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Catechol oestrogens inhibit oestrogen elicited accumulation of hypothalamic cyclic AMP suggesting role as endogenous anti-oestrogens

Naturevolume 266pages559561 (1977) | Download Citation

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Abstract

THE catechol oestrogens, including 2-hydroxyoestradiol and 2-hydroxyoestrone, are recognised as major metabolic products of oestrogen1. Catechol oestrogens are present in both pituitary and hypothalamus in concentrations at least tenfold higher than the parent oestrogens2. In addition, the synthesis of catechol oestrogens by rat hypothalamic tissue in vitro has also been reported2,3. Catechol oestrogens compete with 17-β-oestradiol (E2) for soluble oestrogen receptors of the pituitary and hypothalamus4, suggesting a role for these compounds in the control of gonadotrophin secretion within the pituitary–hypothalamic axis. We have investigated the effects of 2-hydroxyoestradiol on the oestrogen-elicited accumulation of cyclic AMP in intact hypothalami in vitro, and we report here that 2-hydroxyoestradiol antagonises the increase in cyclic AMP elicited in hypothalami of immature female rats by both diethylstilboestrol (DBS) and E2, suggesting that 2-hydroxyoestradiol may function as an endogenous anti-oestrogen.

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Affiliations

  1. Laboratory of Clinical Science, Section on Pharmacology, NIMH

    • STEVEN M. PAUL
  2. Laboratory of Chemistry, Section on Pharmacodynamics, NIAMDD, Bethesda, Maryland, 20014

    • PHIL SKOLNICK

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https://doi.org/10.1038/266559a0

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