Influence of a TcN core on the biological and physicochemical behavior of Tc complexes of L,L-EC and L,L-ECD |
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Authors: | Kennedy O Mang'era Hubert P Vanbilloen Emmanuel Bellande Roberto Pasqualini Alfons M Verbruggen |
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Institution: | a Laboratory of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, K.U. Leuven, U.Z. Gasthuisberg, B-3000, Leuven, Belgium b Cis Bio International, 91192, Gif-Sur-Yvette, Cedex, France |
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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 pH 6, 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. |
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Keywords: | 99mTc-L L-ethylene dicysteine 99mTc-L L-ethylene dicysteine diethylester Nitrido 99mTc-nitrido 99mTc-oxo |
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