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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1997-6-5
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pubmed:abstractText |
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.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0969-8051
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
24
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
65-75
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:9080477-Animals,
pubmed-meshheading:9080477-Breast Neoplasms,
pubmed-meshheading:9080477-Estradiol,
pubmed-meshheading:9080477-Female,
pubmed-meshheading:9080477-Humans,
pubmed-meshheading:9080477-Mammary Neoplasms, Animal,
pubmed-meshheading:9080477-Middle Aged,
pubmed-meshheading:9080477-Radioligand Assay,
pubmed-meshheading:9080477-Rats,
pubmed-meshheading:9080477-Rats, Sprague-Dawley,
pubmed-meshheading:9080477-Receptors, Estrogen,
pubmed-meshheading:9080477-Stereoisomerism,
pubmed-meshheading:9080477-Structure-Activity Relationship,
pubmed-meshheading:9080477-Tissue Distribution,
pubmed-meshheading:9080477-Tomography, Emission-Computed, Single-Photon
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pubmed:year |
1997
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pubmed:articleTitle |
The Z-isomer of 11 beta-methoxy-17 alpha-[123I]iodovinylestradiol is a promising radioligand for estrogen receptor imaging in human breast cancer.
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pubmed:affiliation |
Department of Nuclear Medicine, University of Amsterdam, The Netherlands.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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