99m)Tc(III) complexes [(99m)Tc(L)(CDO)(CDOH)2BMe] (L=Cl, F, SCN and N3; CDOH2=cyclohexanedione dioxime).
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DOI：
10.1016/j.nucmedbio.2014.07.009
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发表时间：
2014-11
影响因子：
3.1
通讯作者：
Liu S
中科院分区：
文献类型：
--
作者：
Zheng Y;Ji S;Tomaselli E;Ernest C;Freiji T;Liu S
99 mTc-Teboroxime（[99 mTcCl（CDO）（CDOH）2BMe]）是BATO（boronic acid adducts of technetium dioximes）类99 mTc（III）配合物的成员。本研究试图探索共配体对[99 mTc（L）（CDO）（CDOH）2BMe]（99 mTc-替硼肟：L = Cl; 99 mTc-替硼肟（F）：L = F; 99 mTc-替硼肟（SCN）：L = SCN;和99 mTc-替硼肟（N3）：L = N3）的溶液稳定性、心脏摄取和心肌保留的影响。用~（99）mTc-替硼肟分别与NaF、NaSCN和NaN_3反应，制备了~（99）mTc-替硼肟（L）（L = F、SCN和N_3）。在Sprague-Dawley大鼠中进行了生物分布和成像研究。进行图像定量以比较它们的心脏保留和肝脏清除动力学。本文报道了99 mTc-Teboroxime（L）（L = F、SCN和N_3）的高产率、高放化纯度的合成。所有新的放射性示踪剂在试剂盒基质中稳定>6小时。在其HPLC色谱图中，99 mTc-Teboroxime在~15.5 min处显示一个峰，其比99 mTc-Teboroxime（F）（~16.4 min）短。99 mTc-Teboroxime（SCN）在16.5和18.3min出现两个峰，99 mTc-Teboroxime（N3）在18.4min出现一个单峰，它们的心脏滞留和肝脏清除曲线均符合双指数衰减函数。99 mTc-Teboroxime（F）、99 mTc-Teboroxime（SCN）和99 mTc-Teboroxime（N3）的快/慢组分半衰期分别为1.6 ± 0.4/60.7±8.9、0.8±0.2/101.7±20.7、1.2±0.3/84.8±16.6和2.9±0.9/51.6±5.0 min。2min心肌摄取99mTc-Teboroxime（3.00±0.37%ID/g）> 99mTc-Teboroxime（N3）（2.66± 0.01%ID/g）> 99mTc-Sestamibi（2.55± 0.46%ID/g）> 99mTcN-MPO（2.38± 0.15%ID/g）。99 mTc-Teboroxime的首过萃取效果最好。99 mTc-Teboroximine（N3）的最佳图像采集窗口为0 - 5 min，99 mTc-Teboroximine（N3）为0 - 15 min。共配体对配合物[99 mTc（L）（CDO）（CDOH）2BMe]（L = Cl，F，SCN和N3）的心脏摄取和心肌滞留有显著影响。未来的研究应致力于最大限度地减少肝脏摄取和血管中的放射性积聚，同时保持其高心脏摄取。
99mTc-Teboroxime ([99mTcCl(CDO)(CDOH)2BMe]) is a member of the BATO (boronic acid adducts of technetium dioximes) class of 99mTc(III) complexes. This study sought to explore the impact of co-ligands on solution stability, heart uptake and myocardial retention of [99mTc(L)(CDO)(CDOH)2BMe] (99mTc-Teboroxime: L = Cl; 99mTc-Teboroxime(F): L = F; 99mTc-Teboroxime(SCN): L = SCN; and 99mTc-Teboroxime(N3): L = N3). Radiotracers 99mTc-Teboroxime(L) (L = F, SCN and N3) were prepared by reacting 99mTc-Teboroxime with NaF, NaSCN and NaN3, respectively. Biodistribution and imaging studies were carried out in Sprague-Dawley rats. Image quantification was performed to compare their heart retention and liver clearance kinetics. Complexes 99mTc-Teboroxime(L) (L = F, SCN and N3) were prepared in high yield with high radiochemical purity. All new radiotracers were stable for >6 h in the kit matrix. In its HPLC chromatogram, 99mTc-Teboroxime showed one peak at ~15.5 min, which was shorter than that of 99mTc-Teboroxime(F) (~16.4 min). There were two peaks for 99mTc-Teboroxime(SCN) at 16.5 and 18.3 min. 99mTc-Teboroxime(N3) appeared as a single peak at 18.4 min. Their heart retention and liver clearance curves were best fitted to the bi-exponential decay function. The half-times of fast/slow components were 1.6 ± 0.4/60.7±8.9 min for 99mTc-Teboroxime, 0.8±0.2/101.7±20.7 min for 99mTc-Teboroxime(F), 1.2±0.3/84.8±16.6 min for 99mTc-Teboroxime(SCN), and 2.9±0.9/51.6±5.0 min for 99mTc-Teboroxime(N3). The 2-min heart uptake followed the order of 99mTc-Teboroxime (3.00±0.37%ID/g) > 99mTc-Teboroxime(N3) (2.66±0.01 %ID/g) ≈ 99mTc-Sestamibi (2.55±0.46 %ID/g) > 99mTcN-MPO (2.38±0.15 %ID/g). 99mTc-Teboroxime remains the best in first-pass extraction. The best image acquisition window is 0 – 5 min for 99mTc-Teboroximine and 0 – 15 min for 99mTc-Teboroximine(N3). Co-ligands had significant impact on the heart uptake and myocardial retention of complexes [99mTc(L)(CDO)(CDOH)2BMe] (L = Cl, F, SCN and N3). Future studies should be directed towards minimizing the liver uptake and radioactivity accumulation in the blood vessels while maintaining their high heart uptake.
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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.
影响因子：
4.7
作者：
Kim, Dong-Yeon;Kim, Hee-Jung;Min, Jung-Joon
通讯作者：
Min, Jung-Joon
影响因子：
9.3
作者：
Higuchi, Takahiro;Fukushima, Kenji;Bengel, Frank M.
通讯作者：
Bengel, Frank M.
影响因子：
2.4
作者：
Duvall, W. Lane;Croft, Lori B.;Henzlova, Milena J.
通讯作者：
Henzlova, Milena J.
影响因子：
2.4
作者：
Kim, Young-Seung;Shi, Jiyun;Liu, Shuang
通讯作者：
Liu, Shuang