PMID: 7767309Feb 1, 1995Paper

N,N'-ethylene-di-L-cysteine (EC) complexes of Ga(III) and In(III): molecular modeling, thermodynamic stability and in vivo studies

Nuclear Medicine and Biology
C J AndersonM J Welch

Abstract

There are several reports in the literature on the evaluation of chelates containing two nitrogens and two sulfurs (N2S2) as four coordinate ligands (in solution) for gallium and indium radiopharmaceuticals. No thermodynamic stability constants of these ligands were reported, and the stability of these complexes in vivo has been questioned. L,L-Ethylenedicysteine (EC) is a N2S2 ligand that also contains two carboxylic acid moieties for complexation of Ga(III) and In(III) in a hexacoordinate environment. The stability constants of Ga- and In-EC have been determined by potentiometric methods. The stability of In-EC was found to be greater than that of Ga-EC, with stability constants (log K's) of 33.0 and 31.5, respectively. A molecular mechanics evaluation of the Ga- and In-EC complexes support the thermodynamic results. 67Ga- and 111In-labeled complexes of EC were prepared and analyzed by thin layer chromatography and electrophoresis. Both complexes were evaluated in biodistribution studies in normal Sprague-Dawley rats. 111In-EC cleared rapidly through the hepatobiliary system, whereas 67Ga-EC remained in the liver at 1 h post-injection. Although 67Ga-EC was retained in the liver, suggesting instability of the complex in vivo. ...Continue Reading

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Citations

Feb 21, 2006·Annals of Nuclear Medicine·David J YangTomio Inoue
Sep 30, 2004·Cancer Biotherapy & Radiopharmaceuticals·David YangDonald Podoloff
Oct 20, 2009·European Journal of Pharmacology·Frederic ZollerWalter Mier
Aug 19, 2015·Nuclear Medicine and Molecular Imaging·Alireza MirzaeiDavood Beiki
Apr 13, 2012·Journal of Biomedicine & Biotechnology·Fan-Lin KongDavid J Yang
Jan 11, 2007·Nuclear Medicine and Biology·Ali AzhdariniaFiras Mourtada
Dec 17, 2008·Dalton Transactions : an International Journal of Inorganic Chemistry·Grazia PapiniCarlo Santini
Apr 3, 2008·Contrast Media & Molecular Imaging·Melpomeni FaniHelmut R Maecke
Apr 30, 1999·Journal of Psychopharmacology·G DarcourtJ Lavoisy
Nov 1, 2018·Chemical Reviews·Thomas I Kostelnik, Chris Orvig

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