Metal-Based Drugs 
Volume 5 (1998), Issue 5, Pages 259-264
doi:10.1155/MBD.1998.259

In Vitro and In Vivo Behaviour of I111n Complexes of TTHA, TTHA-Bis(Butylamide) and TTHA-Bis(Glucamide): Stability, Biodistribution and Excretion Studied by Gamma Imaging

M. I. M. Prata,1,2 M. J. Ribeiro,1 A. C. Santos,1 J. A. Peters,3 F. Nepveu,4 C. F. G. C. Geraldes,2 and J. J. P. de Lima1

 1Serviço de Biofísica e Biomatemática, Fac. Medicina, Univ. de Coimbra, Portugal
2Departamento de Bioquímica e Centro de Neurociências, Univ. de Coimbra, Portugal
3Lab. of Organic Chemistry and Catalysis, Delft University of Technology, Delft, The Netherlands
4Laboratoire de Synthèse, Physico-Chimie et Radiobiologie, Université Paul Sabatier, Toulouse, France
Received 30 April 1998; Accepted 11 May 1998

Abstract

Aiming at radiopharmaceutical application, I111n3+ complexes of the polyaminocarboxylates TTHA, TTHA-bis(butylamide) and TTHA-bis(glucamide) were investigated. The in vitro stability of I111n(TTHA)3− and I111n(TTHA-bis(butylamide)- was evaluated by measuring the exchange of I111n3+ from the complexes to transferrin and the results were compared with those for I111n(DTPA)2−. We also performed biodistribution studies of the three I111n3+ 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.