Novel (99m)Tc(III)-azide complexes [(99m)Tc(N(3))(CDO)(CDOH)(2)B-R] (CDOH(2)=cyclohexanedione dioxime) as potential radiotracers for heart imaging.
Novel (99m)Tc(III)-azide complexes [(99m)Tc(N(3))(CDO)(CDOH)(2)B-R] (CDOH(2)=cyclohexanedione dioxime) as potential radiotracers for heart imaging.
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新型 99mTc(III)-叠氮化物配合物 [99mTc(N3)(CDO)(CDOH)2B-R]（CDOH2 = 环己二酮二肟）作为心脏成像的潜在放射性示踪剂
DOI：
10.1016/j.nucmedbio.2016.05.001
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发表时间：
2016-11
影响因子：
3.1
通讯作者：
Liu S
中科院分区：
文献类型：
--
作者：
Liu M;Zheng Y;Avcibasi U;Liu S
在本研究中，评价了新型99 mTc（III）-叠氮化物络合物[99 mTc（N3）（CDO）（CDOH）2B-R]（99 mTc-IS硼肟-N3：R = IS; 99 mTc-MP硼肟-N3：R = MP; 99 mTc-PA硼肟-N3：R = PA; 99 mTc-PY硼肟-N3：R = PY;和99 mTc-U硼肟-N3：R = 5 U）作为心脏显像剂。用NaN 3与[99 mTcCl（CDO）（CDOH）2B-R]进行配体交换，合成了配合物[99 mTc（N3）（CDO）（CDOH）2B-R]（R = IS，MP，PA，PY和5 U）。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初始心脏摄取和心肌保留。以高RCP（93-98%）制备99 mTc-ISboroxime-N3、99 mTc-PYboroxime-N3和99 mTc-Uboroxime-N3，而99 mTc-MPboroxime-N3和99 mTc-PA boroxime-N3的RCP为80- 85%。~（99）mTc-ISboroxime-N_3、~（99）mTc-PYboroxime-N_3和~（99）mTc-Uboroxime-N_3的心肌保留曲线均符合双指数衰减函数。99 mTc-ISboroxime-N3、99 mTc-PYboroxime-N3和99 mTc-Uboroxime-N3的快组分半衰期分别为1.6 ± 0.4 min、0.7 ± 0.1 min和0.9 ± 0.4 min。生物分布研究的2分钟心脏摄取遵循99 mTc-ISboroxime-N3（3.60 ± 0.68%ID/g）> 99 mTc-PYboroxime-N3（2.35 ± 0.37%ID/g）> 99 mTc-Uboroxime-N3（1.29 ± 0.06%ID/g）的排序。99 mTc-ISboroxime-N3在SD大鼠心脏中的2 min摄取最高。获得了高质量的SPECT图像，左心室壁和右心室壁被清楚地描绘。99 mTc-ISboroxime-N3的最佳图像采集窗口为0-5 min。叠氮共配体和硼酸酯帽对复合物[99 mTc（N3）（CDO）（CDOH）2B-R]的心脏摄取和心肌保留具有显著影响。在SD大鼠中评估的放射性示踪剂中，99 mTc->ISboroxime-N3具有最高的初始心脏摄取，心脏保留与99 mTc-替硼肟相当。99 mTc-ISboroxime-N3是SPECT MPI中99 mTc-Teboroxime的一种有前途的替代品。
In this study, novel 99mTc(III)-azide complexes [99mTc(N3)(CDO)(CDOH)2B-R] (99mTc-ISboroxime-N3: R = IS; 99mTc-MPboroxime-N3: R = MP; 99mTc-PAboroxime-N3: R = PA; 99mTc-PYboroxime-N3: R = PY; and 99mTc-Uboroxime-N3: R = 5U) were evaluated as heart imaging agents. Complexes [99mTc(N3)(CDO)(CDOH)2B-R] (R = IS, MP, PA, PY and 5U) were prepared by ligand exchange between NaN3 and [99mTcCl(CDO)(CDOH)2B-R]. Biodistribution and imaging studies were carried out in Sprague–Dawley rats. Image quantification was performed to compare their initial heart uptake and myocardial retention. 99mTc-ISboroxime-N3, 99mTc-PYboroxime-N3 and 99mTc-Uboroxime-N3 were prepared with high RCP (93–98%) while the RCP of 99mTc-MPboroxime-N3 and 99mTc-PAboroxime-N3 was 80–85%. The myocardial retention curves of 99mTc-ISboroxime-N3, 99mTc-PYboroxime-N3 and 99mTc-Uboroxime-N3 were best fitted to the bi-exponential decay function. The half-time of the fast component was 1.6 ± 0.4 min for 99mTc-ISboroxime-N3, 0.7 ± 0.1 min for 99mTc-PYboroxime-N3 and 0.9 ± 0.4 min for 99mTc-Uboroxime-N3. The 2-min heart uptake from biodistribution studies followed the ranking order of 99mTc-ISboroxime-N3 (3.60 ± 0.68%ID/g) > 99mTc-PYboroxime-N3 (2.35 ± 0.37%ID/g) ≫ 99mTc-Uboroxime-N3 (1.29 ± 0.06%ID/g). 99mTc-ISboroxime-N3 had the highest 2-min heart uptake among 99mTc radiotracers revaluated in SD rats. High quality SPECT images were obtained with the right and left ventricular walls being clearly delineated. The best image acquisition window was 0–5 min for 99mTc-ISboroxime-N3. Both azide coligand and boronate caps had significant impact on the heart uptake and myocardial retention of complexes [99mTc(N3)(CDO)(CDOH)2B-R]. Among the radiotracers evaluated in SD rats, 99mTc->ISboroxime-N3 has the highest initial heart uptake with the heart retention comparable to that of 99mTc-Teboroxime. 99mTc-ISboroxime-N3 is a promising alternative to 99mTc-Teboroxime for SPECT MPI.
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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：
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影响因子：
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作者：
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DOI：
10.1016/0735-1097(92)90029-m
发表时间：
1992-09-01
影响因子：
24
作者：
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通讯作者：
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影响因子：
14
作者：
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通讯作者：
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影响因子：
2.4
作者：
Duvall, W. Lane;Croft, Lori B.;Henzlova, Milena J.
通讯作者：
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