期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 105, 期 1, 页码 31-38出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2010.09.012
关键词
Hydroxypyridinones; Tripodal chelators; Gallium radioisotope; Biodistribution; Gamma scintigraphy; Gallium 67
资金
- Portuguese Fundacao para a Clencia e Tecnologia (FCT) [PCDT/QUI/56985/04, PTDC/QUI/70063/2006, SFRH/BD/46370/2008, SFRH/BPD/29874/2006]
- FEDER
- Programa Nacional de Reequipamento Cientifico of the FCT Portugal [REDE/1517/RMN/2005]
The gallium(III) complex of a new tripodal 3 hydroxy 4-pyridinone (3 4-HP) chelator has been studied in terms of its physico-chemical and in vivo properties aimed at potential application as probe for nuclear imaging In particular based on spectrophotometric titrations the hexa-coordinated (1 1) gallium complex appeared as the major species in a wide physiological acid neutral pH range and its high stability (pGa = 27 5) should avoid drug-induced toxicity resulting from Ga(III) accumulation in tissues due to processes of transmetallation with endogenenous ligands or demetallation A multinuclear (H-1 and Ga-71) NMR study gave some insights into the structure and dynamics of the gallium(III) chelate in solution which are consistent with the tris-(3 4-HP) coordination and an eventual pseudo octahedral geometry Biodistribution and scintigraphic studies of the Ga-67(III) labelled chelate performed in Wistar rats confirmed the in vivo stability of the radiolabelled complex its non interaction with blood proteins and its quick renal clearance These results indicate good perspectives for potential application of extrafunctionalized analogues in radiodiagnostic techniques (C) 2010 Elsevier Inc All rights reserved
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