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Androsterone - Androgenic, Anti-estrogenic, Thyromimetic Neurosteroid

Discussion in 'IdeaLabs' started by haidut, Sep 15, 2016.

  1. haidut

    haidut Member

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    EDIT: Since I keep getting questions about androsterone, here is Ray's response when asked about it:
    Ray Peat Email Advice Depository Discussion/Comment Thread
    "...I think it would be safe enough to try in treating cancer or brain degenerative diseases."

    Here is one reference that gives backing to his statement above:
    Antitumor Steroids - ScienceDirect
    "...Androsterone (11) effected a 63% inhbition of bronchiogenic carcinoma A-42, 42% inhibition of epidermoid carcinoma HEp3, 81% inhibition of sarcoma HS1, and 35% inhbition of intestinal adenocarcinoma HAd1, all tested in egg [9]."

    Unlike other products that we have released over the years, this one is almost completely unknown outside bodybuilding circles. Even among die-hard bodybuilders it is exclusively known as its ability to function as pro-hormone for more potent androgens like DHT and 5-androstanedione. See attached images for tha pathways of androsterone conversion back into potent androgens like DHT.
    Androsterone - Wikipedia, the free encyclopedia

    "...Androsterone, or 3α-hydroxy-5α-androstan-17-one, is an endogenous steroid hormone, neurosteroid, and putative pheromone.[1] It is a weak androgen with a potency that is approximately 1/7th that of testosterone.[2]In addition, it can be converted to dihydrotestosterone (DHT) from 3α-hydroxysteroid dehydrogenase and 17β-hydroxysteroid dehydrogenase, bypassing conventional intermediates such as androstenedione and testosterone, and as such, can be considered to be a metabolic intermediate in its own right.[3][4] Androsterone is also known to be an inhibitory androstane neurosteroid,[5][6] acting as a positive allosteric modulator of theGABAA receptor,[7] and possesses anticonvulsant effects.[8] The unnatural enantiomer of androsterone is more potent as a positive allosteric modulator of GABAA receptors and as an anticonvulsant than the natural form.[9] Androsterone's 3β-isomer is epiandrosterone, and its 5β-epimer is etiocholanolone."

    Dihydrotestosterone synthesis pathways from inactive androgen 5α-androstane-3β,17β-diol in prostate cancer cells: Inhibition of intratumoural 3β-hydroxysteroid dehydrogenase activities by abiraterone : Scientific Reports
    Androgen deprivation promotes intratumoral synthesis of dihydrotestosterone from androgen metabolites in prostate cancer
    Dihydrotestosterone synthesis bypasses testosterone to drive castration-resistant prostate cancer
    "...The four 5α-reduced 19-carbon steroids [5α-dione, DHT, androsterone, and Adiol] are interconvertible through reversible reactions (Fig. 1). Comparison of the accumulation of total 5α-reduced steroids with [3H]-AD and [3H]-T treatments further shows that AD→5α-dione is the dominant entryway to 5α-reduced steroids (Fig. 2E)."

    However, androsterone is a very interesting steroid in its own right and for a lack of a better analogy I would call it the "mirror image of DHT" due to identical structure but with reversed functional groups. It also seems to share quite a few of progesterone's effects - i.e. anti-estrogenic, sedative, anti-convulsant, pro-thyroid, pro-metabolic, brain protective, promoting insulin sensitivity, anti-adrenaline, anti-cortisol, anti-cancer, anti-depressant, etc. Some studies have gone as far as to suggest that it is androsterone that is the actual steroid with real metabolic activity while all other steroids before it in the pathways (including T and DHT) are the actual pro-hormones.

    http://press.endocrine.org/doi/abs/10.1210/jcem-27-8-1208?journalCode=jcem
    "...These two studies demonstrate the surprising extent to which an important, biologically active, hormone metabolite is further utilized in vivo in man. They raise many further problems. Perhaps the most important of these is the fate of the large portion that was not detected in urine or feces. From the extent of the oxidation of the C-3 hydroxyl group, it might be concluded that a part of the androsterone could serve an important function in man as the coenzyme in a transhydrogenase system, as has indeed been demonstrated with bacterial (15) and rat liver (16) preparations."
    "...In view of its biological activity and its participation in oxidation-reduction systems, it seems clear that androsterone may have metabolic functions equal to those of the hormones which generate it. Since, with the exception of testosterone, the physiological role of the other androgens is unclear, it is perhaps not too speculative to suggest that one function of these hormones may be the production of this important "metabolite."

