Inhibitory effect of 5-alpha-dihydroprogesterone on nuclear estrogen receptor binding of the anterior pituitary and uterus in the rat

Neuroendocrinology
M A FuentesV B Mahesh

Abstract

Progesterone and its metabolite 5 alpha-dihydroprogesterone (5 alpha-DHP) have been shown to bring about gonadotropin release in the estrogen-primed ovariectomized rat. One of the actions of progesterone is the decrease in occupied estrogen receptors (E2Rs) in the anterior pituitary and uterus. This study attempted to determine if 5 alpha-DHP had a similar effect on pituitary and uterine E2Rs. Estrogen-primed ovariectomized mature female rats were injected with either vehicle, or 0.2, 0.8 or 2 mg/kg body weight (BW) of 5 alpha-DHP, 2 h before sacrifice and 1 h before the last estradiol injection (2 micrograms/rat). Nuclear E2Rs were determined by Scatchard analyses in the uterus and anterior pituitary. Total nuclear E2R levels of both tissues showed a 2-fold increase in the number of estradiol-binding sites after estradiol administration, as compared to control groups. In estradiol-primed rats, 5 alpha-DHP produced a significant decrease in total nuclear E2R levels in a tissue-specific manner. In the pituitary, there was a maximal and significant decrease in nuclear E2Rs with 0.2 and 2.0 mg/kg BW of 5 alpha-DHP as compared to estradiol alone; the intermediate dose of 0.8 mg/kg BW of 5 alpha-DHP induced a smaller nonsignificant ...Continue Reading

Citations

Mar 1, 1992·The Journal of Steroid Biochemistry and Molecular Biology·V B Mahesh, D W Brann
Oct 27, 2011·American Journal of Physiology. Endocrinology and Metabolism·Virendra B Mahesh

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