Cytoplasmic progesterone receptors in the hypothalamus-preoptic area of the mouse: Effect of estrogen priming

A synthetic progestin, R5020, was used to identify cytoplasmic progestin receptors in the hypothalamuspreoptic area (HPOA) of ovariectomized mice. These high-affinity receptors exhibited an apparent dissociation constant of approx. 1 nM. The receptors were specific for progestins. [ 3H]R5020 binding...

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Published inJournal of steroid biochemistry Vol. 19; no. 5; pp. 1571 - 1575
Main Authors Roselli, Charles E., Snipes, Charles A.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier B.V 01.01.1983
New York, NY Pergamon
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Abstract A synthetic progestin, R5020, was used to identify cytoplasmic progestin receptors in the hypothalamuspreoptic area (HPOA) of ovariectomized mice. These high-affinity receptors exhibited an apparent dissociation constant of approx. 1 nM. The receptors were specific for progestins. [ 3H]R5020 binding was inhibited by more than 50% with a 50-fold excess of either radioinert R5020 or progesterone. 5α-Dihydroprogesterone inhibited binding to a lesser extent. 3α-Hydroxy-5α-pregnane 20-one and cortisol did not compete for [ 3H]R5020 binding. Administration of estradiol benzoate (10 μg), 48 h prior to death, resulted in a 54% increase in the HPOA progestin receptor concentration when compared to oil-injected controls. These data demonstrate that there are specific and saturable cytoplasmic progestin receptors in the mouse HPOA and that the concentration of these receptors is increased after estrogen treatment.
AbstractList A synthetic progestin, R5020, was used to identify cytoplasmic progestin receptors in the hypothalamuspreoptic area (HOPOA) of ovariectomized mice. These high-affinity receptors exhibited an apparent dissociation constant of approx. 1 nM. The receptors were specific for progestins. ( super(3)H)R5020 binding was inhibited by more than 50% with a 50-fold excess of either radioinert R5020 or progesterone. Administration of estradiol benzoate (10 mu g), 48 h prior to death, resulted in a 54% increase in the HPOA progestin receptor concentration when compared to oil-injected controls. These data demonstrate that there are specific and saturable cytoplasmic progestin receptors in the mouse HPOA and that the concentration of these receptors is increased after estrogen treatment.
A synthetic progestin, R5020, was used to identify cytoplasmic progestin receptors in the hypothalamuspreoptic area (HPOA) of ovariectomized mice. These high-affinity receptors exhibited an apparent dissociation constant of approx. 1 nM. The receptors were specific for progestins. [ 3H]R5020 binding was inhibited by more than 50% with a 50-fold excess of either radioinert R5020 or progesterone. 5α-Dihydroprogesterone inhibited binding to a lesser extent. 3α-Hydroxy-5α-pregnane 20-one and cortisol did not compete for [ 3H]R5020 binding. Administration of estradiol benzoate (10 μg), 48 h prior to death, resulted in a 54% increase in the HPOA progestin receptor concentration when compared to oil-injected controls. These data demonstrate that there are specific and saturable cytoplasmic progestin receptors in the mouse HPOA and that the concentration of these receptors is increased after estrogen treatment.
A synthetic progestin, R5020, was used to identify cytoplasmic progestin receptors in the hypothalamuspreoptic area (HPOA) of ovariectomized mice. These high-affinity receptors exhibited an apparent dissociation constant of approx. 1 nM. The receptors were specific for progestins. [3H]R5020 binding was inhibited by more than 50% with a 50-fold excess of either radioinert R5020 or progesterone. 5 alpha-Dihydroprogesterone inhibited binding to a lesser extent. 3 alpha-Hydroxy-5 alpha-pregnane-20-one and cortisol did not compete for [3H]R5020 binding. Administration of estradiol benzoate (10 micrograms), 48 h prior to death, resulted in a 54% increase in the HPOA progestin receptor concentration when compared to oil-injected controls. These data demonstrate that there are specific and saturable cytoplasmic progestin receptors in the mouse HPOA and that the concentration of these receptors is increased after estrogen treatment.
Author Roselli, Charles E.
Snipes, Charles A.
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IsPeerReviewed true
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Issue 5
Keywords B
progesterone
EDTA
K d
Tris
5α-dihydroprogesterone (5α-DHP)
3α-ol
RBA
TED buffer
cortisol
B 0
B s
R5020
HPOA
Priming effect
Rodentia
Hypothalamus
Vertebrata
Mammalia
Synthetic product
Mouse
Estrogenization
Preoptic nucleus
Progesterone
Sex steroid hormone
Cytoplasm
Hormonal receptor
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Snippet A synthetic progestin, R5020, was used to identify cytoplasmic progestin receptors in the hypothalamuspreoptic area (HPOA) of ovariectomized mice. These...
A synthetic progestin, R5020, was used to identify cytoplasmic progestin receptors in the hypothalamuspreoptic area (HOPOA) of ovariectomized mice. These...
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SubjectTerms Animals
Binding, Competitive
Biological and medical sciences
Cytosol - metabolism
Estradiol - pharmacology
Female
Fundamental and applied biological sciences. Psychology
Hypothalamus - metabolism
Kinetics
Mammalian female genital system
Mice
Morphology. Physiology
Norpregnadienes - metabolism
Preoptic Area - metabolism
Promegestone - metabolism
Receptors, Progesterone - drug effects
Receptors, Progesterone - metabolism
Vertebrates: reproduction
Title Cytoplasmic progesterone receptors in the hypothalamus-preoptic area of the mouse: Effect of estrogen priming
URI https://dx.doi.org/10.1016/0022-4731(83)90372-2
https://www.ncbi.nlm.nih.gov/pubmed/6685796
https://search.proquest.com/docview/13850267
https://search.proquest.com/docview/80787716
Volume 19
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