The Z-isomer of 11 beta-methoxy-17 alpha-[123I]iodovinylestradiol is a promising radioligand for estrogen receptor imaging in human breast cancer
| Autor: | Eric A. van Royen, Erik Endert, L. J. M. Rijks, A. G. M. Janssen, Kora de Bruin, G. J. Boer |
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| Přispěvatelé: | Other departments |
| Jazyk: | angličtina |
| Rok vydání: | 1997 |
| Předmět: |
Cancer Research
medicine.medical_specialty medicine.drug_class Mammary gland Estrogen receptor Breast Neoplasms Mammary Neoplasms Animal Biology Rats Sprague-Dawley Radioligand Assay Structure-Activity Relationship Breast cancer In vivo Internal medicine medicine Radioligand Animals Humans Tissue Distribution Radiology Nuclear Medicine and imaging Tomography Emission-Computed Single-Photon Estradiol Cancer Stereoisomerism Middle Aged medicine.disease Rats medicine.anatomical_structure Endocrinology Receptors Estrogen Estrogen Molecular Medicine Female |
| Zdroj: | Nuclear medicine and biology, 24(1), 65-75. Elsevier Inc. |
| ISSN: | 0969-8051 |
| Popis: | The potential of both stereoisomers of 11 beta-methoxy-17 alpha-[123I] iodovinylestradiol (E- and Z-[123I]MIVE) as suitable radioligands for imaging of estrogen receptor (ER)-positive human breast tumours was studied. The 17 alpha-[123I]iodovinylestradiol derivatives were prepared stereospecifically by oxidative radioiododestannylation of the corresponding 17 alpha-tri-n-butylstannylvinylestradiol precursors. Both isomers of MIVE showed high in vitro affinity for dimethylbenzanthracene-induced rat and fresh human mammary tumour ER, that of Z-MIVE however being manyfold higher than that of E-MIVE. In vivo distribution studies with E- and Z-[123I]MIVE in normal and tumour-bearing female rats showed ER-mediated uptake and retention in uterus, ovaries, pituitary, hypothalamus and mammary tumours, again the highest for Z-[123I]MIVE. The uterus- and tumour-to-nontarget tissue (far, muscle) uptake ratios were also highest for Z-[123I]MIVE. Additionally, planar whole body imaging of two breast cancer patients 1-2 h after injection of Z-[123I]MIVE showed increased focal uptake at known tumour sites. Therefore, we conclude that Z-[123I]MIVE is a promising radioligand for the diagnostic imaging of ER in human breast cancer. |
| Databáze: | OpenAIRE |
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