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- W2044068573 abstract "The aim of this study was to evaluate new ligands which can be applied for labeling biomolecules with scandium radionuclides. Two radionuclides of scandium, 47Sc and 44Sc, are perspective radioisotopes for radiotherapy and diagnostic imaging. 47Sc decays with a half-life of 3.35 days and a maximum β− energy of 600 keV and could be an alternative to carrier added 177Lu radionuclide for targeted radionuclide therapy. Another scandium radionuclide 44Sc (t1/2 = 3.92 h) is an ideal β+ emitter for PET diagnosis. It can be obtained as a daughter of the long-lived 44Ti (t1/2 = 60.4 y) from 44Ti/44Sc generator. For complexation of scandium radionuclides macrocyclic ligands having a cavity size similar to Sc3+ ionic radius were selected: 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-1,4,7 triacetic acid (NOTA), 1,4,7-triazacyclodecane-1,4,7 triacetic acid and 1,4,7-triazacycloundecane triacetic acid, and analogs of NOTA with 10, 11 and 12 atoms of the carbon in the ring. Our results have shown that from the studied macrocyclic ligands studied DOTA is most efficient for binding scandium radionuclides 44Sc and 47Sc to biomolecules. The determined stability constant of Sc–DOTA complex logK = 27.0 is comparable with stability constants for Y3+ and heaviest lanthanides but is higher than those for In3+ and Ga3+. Also 46Sc-DOTATATE conjugate exhibits high stability in-vitro studies. The 13C NMR studies have shown that Sc–DOTA like Lu–DOTA forms in solution complexes with eight-coordination geometry. The lipophilicity of Sc-DOTATATE is nearly identical to that of Lu-DOTATATE, which suggests similar receptor affinity of both radioconjugates." @default.
- W2044068573 created "2016-06-24" @default.
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- W2044068573 date "2011-02-01" @default.
- W2044068573 modified "2023-10-03" @default.
- W2044068573 title "Macrocyclic complexes of scandium radionuclides as precursors for diagnostic and therapeutic radiopharmaceuticals" @default.
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- W2044068573 doi "https://doi.org/10.1016/j.jinorgbio.2010.11.003" @default.
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