Temporal relationships between hormone receptor binding and biological responses inthe uterus: Studies with short- and long-acting derivatives of estriol

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Abstract

The temporal relationships between hormone receptor binding and early and late biological responses in the uterus were examined using estriol (E3), a weak estrogen, and several morelong acting estriol derivatives, namely ethinyl estriol (EE3) (estriol cyclopentyl ether (E3CPE), and ethinyl estriol)cyclopentyl ether (EE3CPE). Dose-response curves) of 3‐day uterotrophic assays indicate that biological potency follows the order EE3CPE (EE3 or estradiol) E3 CPE > E3 After a single injection of 5 μg of compound, E3 elicits the early uterotrophic responses (increased uterine wet weight and 2‐deoxyglucose phosphorylation at 2‐6 h) but gives only weak stimulation of later uterotrophic responses (enhanced rates of 2‐deoxyglucose phosphorylation at 20‐24 h and increased DNA synthesis rate and uterine weight (over a 72 h period). E3, EE3 and estradiol all elicit a rapid (maximal by 1/2ȁ1 h) uptake of receptor into the nucleus and show an equivalent wet weight response at 3 h. After E3 nuclear receptor levels and uterine weight decline rapidly; however, after (EE)3 estradiol, nuclear receptor levels decline less rapidly remaining at least two-fold above the control until 24ȁ48 h, and uterine weight also remains elevated for at least 48ȁ72 h. EE3 CPE elicits both the early (4 h) and later (20‐24 h) waves ofglucose metabolism, shows a prolonged effect on DNA synthesis rate, and shows the most dramatic andprolonged (beyond 72 h) maintenance of elevated uterine weight and high nuclear receptor (beyond 24 h).

Original languageEnglish (US)
Pages (from-to)220-227
Number of pages8
JournalEndocrinology
Volume98
Issue number1
DOIs
StatePublished - Jan 1976

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Estriol
Uterus
Hormones
Weights and Measures
Ether
Cytoplasmic and Nuclear Receptors
Estradiol
Phosphorylation
Estradiol Receptors
DNA
Biological Assay
Estrogens
Maintenance
Injections
ethinyl estriol

ASJC Scopus subject areas

  • Endocrinology

Cite this

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title = "Temporal relationships between hormone receptor binding and biological responses inthe uterus: Studies with short- and long-acting derivatives of estriol",
abstract = "The temporal relationships between hormone receptor binding and early and late biological responses in the uterus were examined using estriol (E3), a weak estrogen, and several morelong acting estriol derivatives, namely ethinyl estriol (EE3) (estriol cyclopentyl ether (E3CPE), and ethinyl estriol)cyclopentyl ether (EE3CPE). Dose-response curves) of 3‐day uterotrophic assays indicate that biological potency follows the order EE3CPE (EE3 or estradiol) E3 CPE > E3 After a single injection of 5 μg of compound, E3 elicits the early uterotrophic responses (increased uterine wet weight and 2‐deoxyglucose phosphorylation at 2‐6 h) but gives only weak stimulation of later uterotrophic responses (enhanced rates of 2‐deoxyglucose phosphorylation at 20‐24 h and increased DNA synthesis rate and uterine weight (over a 72 h period). E3, EE3 and estradiol all elicit a rapid (maximal by 1/2ȁ1 h) uptake of receptor into the nucleus and show an equivalent wet weight response at 3 h. After E3 nuclear receptor levels and uterine weight decline rapidly; however, after (EE)3 estradiol, nuclear receptor levels decline less rapidly remaining at least two-fold above the control until 24ȁ48 h, and uterine weight also remains elevated for at least 48ȁ72 h. EE3 CPE elicits both the early (4 h) and later (20‐24 h) waves ofglucose metabolism, shows a prolonged effect on DNA synthesis rate, and shows the most dramatic andprolonged (beyond 72 h) maintenance of elevated uterine weight and high nuclear receptor (beyond 24 h).",
author = "Lan, {Nancy C.} and Katzenellenbogen, {Benita S.}",
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T1 - Temporal relationships between hormone receptor binding and biological responses inthe uterus

T2 - Studies with short- and long-acting derivatives of estriol

AU - Lan, Nancy C.

AU - Katzenellenbogen, Benita S.

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N2 - The temporal relationships between hormone receptor binding and early and late biological responses in the uterus were examined using estriol (E3), a weak estrogen, and several morelong acting estriol derivatives, namely ethinyl estriol (EE3) (estriol cyclopentyl ether (E3CPE), and ethinyl estriol)cyclopentyl ether (EE3CPE). Dose-response curves) of 3‐day uterotrophic assays indicate that biological potency follows the order EE3CPE (EE3 or estradiol) E3 CPE > E3 After a single injection of 5 μg of compound, E3 elicits the early uterotrophic responses (increased uterine wet weight and 2‐deoxyglucose phosphorylation at 2‐6 h) but gives only weak stimulation of later uterotrophic responses (enhanced rates of 2‐deoxyglucose phosphorylation at 20‐24 h and increased DNA synthesis rate and uterine weight (over a 72 h period). E3, EE3 and estradiol all elicit a rapid (maximal by 1/2ȁ1 h) uptake of receptor into the nucleus and show an equivalent wet weight response at 3 h. After E3 nuclear receptor levels and uterine weight decline rapidly; however, after (EE)3 estradiol, nuclear receptor levels decline less rapidly remaining at least two-fold above the control until 24ȁ48 h, and uterine weight also remains elevated for at least 48ȁ72 h. EE3 CPE elicits both the early (4 h) and later (20‐24 h) waves ofglucose metabolism, shows a prolonged effect on DNA synthesis rate, and shows the most dramatic andprolonged (beyond 72 h) maintenance of elevated uterine weight and high nuclear receptor (beyond 24 h).

AB - The temporal relationships between hormone receptor binding and early and late biological responses in the uterus were examined using estriol (E3), a weak estrogen, and several morelong acting estriol derivatives, namely ethinyl estriol (EE3) (estriol cyclopentyl ether (E3CPE), and ethinyl estriol)cyclopentyl ether (EE3CPE). Dose-response curves) of 3‐day uterotrophic assays indicate that biological potency follows the order EE3CPE (EE3 or estradiol) E3 CPE > E3 After a single injection of 5 μg of compound, E3 elicits the early uterotrophic responses (increased uterine wet weight and 2‐deoxyglucose phosphorylation at 2‐6 h) but gives only weak stimulation of later uterotrophic responses (enhanced rates of 2‐deoxyglucose phosphorylation at 20‐24 h and increased DNA synthesis rate and uterine weight (over a 72 h period). E3, EE3 and estradiol all elicit a rapid (maximal by 1/2ȁ1 h) uptake of receptor into the nucleus and show an equivalent wet weight response at 3 h. After E3 nuclear receptor levels and uterine weight decline rapidly; however, after (EE)3 estradiol, nuclear receptor levels decline less rapidly remaining at least two-fold above the control until 24ȁ48 h, and uterine weight also remains elevated for at least 48ȁ72 h. EE3 CPE elicits both the early (4 h) and later (20‐24 h) waves ofglucose metabolism, shows a prolonged effect on DNA synthesis rate, and shows the most dramatic andprolonged (beyond 72 h) maintenance of elevated uterine weight and high nuclear receptor (beyond 24 h).

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