Radiolabeling of PAMAM dendrimers conjugated to a pyridine-N-oxide DOTA analog with ¹¹¹In: Optimization of reaction conditions and biodistribution
Jazyk angličtina Země Velká Británie, Anglie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
21757312
DOI
10.1016/j.jpba.2011.06.009
PII: S0731-7085(11)00329-3
Knihovny.cz E-zdroje
- MeSH
- dendrimery chemie farmakokinetika MeSH
- heterocyklické sloučeniny monocyklické chemie farmakokinetika MeSH
- izotopové značení metody MeSH
- krysa rodu Rattus MeSH
- nosiče léků chemie farmakokinetika MeSH
- potkani Wistar MeSH
- pyridiny chemie farmakokinetika MeSH
- radiofarmaka chemie farmakokinetika MeSH
- radioizotopy india chemie farmakokinetika MeSH
- tkáňová distribuce MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid MeSH Prohlížeč
- dendrimery MeSH
- heterocyklické sloučeniny monocyklické MeSH
- nosiče léků MeSH
- PAMAM Starburst MeSH Prohlížeč
- pyridine N-oxide MeSH Prohlížeč
- pyridiny MeSH
- radiofarmaka MeSH
- radioizotopy india MeSH
Polyamidoamine dendrimers (PAMAMs) of generations 1 (G1) and 4 (G4) were conjugated with a bifunctional pyridine-N-oxide DOTA analog, 10-[(4-carboxy-1-oxidopyridin-2-yl)methyl]-1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid (H(4)do3a-py(NO-C)), through the pyridine-4-carboxylic acid group, and the conjugates were radiolabeled with indium-111. Reaction conditions for the radiolabelling were optimized. Both radiolabeled conjugates, G1-[(111)In(do3a-py(NO-C))] and G4-[(111)In(do3a-py(NO-C))], were kinetically stable for at least 48h after preparation; in the presence of competitive ligands, the radiochemical purity of the conjugates slightly decreased (4-7%) over the same time period. The preclinical pharmacokinetics of both agents were evaluated. Biodistribution and elimination in rats were more favorable for the G1-[(111)In(do3a-py(NO-C))] conjugate than G4-[(111)In(do3a-py(NO-C))] conjugate. However, the G1-[(111)In(do3a-py(NO-C))] conjugate was rapidly eliminated from the body, mainly through urine, while, significant and long-term radioactivity uptake in the liver and kidney was observed for the G4-[(111)In(do3a-py(NO-C))] conjugate.
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