Influence of a 99mTcN core on the biological and physicochemical behavior of 99mTc complexes of L,L-EC and L,L-ECD.
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.
Mang'era
K O
KO
Laboratory of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, K. U. Leuven, U.Z. Gasthuisberg, Belgium.
Vanbilloen
H P
HP
Bellande
E
E
Pasqualini
R
R
Verbruggen
A M
AM
D000818:Animals; D001921:Brain / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003545:Cysteine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D004586:Electrophoresis; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D015609:Organotechnetium Compounds / Q000737:chemistry* / Q000493:pharmacokinetics*; D010215:Papio; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C073806:technetium Tc 99m-ethylenedicysteine; C059659:technetium Tc 99m bicisate; D003545:Cysteine