The stereoisomers of 17alpha-[123I]iodovinyloestradiol and its 11beta-methoxy derivative evaluated for their oestrogen receptor binding in human MCF-7 cells and rat uterus, and their distribution in immature rats

European Journal of Nuclear Medicine
L J RijksE A van Royen

Abstract

We studied the potential of both stereoisomers of 17alpha-[123I]iodovinyloestradiol (E- and Z-[123I]IVE) and of 11beta-methoxy-17alpha-[123I]iodovinyloestradiol (E- and Z-[123I]MIVE) as suitable radioligands for the imaging of oestrogen receptor(ER)-positive human breast tumours. The 17alpha-[123I]iodovinyloestradiols were prepared stereospecifically by oxidative radio-iododestannylation of the corresponding 17alpha-tri-n-butylstannylvinyloestradiol precursors. Competitive binding studies were performed in order to determine the relative binding affinity (RBA) of the unlabelled 17alpha-iodovinyloestradiols for the ER in both human MCF-7 breast tumour cells and rat uterine tissue, compared with that of diethylstilboestrol (DES). Target tissue uptake, retention and uptake selectivity of their 123I-labelled analogues were studied in immature female rats. All four 17alpha-iodovinyloestradiols showed high affinity for the ER in human MCF-7 cells, as well as rat uterus. Their RBA for the ER showed the following order of decreasing potency: RBA of DES >Z-IVE >Z-MIVE >E-MIVE > or =E-IVE. Neither of these 17alpha-iodovinyloestradiols showed any significant binding to the sex hormone binding globulin in human plasma. The biodistribution ...Continue Reading

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Citations

Jul 1, 1997·European Journal of Nuclear Medicine·E BombardieriM Greco
May 15, 2013·The Journal of Steroid Biochemistry and Molecular Biology·Susana CunhaMaria Cristina Oliveira
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Jul 1, 2020·Chemical Biology & Drug Design·Duo XuXianzhong Zhang

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