2-Hydroxyestradiol-17α and 4-hydroxyestradiol-17α, catechol estrogfn analogs with reduced estrogen receptor affinity |
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Authors: | George R. Merriam Neil J. MacLusky Leslie A. Johnson Frederick Naftolin |
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Affiliation: | 1. National Institute of Child Health and Hunan Development, Bethesda, MarylandUSA;2. Royal Victoria Hospital, Montreal, QuebecCanada;3. Yale University School of Medicine, New Haven, ConnecticutUSA |
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Abstract: | 2-Hydroxyestradiol-17α and 4-hydroxyestradiol-17α, the catechol derivatives of estradiol-17α, have reduced affinity for hypothalamic, pituitary, and uterine estrogen receptors, but retain a potency for interaction with catechol-O-methyltransferase equal to that of the natural, 17β-hydroxy catechols. This dissociation of receptor binding and catecholamine interactions nay allow the use of the 17α catechols as a probe for the mechanism of action of the catechol estrogens. |
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Keywords: | Address for reprint requests: NIH Building 10 Room 10B09 Bethesda Md. 20205. |
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