Sulfonyl-Containing Boronate Caps for Optimization of Biological Properties of 99mTc(III) Radiotracers [99mTcCl(CDO)(CDOH)2B-R] (CDOH2 = Cyclohexanedione Dioxime).
Sulfonyl-Containing Boronate Caps for Optimization of Biological Properties of 99mTc(III) Radiotracers [99mTcCl(CDO)(CDOH)2B-R] (CDOH2 = Cyclohexanedione Dioxime).
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DOI：
10.1021/acs.jmedchem.7b01412
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发表时间：
2018-01
影响因子：
7.3
通讯作者：
Zuoquan Zhao;Min Liu;W. Fang;Shuang Liu
中科院分区：
文献类型：
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作者：
Zuoquan Zhao;Min Liu;W. Fang;Shuang Liu
本研究采用不同的硼酸酯帽优化放射性示踪剂[99 mTcCl（CDO）（CDOH）2B-R]的生物分布特性（1，R = 3S; 2，R = 3SP; 3，R = 3MS; 4，R = 3DMS; 5，R = 3MSB; 6，R = 3MMS; 7，R = 3MSA; 8，R = 3DMSA; 9，R = 4S; 10，R = 4MS; 11，R = 4MSB）。在11种新的99 mTc放射性示踪剂中，2种显示出最有希望的最佳心脏显像剂的特性。它的初始心脏摄取接近于99 mTc-Teboroxime，但其心脏保留时间明显更长。它的心脏/肝脏、心脏/肺和心脏/肌肉比也优于99 mTc-Teboroxime。SD大鼠2的SPECT图像质量优于99 mTc-Teboroxime。高初始心脏摄取、长心脏保留和高心脏/背景比使2成为MPI的优秀SPECT放射性示踪剂。
In this study, different boronate caps were used to optimize biodistribution properties of radiotracers [99mTcCl(CDO)(CDOH)2B-R] (1, R = 3S; 2, R = 3SP; 3, R = 3MS; 4, R = 3DMS; 5, R = 3MSB; 6, R = 3MMS; 7, R = 3MSA; 8, R = 3DMSA; 9, R = 4S; 10, R = 4MS; 11, R = 4MSB). Among the 11 new 99mTc radiotracers, 2 shows the most promising characteristics of an optimal heart imaging agent. Its initial heart uptake is close to that of 99mTc-Teboroxime, but its heart retention time is significantly longer. Its heart/liver, heart/lung, and heart/muscle ratios are also better than those of 99mTc-Teboroxime. The SPECT image quality with 2 in SD rats is better than that with 99mTc-Teboroxime. The high initial heart uptake, long heart retention, and high heart/background ratios make 2 an excellent SPECT radiotracer for MPI.