Radiochemical and biological behaviour of 153Sm and 166Ho complexes anchored by a novel bis(methylphosphonate) tetraazamacrocycle
-
M. Paula Campello
The novel bis(methylphosphonate) 2,2′-[4,10-bis(phosphonomethyl)-1,4,7,10-tetraazacyclododecane-1,7-diyl] diacetic acid, trans-H6DO2A2P, has been synthesized and characterized by multinuclear NMR spectroscopy (1H, 13C and 31P). 153Sm and 166Ho complexes with trans-H6DO2A2P have been prepared in high yield using a 1:2 metal to ligand molar ratio at 70 °C, pH 8−9. These complexes are hydrophilic, negatively charged and stable in vitro under physiological solutions, up to 48 h. They present a low plasmatic protein binding and some in vitro hydroxyapatite adsorption, mainly for 166Ho-trans-DO2A2P. Both complexes are stable in vivo, have a fast tissue clearance from most organs and a rapid total excretion from whole animal body. Moderate bone uptake was also observed but the accumulated radioactivity rapidly decreases with time.
© Oldenbourg Wissenschaftsverlag
Artikel in diesem Heft
- Preface
- Radiolanthanides in endoradiotherapy: an overview
- Nuclear data for production of 88Y, 140Nd, 153Sm and 169Yb via novel routes
- A 140Nd/140Pr radionuclide generator based on physico-chemical transitions in 140Pr complexes after electron capture decay of 140Nd-DOTA
- Radiochemical and biological behaviour of 153Sm and 166Ho complexes anchored by a novel bis(methylphosphonate) tetraazamacrocycle
- Biological evaluation of 153Sm and 166Ho complexes with tetraazamacrocycles containing methylcarboxylate and/or methylphosphonate pendant arms
- Radiolabelled 153Sm-chelates of glycoconjugates: multivalence and topology effects on the targeting of the asialoglycoprotein receptor
- 177Lu-labeled-VG76e monoclonal antibody in tumor angiogenesis: A comparative study using DOTA and DTPA chelating systems
- Preclinical evaluation of somatostatin analogs bearing two macrocyclic chelators for high specific activity labeling with radiometals
Artikel in diesem Heft
- Preface
- Radiolanthanides in endoradiotherapy: an overview
- Nuclear data for production of 88Y, 140Nd, 153Sm and 169Yb via novel routes
- A 140Nd/140Pr radionuclide generator based on physico-chemical transitions in 140Pr complexes after electron capture decay of 140Nd-DOTA
- Radiochemical and biological behaviour of 153Sm and 166Ho complexes anchored by a novel bis(methylphosphonate) tetraazamacrocycle
- Biological evaluation of 153Sm and 166Ho complexes with tetraazamacrocycles containing methylcarboxylate and/or methylphosphonate pendant arms
- Radiolabelled 153Sm-chelates of glycoconjugates: multivalence and topology effects on the targeting of the asialoglycoprotein receptor
- 177Lu-labeled-VG76e monoclonal antibody in tumor angiogenesis: A comparative study using DOTA and DTPA chelating systems
- Preclinical evaluation of somatostatin analogs bearing two macrocyclic chelators for high specific activity labeling with radiometals
