Novel hexadentate and pentadentate chelators for ⁶⁴Cu-based targeted PET imaging.
Novel hexadentate and pentadentate chelators for ⁶⁴Cu-based targeted PET imaging.
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用于基于 Cu 的靶向 PET 成像的新型六齿和五齿螯合剂。
DOI：
10.1016/j.bmc.2014.02.041
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发表时间：
2014
影响因子：
3.5
通讯作者：
Chong,Hyun-Soon
中科院分区：
文献类型：
--
作者：
Sin,Inseok;Kang,ChiSoo;Bandara,Nilantha;Sun,Xiang;Zhong,Yongliang;Rogers,BuckE;Chong,Hyun-Soon
设计并合成了一系列新的六齿和五齿螯合剂作为64 Cu的螯合剂。新的五齿和六齿螯合剂含有不同类型的供体基团，并有望与Cu（II）形成中性配合物。评价了新螯合剂与64 Cu的络合动力学和稳定性。新的螯合剂立即结合到64 Cu具有高标记效率和最大的比活性。人血清中所有64 Cu放射性标记的复合物在2天内保持完整。64 Cu放射性标记的络合物进一步挑战EDTA在100倍摩尔过量。在评价的64 Cu-放射性标记络合物中，新螯合剂E的64 Cu-络合物耐受性良好，64 Cu向EDTA的转移最小。新螯合剂E的64 Cu-放射性标记络合物进一步评价用于小鼠的生物分布研究，并显示快速的血液清除和低器官摄取。64 Cu-螯合剂E产生了与已知的六齿NOTA螯合剂的64 Cu络合物相当的有利的体外和体内络合物稳定性概况。体外和体内数据突出了新螯合剂E用于靶向PET成像应用的强大潜力。
A series of new hexadentate and pentadentate chelators were designed and synthesized as chelators of64Cu. The new pentadentate and hexadentate chelators contain different types of donor groups and are expected to form neutral complexes with Cu(II). The new chelators were evaluated for complex kinetics and stability with64Cu. The new chelators instantly bound to64Cu with high labeling efficiency and maximum specific activity. All64Cu-radiolabeled complexes in human serum remained intact for 2 days. The64Cu-radiolabeled complexes were further challenged by EDTA in a 100-fold molar excess. Among the64Cu-radiolabeled complexes evaluated,64Cu-complex of the new chelatorEwas well tolerated with a minimal transfer of64Cu to EDTA.64Cu-radiolabeled complex of the new chelatorEwas further evaluated for biodistribution studies using mice and displayed rapid blood clearance and low organ uptake.64Cu-chelatorEproduced a favorable in vitro and in vivo complex stability profiles comparable to64Cu complex of the known hexadentate NOTA chelator. The in vitro and in vivo data highlight strong potential of the new chelatorEfor targeted PET imaging application.
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影响因子：
7.3
作者：
Boswell, CA;Sun, XK;Anderson, CJ
通讯作者：
Anderson, CJ
影响因子：
3.1
作者：
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作者：
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通讯作者：
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