Abstract
A hybrid compound (DO3A-BP) featuring a radiometal bifunctional chelator (1,4,7,10-tetraazacyclotetradecane-N,N',N'',N'''-tetraacetic acid, DOTA) and an osteoclast-targeting moiety (bisphosphonate) was designed and synthesized. The (111)In-labeled complex of DO3A-BP showed significantly elevated uptake in osteoclasts compared to the undifferentiated adherent bone marrow derived cells. Biodistribution studies revealed a favorable tissue distribution profile in normal mice with high bone uptake and long retention, and low or negligible accumulation in non-target organs.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Bone Neoplasms / diagnostic imaging*
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Bone Neoplasms / drug therapy*
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Bone Neoplasms / secondary
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Cells, Cultured
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Diagnostic Imaging*
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Diphosphonates / chemistry
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Diphosphonates / pharmacokinetics
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Diphosphonates / pharmacology*
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Heterocyclic Compounds, 1-Ring / chemistry
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Heterocyclic Compounds, 1-Ring / pharmacokinetics
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Heterocyclic Compounds, 1-Ring / pharmacology*
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Indium Radioisotopes
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Male
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Mice
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Mice, Inbred BALB C
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Osteoclasts / metabolism*
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Radionuclide Imaging
Substances
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1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid
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Diphosphonates
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Heterocyclic Compounds, 1-Ring
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Indium Radioisotopes
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1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid