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5α-Dihydroprogesterone (5α-DHP) Is More Effective Than Progesterone In Lowering Prolactin

Discussion in 'Scientific Studies' started by haidut, Nov 23, 2016.

  1. haidut

    haidut Member

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    Similar to the stud on estrogen receptor decrease, this study shows that the saturated progesterone metabolite 5α-dihydroprogesterone (5α-DHP) is more effective than progesterone at inhibiting prolactin release from the
    pituitary. Just as in the estrogen study, the effective doses of 5α-DHP were 2-3 times lower than the ones needed for progesterone and the most effective dose of 5α-DHP was a relatively low HED of 0.3mg/kg, which brought about a 70% decrease in prolactin release.

    https://www.ncbi.nlm.nih.gov/pubmed/19215357

    "...The purpose of this study was to examine whether the effect of different doses of progesterone on estrogen-induced prolactin release correlated with the effects of progesterone on estrogen receptor dynamics of the anterior pituitary demonstrated by Fuentes et al. (13). In our study, the 0.8 mg/kg body wt and 3.2 mg/kg body wt doses of progesterone inhibited estrogen-induced prolactin release (64% and 60% reduction) whereas the 2.0mg/kg body wt dose was ineffective (4% reduction)."

    "...In view of the uniqueness of this observation it was important to confirm that two doses of the same steroid were active in bringing about a biological change while the intermediate dose was either ineffective or minimally effective. For this purpose we sought out another steroid 5a-dihydroprogesterone, which was related to progesterone and interacted with the progesterone receptor. It also was reported to bring about the selective release of follicle-stimulating hormone by Murphy and Mahesh (15). Progesterone is actively metabolized by both the hypothalamus and anterior pituitary to various metabolites, principally 5adihydroprogesterone (14). 5a-dihydroprogesterone has been shown to bind with high affinity to the progesterone receptor in a variety of tissues (21 -23). In this study 5a-dihydroprogesterone was found to inhibit estrogen-induced prolactin release similar to progesterone (Fig. 2)."

    "...The effect of 5a-dihydroprogesterone upon estradiol-induced prolactin release was influenced by the dose used (Fig. 2). Similar to progesterone, Sa-dihydroprogesterone caused a decrease or no effect on pituitary nuclear estradiol receptors depending upon the dose used (24). A strong correlation was found between those doses which depleted pituitary-occupied nuclear estrogen receptors in the Fuentes et al. study (13) and those that inhibited estradiol-induced prolactin release in this study. In the study of Fuentes et al. (24), the 0.2 mg/kg body wt and 2.0 mg/kg body wt doses of 5α-dihydroprogesterone were more effective in reducing occupied pituitary estrogen receptor levels (54% and 74% reduction; P < 0.01 for both groups) as compared to the 0.8 mg/kg body wt dose (31% reduction) in which the reduction was not significant. In our study, the 0.4 mg/kg body wt and 2.0 mg/kg body wt doses of 5α-dihydroprogesterone inhibited estrogen-induced prolactin release (68% reduction for each), whereas the 0.8 mg/kg body wt dose was ineffective (17% reduction)."

    "...Of considerable interest is the finding that 5α-dihydroprogesterone is twice as potent as progesterone with respect to its effect upon both the estrogen receptor depletion (24) and inhibition of estrogen-induced prolactin secretion (compare Fig. 1 vs Fig. 2). Murphy and Mahesh also reported that the 0.4 mg/kg body wt dose of 5α-dihydroprogesterone brought about selective release of follicle-stimulating hormone in ovariectomized estrogen-primed immature rats (15) and adult rats ovariectomized on the day of proestrus (19), while the 0.8 mg/kg body wt dose was ineffective. The higher potency of 5α-dihydroprogesterone compared to progesterone may suggest a critical role for 5α-dihydroprogesterone as an active mediator of progesterone action at the level of the anterior pituitary."
     
  2. Koveras

    Koveras Member

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    I sense a product release imminent
     
  3. lollipop

    lollipop Guest

    :-D
     
  4. OP
    haidut

    haidut Member

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    Yep, coming up in a few minutes :):
     
  5. aarfai

    aarfai Member

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    Does 5α-DHP have any activity towards androgens? I wasn't able to find anything via a google search
     
  6. moss

    moss Member

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    Excellent find haidut!
     
  7. OP
    haidut

    haidut Member

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  8. tca300

    tca300 Member

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    It seems strange that low doses and high doses are effective for lowering estrogen driven prolactin but medium doses were not very effective. Do you have any speculation as to why? @haidut
    Please only respond if you have extra time, I know you're busy and my question is not important. Thanks!
     
  9. OP
    haidut

    haidut Member

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    Don't have an explanation but the same effects were seen with progesterone as those studies mention - i.e. low and high progesterone doses were effective while medium one was not. Here is the study discussion on this:
    "...The mechanisms involved in the dose-related effects of 5α-DHP on E2R decrease are not clear. The differences observed in the pattern of E2R decrease in the anterior pituitary and uterus strongly suggest that different tissue-specific mechanisms could be involved in this response to 5α-DHP. This study provides another example of the difference in the pattern of E2R decreases in the anterior pituitary and uterus induced by another steroid 5α-DHP, that were observed by us earlier using progesterone."

    Btw, this effect was only seen in pituitary for both prolactin and estrogen inhibition. In other tissues like uterus and periphery the effect was dose-dependent and the medium dose was effective. But given how important the pituitary is for overall metabolism I'd say making sure the proper dose for it is taken is important. Either way, I suspect that most people will experiment on their rats with the higher dose given the strong inhibition of both prolactin and estrogen.
     
  10. tca300

    tca300 Member

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    @haidut Thank you very much for your input!
     
  11. aarfai

    aarfai Member

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