DHT Is Estrogen "receptor" Antagonist

Discussion in 'Scientific Studies' started by haidut, Mar 28, 2016.

  1. haidut

    haidut Member

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    I have posted studies on DHT inhibiting aromatase and increaseing estrogen conjugation and excretion by the liver. However, this study shows that DHT is actually capable of direct anti-estrogen activity by binding to and antagonizing the estrogen "receptor" similarly to progesterone and vitamin E. As I posted in another thread, DHT is also a glucocorticoid antagonist AND increases its excretion.
    DHT Is A Glucocorticoid (cortisol) Antagonist

    Antiestrogenic action of dihydrotestosterone in mouse breast. Competition with estradiol for binding to the estrogen receptor. - PubMed - NCBI

    "...Feminization in men occurs when the effective ratio of androgen to estrogen is lowered. Since sufficient estrogen is produced in normal men to induce breast enlargement in the absence of adequate amounts of circulating androgens, it has been generally assumed that androgens exert an antiestrogenic action to prevent feminization in normal men. We examined the mechanisms of this effect of androgens in the mouse breast. Administration of estradiol via silastic implants to castrated virgin CBA/J female mice results in a doubling in dry weight and DNA content of the breast. The effect of estradiol can be inhibited by implantation of 17 beta-hydroxy-5 alpha-androstan-3-one (dihydrotestosterone), whereas dihydrotestosterone alone had no effect on breast growth. Estradiol administration also enhances the level of progesterone receptor in mouse breast. Within 4 d of castration, the progesterone receptor virtually disappears and estradiol treatment causes a twofold increase above the level in intact animals. Dihydrotestosterone does not compete for binding to the progesterone receptor, but it does inhibit estrogen-mediated increases of progesterone receptor content of breast tissue cytosol from both control mice and mice with X-linked testicular feminization (tfm)/Y. Since tfm/Y mice lack a functional androgen receptor, we conclude that this antiestrogenic action of androgen is not mediated by the androgen receptor. Dihydrotestosterone competes with estradiol for binding to the cytosolic estrogen receptor of mouse breast, whereas 17 beta-hydroxy-5 beta-androstan-3-one (5 beta-dihydrotestosterone) neither competes for binding nor inhibits estradiol-mediated induction of the progesterone receptor. Dihydrotestosterone also promotes the translocation of estrogen receptor from cytoplasm to nucleus; the ratio of cytoplasmic-to-nuclear receptor changes from 3:1 in the castrate to 1:2 in dihydrotestosterone-treated mice. Thus, the antiestrogenic effect of androgen in mouse breast may be the result of effects of dihydrotestosterone on the estrogen receptor. If so, dihydrotestosterone performs one of its major actions independent of the androgen receptor."
     
  2. dookie

    dookie Member

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    The more I read about DHT, the more impressed I am by its beneficial effects. Not only is it antagonistic to estrogen, cortisol, serotonin - the major degenerative forces - but it is also powerfully neuroprotective, and it "quiets" the pituitary, which again may be beneficial in itself.

    DHT may turn out to have some of the same benefits as progesterone and pregnenolone. I actually remember seeing a study that DHT raised progesterone or some of the progesterone-metabolites. (i'll try to find it and post it)

    I am theorizing that DHT may be the "progesterone for men", since it confers some of the same benefits, without damaging libido, or having any feminizing effects. Also, for people having too many side-effects with progesterone (eg it aromatizes into estrogen), maybe DHT could be a solution?

    @haidut - Have you used DHT yourself, or heard from someone who has? Do you have any idea as to how "someone I Know" would go about obtaining DHT? :P (Online bodybuilding pharmacies seem to only have the modified forms like Proviron, and I think Peat prefers the 'bioidenticial' DHT)


    PS: I made a post about DHT too, not too long ago:
    DHT Lowers Cortisol, Estrogen And Is Neuroprotective
     
  3. OP
    haidut

    haidut Member

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    I concur, and as I said in another post, in males the only two hormones worth optimizing for are probably progesterone and DHT. Peat said that to him testosterone is almost as dangerous as estrogen.
    Some people on the forum have used DHT before but I don't think it was bioidentical. As for me, I have only used DHEA, which seems to do a decent job but will probably not match the effects of direct DHT supplementation.
     
  4. Kasper

    Kasper Member

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    Wouldn't it shrink the testicles like supplementing testosterone does? If I recall this correctly about testosterone.
     
  5. Bulletproof?

    Bulletproof? Member

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    I don't know if I can post here, but I found some DHT cream out of Cyrpus, and I have been using that for a little over a week. Can I post the site where I got it from, or is that something that can only be done through PM? Haven't felt much, yet, but they do say not to expect anything for about 2-3 weeks. Will keep you guys posted. @Kasper I have been on TRT for years now and stopped everything about a month ago. I will let you know how my testicles respond.
     
  6. dookie

    dookie Member

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    @haidut
    You said in another post that in nursing homes they were giving people DHT, do you know what doses they were using?
     
  7. OP
    haidut

    haidut Member

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    Nope, it actually increases testicle size as well as prostate (but in a good way).
     
  8. OP
    haidut

    haidut Member

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    The luxury nursing homes in Florida often administer DHT gel to older males (if they want). The dose I have heard used are about 5mg daily for a 70-year old male.
     
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