In Vitro and In Vivo Behaviour of In Complexes of TTHA, TTHA-Bis(Butylamide) and TTHA-Bis(Glucamide): Stability, Biodistribution and Excretion Studied by Gamma Imaging |
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| Authors: | Prata M I Ribeiro M J Santos A C Peters J A Nepveu F Geraldes C F de Lima J J |
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| Affiliation: | 1. Serviço de Biofísica e Biomatemática, Fac. Medicina, Univ. de Coimbra, Portugal.;2. Departamento de Bioquímica e Centro de Neurociências, Univ. de Coimbra, Portugal.;3. Lab. of Organic Chemistry and Catalysis, Delft University of Technology, Delft, The Netherlands.;4. Laboratoire de Synthèse, Physico-Chimie et Radiobiologie, Université Paul Sabatier, Toulouse, France, |
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| Abstract: | Aiming at radiopharmaceutical application, (111)In(3+) complexes of the polyaminocarboxylates TTHA, TTHA-bis(butylamide) and TTHA-bis(glucamide) were investigated. The in vitro stability of (111)In(TTHA)(3-) and (111)In(TTHA-bis(butylamide)(-) was evaluated by measuring the exchange of (111)In(3+) from the complexes to transferrin and the results were compared with those for (111)In(DTPA)(2-). We also performed biodistribution studies of the three (111)In(3+) complexes by gamma-imaging in Wistar rats and by measuring the radioactivity in their organs. TTHA and its derivatives seem to have similar in vivo biodistribution with prevailing renal excretion. |
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