Complexation and biodistribution study of 111In and 90Y complexes of bifunctional phosphinic acid analogs of H4dota
| Autor: | Miloš Petřík, Alice Laznickova, Michaela Försterová, Frantisek Melichar, Petr Hermann, Ivan Lukeš, Milan Laznicek |
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| Rok vydání: | 2009 |
| Předmět: |
Biodistribution
Radiation Chemistry Stereochemistry Similar distribution Indium Radioisotopes Phosphinate Phosphinic Acids In vitro Rats Heterocyclic Compounds 1-Ring chemistry.chemical_compound Pharmacokinetics Organometallic Compounds Animals DOTA Tissue Distribution Yttrium Radioisotopes Radiopharmaceuticals Bifunctional |
| Zdroj: | Applied Radiation and Isotopes. 67:21-29 |
| ISSN: | 0969-8043 |
| Popis: | In this study, the complexation rates of two new phosphinate H 4 dota (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) analogs, H 5 do3ap PrA and H 4 do3ap ABn , and H 4 dota itself were compared under identical conditions (H 5 do3ap PrA =10-{[(2-carboxyethyl)hydroxyphosphoryl]methyl}-1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid; H 4 do3ap ABn =10-{[(4-aminophenyl)hydroxyphosphoryl]methyl}-1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid). The biodistribution of their 111 In and 90 Y complexes in healthy rats was also studied. Unlike the observation obtained under “chemical” conditions where differences between the ligands were observed no such differences in complexation rates were found under radiochemical conditions. The ligands bind the radiometals similarly to H 4 dota. So, “chemical” formation kinetic data should be transferred into radiochemical conditions only with high care and “radiochemical” complexation experiments should be run as part of standard in vitro studies with new ligands considered as potential radiopharmaceuticals. Pharmacokinetic studies in rats showed similar distribution characteristics for both phosphinate H 4 dota analogs radiolabelled with 111 In and 90 Y when compared with that of the 111 In–H 4 dota complex. No specific uptake in any organ and tissue of rats was determined. The phosphinate complexes are not accumulated in calcified tissues. |
| Databáze: | OpenAIRE |
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