Abstract
2-Hydroxyest radiol-17 alpha and 4-hydroxyestradiol-17 alpha, the catechol derivatives of estradiol-17 alpha, have reduced affinity for hypothalamic, pituitary, and uterine estrogen receptors, but retain a potency for interaction with catechol-0-methyltransferase equal to that of the natural, 17 beta-hydroxy catechols. This dissociation of receptor binding and catecholamine interactions may allow the use of the 17 alpha catechols as a probe for the mechanism of action of the catechol estrogens.
MeSH terms
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Amygdala / metabolism
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Animals
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Catechol O-Methyltransferase / pharmacology
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Cytosol / enzymology
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Estradiol / analogs & derivatives*
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Estradiol / analysis
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Estradiol / metabolism
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Estradiol / pharmacology
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Estrogens, Catechol
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Female
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Hypothalamus / metabolism
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Methylation
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Norepinephrine / antagonists & inhibitors
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Pituitary Gland / metabolism*
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Preoptic Area / metabolism
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Rats
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Receptors, Estrogen / metabolism*
Substances
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Estrogens, Catechol
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Receptors, Estrogen
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Estradiol
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2-hydroxyestradiol
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4-hydroxyestradiol
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Catechol O-Methyltransferase
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Norepinephrine