一种中性亲脂性Tc-99m N3S2螯合物的合成、表征及生物分布研究。

Synthesis, characterization and biodistribution studies of a neutral-lipophilic Tc-99m N3S2 chelate.

作者信息

Singh P R, Corlija M, Troutner D E, Ketring A R, Volkert W A

机构信息

Department of Radiology, Harry S. Truman Memorial Veterans Hospital, Columbia, MO 65211.

出版信息

Int J Rad Appl Instrum B. 1992 Oct;19(7):791-5. doi: 10.1016/0883-2897(92)90141-k.

DOI:10.1016/0883-2897(92)90141-k

PMID:1399701

Abstract

Diaminedithiols (DADT) are known to form neutral-lipophilic complexes with 99mTc in aqueous solutions, where they are readily formed in high yields and demonstrate excellent stability. A new triaminedithiol (TADT) ligand was synthesized, characterized and shown to form a neutral-lipophilic 99mTc-chelate. The biodistribution of this 99mTc chelate in rats showed that its uptake in brain or heart following i.v. injection of the 99mTc chelate was low, but activity taken up was retained over a long period of time. The in vivo and in vitro properties of this chelate indicate the possibility that chemical modification of this TADT ligand may produce ligand systems that form 99mTc chelates with suitable diagnostic properties.

摘要

已知二氨基二硫醇（DADT）在水溶液中能与99mTc形成中性亲脂性络合物，它们易于高产率形成且具有出色的稳定性。一种新的三氨基二硫醇（TADT）配体被合成、表征，并显示能形成中性亲脂性的99mTc螯合物。这种99mTc螯合物在大鼠体内的生物分布表明，静脉注射该99mTc螯合物后，其在脑或心脏中的摄取量较低，但摄取的活性能长时间保留。这种螯合物的体内和体外性质表明，对这种TADT配体进行化学修饰可能产生能形成具有合适诊断特性的99mTc螯合物的配体系统。