Abstract
To establish a strategy for developing (111)In-diethylenetriaminepentaacetic acid ((111)In-DTPA)-octreotide, a diagnostic radiopharmaceutical agent for tumors, with reduced non-specific renal radio-accumulation, the compounds having D-glutamic acid (Glu) or gamma-carboxy-D-glutamic acid (carboxy-Glu) as the N-terminal amino acid were examined for in vivo radio-distribution. Compounds carrying Glu and carboxy-Glu containing one and two negative charges, respectively, showed lower renal radio-accumulation than that carrying D-phenylalanine. It was revealed that the introduction of a negative charge reduces the renal radio-accumulation independently from the number of negative charges. The present result can be a clue for the development of (111)In-DTPA-octreotides with reduced the renal radio-accumulation.
MeSH terms
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1-Carboxyglutamic Acid / chemistry*
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Animals
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Buffers
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Carbon Dioxide / chemistry*
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Drug Stability
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Glutamic Acid / chemistry*
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Hydrogen-Ion Concentration
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Indium Radioisotopes
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Infusions, Intravenous
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Kidney / diagnostic imaging
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Kidney / metabolism*
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Male
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Mice
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Mice, Inbred Strains
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Pentetic Acid / administration & dosage
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Pentetic Acid / analogs & derivatives
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Pentetic Acid / chemical synthesis
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Pentetic Acid / chemistry
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Phenylalanine / chemistry*
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Phosphates / chemistry
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Radionuclide Imaging
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Radiopharmaceuticals / blood
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Radiopharmaceuticals / chemistry
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Radiopharmaceuticals / pharmacokinetics*
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Tissue Distribution
Substances
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(111)indium-DTPA-D-phe octreoide
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Buffers
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Indium Radioisotopes
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Phosphates
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Radiopharmaceuticals
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Carbon Dioxide
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carboxyl radical
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Glutamic Acid
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Phenylalanine
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1-Carboxyglutamic Acid
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Pentetic Acid