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99mTcN核心对L,L-EC和L,L-ECD的99mTc配合物生物及物理化学行为的影响

Influence of a 99mTcN core on the biological and physicochemical behavior of 99mTc complexes of L,L-EC and L,L-ECD.

作者信息

Mang'era K O, Vanbilloen H P, Bellande E, Pasqualini R, Verbruggen A M

机构信息

Laboratory of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, K. U. Leuven, U.Z. Gasthuisberg, Belgium.

出版信息

Nucl Med Biol. 1996 Nov;23(8):987-93. doi: 10.1016/s0969-8051(96)00150-3.

Abstract

99mTc-nitrido complexes of L,L-ethylene dicysteine (99mTcN-L,L-EC) and 99mTcN-L,L-ethylene dicysteine diethylester (99mTcN-L,L-ECD) were prepared and their characteristics compared to those of the respective 99mTc-oxo complexes. 99mTcN-L,L-EC and 99mTcO-L,L-EC migrate to similar extents during electrophoresis at pH 12, but, at pH6, 99mTcN-L,L-EC migrates further than 99mTcO-L,L-EC. Renal excretion of 99mTcN-L,L-EC is inferior to that of 99mTcO-L,L-EC, indicating that the TcN-glycine sequence has lower affinity for the renal tubular system. Both 99mTcO-L,L-ECD and 99mTcN-L,L-ECD are neutral, but 99mTcN-L,L-ECD is hydrophilic and shows minimal brain uptake in both mice and the baboon.

摘要

制备了L,L-乙二胺四乙酸(99mTcN-L,L-EC)和99mTcN-L,L-乙二胺四乙酸二乙酯(99mTcN-L,L-ECD)的99mTc-氮化物配合物,并将它们的特性与相应的99mTc-氧代配合物的特性进行了比较。99mTcN-L,L-EC和99mTcO-L,L-EC在pH 12的电泳过程中迁移程度相似,但在pH 6时,99mTcN-L,L-EC比99mTcO-L,L-EC迁移得更远。99mTcN-L,L-EC的肾脏排泄比99mTcO-L,L-EC差,这表明TcN-甘氨酸序列对肾小管系统的亲和力较低。99mTcO-L,L-ECD和99mTcN-L,L-ECD都是中性的,但99mTcN-L,L-ECD是亲水性的,在小鼠和狒狒中脑摄取都极低。

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