Abstract
This study was aimed at developing a hydrophilic diethylenetriaminepentaacetic acid-tamoxifen (DTPA-Tam) analogue for use in imaging estrogen receptor positive (ER+) lesions. In rat uterine cytosol, the IC50 of DTPA-Tam conjugate was 1 microM and of tamoxifen, 2 microM. Biodistribution, autoradiography, and radionuclide imaging of 111In-DTPA-Tam in breast-tumor-bearing rats showed that tumor-to-tissue ratios increased steadily between 30 min and 48 h. The in vivo response of MCF-7 breast cancer xenografts to tamoxifen and DTPA-Tam in nude mice demonstrated that DTPA-Tam could reduce tumor growth rate. These results indicate that DTPA-Tam, a new hydrophilic ER+ ligand, might be useful in diagnosing ER+ lesions.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Autoradiography
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Breast Neoplasms / diagnostic imaging
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Breast Neoplasms / drug therapy
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Breast Neoplasms / ultrastructure
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Estradiol / metabolism
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Female
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Humans
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Indium Radioisotopes* / chemistry
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Kinetics
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Mammary Neoplasms, Experimental / drug therapy
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Mammary Neoplasms, Experimental / radiotherapy
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Mammary Neoplasms, Experimental / ultrastructure
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Mice
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Mice, Nude
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Pentetic Acid / chemical synthesis*
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Pentetic Acid / pharmacokinetics
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Pentetic Acid / pharmacology
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Radionuclide Imaging
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Rats
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Rats, Inbred F344
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Receptors, Estrogen / analysis*
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Receptors, Estrogen / metabolism
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Tamoxifen / analogs & derivatives*
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Tamoxifen / pharmacokinetics
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Tamoxifen / pharmacology
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Tissue Distribution
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Tritium
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Tumor Cells, Cultured
Substances
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Indium Radioisotopes
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Receptors, Estrogen
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Tamoxifen
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Tritium
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Estradiol
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Pentetic Acid