摘要:
3,3,10,10-四乙基-1,2-二巯基-5,8-二杂氮环癸烷(BAT-TE)和3,3,6,6,10,10-,六甲基-1,2-二巯基-5,8-二杂氮环癸烷(BAT-HM)可与Ga~(3+),Tl~(3+)螯合。螯合反应快速、简单,并且产率很高。BAT类整合物在小白鼠体内主要浓集在心脏。静脉注射2—3min,心脏的清除率下降较慢,而且心/血比较高。由此看来,M-BAT-TE(M=Ga~(3+),In~(3+)),M-BAT-HM(M=Ga~(3+),In~(3+),Tl~93+))是一类新的、值得研究的心肌显像剂,尤其是Tl-BAT-HM可能是一种有前途的心肌显像剂。
Abstract:
The use of 3, 3, 10, 10-tetraethyl-1, 2-dithio-5, 8-diazacyclodecane (BAT-TE) and 3, 3, 6, 6, 10, 10-hexamethyl-1, 2-dithio-5, 8-diazacyclodecane(BAT-HM) as new ligands for the preparation of M-BAT-TE(M=Ga~(3+), In~(3+)) and M-BAT-HM(M=Ga~(3+), In~(3+), Tl~(3+)) were investigated. The chelating reactions with high labelling yield are fairly simple and rapid. The biodistribution of BAT derivative chelates in mice exhibited considerable myocardial uptake and good selectivity. Slow washout in heart and high heart-to-blood ratios were observed during the period from 2min to 30min after intravenous injection. Based on these experimental results, M-BAT-TE(M=Ga~(3+), In~(3+)) and M-BAT-HM(M=Ga~(3+), In~(3+), Tl~(3+)) are considered as potential myocardial imaging agents, and particularly Tl-BAT-HM is likely a promising imaging agent.
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