Rattat Dirk, Cleynhens Bernard, Bormans Guy, Terwinghe Christelle, Verbruggen Alfons
Laboratory for Radiopharmaceutical Chemistry and Nuclear Medicine, Catholic University of Leuven, Herestraat 49, 3000 Leuven, Belgium.
Bioorg Med Chem Lett. 2005 Oct 1;15(19):4192-5. doi: 10.1016/j.bmcl.2005.06.086.
N-(2-Mercapto-propyl)-1,2-phenylenediamine (MPPDA) and N-beta-aminoethylglycine (AEG) were labelled with 99mTc(CO)3(+) to form the neutral complexes [99mTc(CO)3(MPPDA)] and [99mTc(CO)3(AEG)]. Both complexes were formed in excellent yields and their identity was confirmed by LC-MS. In mice, none of the new tracer agents showed brain uptake. [(99m)Tc(CO)3(MPPDA)] was trapped mainly in the liver and excreted via the hepatobiliary system, whereas [99mTc(CO)3(AEG)] was excreted rapidly via the kidneys to the urine.
N-(2-巯基丙基)-1,2-苯二胺（MPPDA）和N-β-氨乙基甘氨酸（AEG）用99mTc(CO)3(+)进行标记，形成中性络合物[99mTc(CO)3(MPPDA)]和[99mTc(CO)3(AEG)]。两种络合物的产率都很高，其结构通过液相色谱-质谱联用（LC-MS）得以确认。在小鼠体内，这些新型示踪剂均未显示出脑摄取。[(99m)Tc(CO)3(MPPDA)]主要蓄积在肝脏，并通过肝胆系统排泄，而[99mTc(CO)3(AEG)]则通过肾脏迅速排泄到尿液中。
