Abstract
In this study, we present the synthesis and characterization of the octadentate bispidine ligand, H2bispox2 and its complexes with medicinally useful radiometal nuclides (111In3+ and 177Lu3+), including their X-ray diffraction single crystal structures with the stable isotopes. 111InCl3 radiolabels the ligand quantitatively at ambient conditions ([L] = 10-5 M, room temperature, pH 7 and 15 min) and the in vitro human serum stability assays demonstrated high stability of the [111In(bispox2)]+ complex over 5 days. Moreover, the β - emitter 177Lu radiolabels the ligand at 37 °C in 30 min (pH 8). These initial investigations reveal the potential of the octadentate bispidine ligand H2bispox2 as a useful chelator for 111In and 177Lu-based radiopharmaceuticals.
MeSH terms
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Animals
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Bridged Bicyclo Compounds, Heterocyclic / blood
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Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis
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Bridged Bicyclo Compounds, Heterocyclic / chemistry*
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Chelating Agents / chemical synthesis
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Chelating Agents / chemistry
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Coordination Complexes / blood
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Coordination Complexes / chemical synthesis
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Coordination Complexes / chemistry*
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Drug Stability
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Humans
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Indium Radioisotopes
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Ligands
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Lutetium
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Mice
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Molecular Structure
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Oxyquinoline / analogs & derivatives*
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Oxyquinoline / blood
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Oxyquinoline / chemical synthesis
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Oxyquinoline / chemistry
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Radioisotopes
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Radiopharmaceuticals / blood
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Radiopharmaceuticals / chemical synthesis
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Radiopharmaceuticals / chemistry*
Substances
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Bridged Bicyclo Compounds, Heterocyclic
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Chelating Agents
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Coordination Complexes
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Indium Radioisotopes
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Ligands
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Radioisotopes
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Radiopharmaceuticals
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bispidine
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Lutetium
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Oxyquinoline
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Lutetium-177
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Indium-111