    Unlike progesterone androsterone does not have the potential for anti-androgenic effects of high doses progesterone in males. It is truly a pity that this amazing chemical saw so much research in the middle of the 20th century and even wild commercial success as the drug Atromid, only to be forgotten and replaced by much more toxic alternatives.

    The units listed on the label are just for measurement purposes. They do not indicate or suggest optimal dose. Please note that similar to the products sold by companies like BlueSky, this product if for lab/research use only. The product can be ordered from the link below:
    http://www.idealabsdc.com/lab

    *******************************************************************************
    Androsterone is an androgenic steroid derived via the activity of the enzyme 5-AR and is a donwstream metabolite of the more potent androgen DHT. Like all 5-AR derived androgens, androsterone displays anti-estrogenic and anti-glucocorticoid activity and in addition serves as a pro-hormone for DHT and other potent androgens. In addition, androsterone is a neurosteroid with potent GABA agonist activity, and is known to function as a pheromone in many animal species including humans. It has been shown to possess anti-depressant and anti-proliferative effects. Perhaps most importantly, it has been found to act like as a potent thyroid mimetic / surrogate and as such to increase basal temperature, oxygen consumption and lower lipid levels in humans.

    Drops per container: about 240
    Each drop contains the following ingredients:

    Androsterone: 1 mg

    Other ingredients: (1) DMSO, ethanol; or (2) tocopherols, MCT
    *******************************************************************************

    References:

    1. Androgenic / pro-sexual
    Remarkable Synergistic Anabolic /androgenic Effect Of Androsterone And DHEA Combination
    Androsterone - Androgenic Neurosteroid Required For Male Sexual Behavior
    Androsterone - The Legal Pro-hormone For Potent 5-AR Derived Androgens

    2. Anti-estrogenic
    Androsterone - A Potent Steroidal Aromatase Inhibitor

    3. Thyroid mimetic / surrogate
    Androsterone - The Forgotten But Potent Thyroid Mimetic
    Androsterone Is A Potent Agonist / Activator Of The Farnesoid X Receptor (FXR)

    4. Anti-adrenaline
    Androsterone Inhibits Catecholamine Release

    5. Anti-cancer
    Androsterone - A Neurosteroid With Anti-cancer Activity

    6. Insulin resistance / sensitivity, diabetes
    Androsterone - A Potential Treatment For Insulin Resistance And Diabetes

    7. Neurosteroid / anti-sepressant
    Androsterone - An Andidepressant Neurosteroid
    The Antidepressant Mechanism Of Androsterone
    Androsterone - A Potent Anxiolytic, Sedative, And Anti-convulsant Neurosteroid
     

    Attached Files:

  2. Tarmander

    Tarmander Member

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    Looks like the old dosage of Atromid was around 2 grams per day. I am guessing by the amount in this bottle, that this is more potent and such an amount is not needed?

    I cannot find a range of dosage that would be appropriate to experiment with. Any clues you could give Haidut?

    Also, this hormone is pretty new to me and I am trying to wrap my head around exactly where it is made in the body. Adrenals? Testicles? Meaning, would castrates have lower levels of this hormone due to lower levels of androgens?
     
  3. haidut

    haidut Member

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    It is made both in testicles and adrenals. Physiological doses are under 10mg a day, and doses as low as 2mg - 3mg should be able to inhibit aromatase by more than 90%.
    Androsterone - A Potent Steroidal Aromatase Inhibitor

    There seems to be great synergy with aromatizable steroids like DHEA, and the optimal ratio is from 1:1 to 1:3 in favor of DHEA.
    Remarkable Synergistic Anabolic /androgenic Effect Of Androsterone And DHEA Combination

    Not sure there is an upper dose limit other than what you can tolerate in terms of higher temps as androsterone is a thyroid mimetic.
    Androsterone - The Forgotten But Potent Thyroid Mimetic
     
  4. encerent

    encerent Member

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    @haidut Any of your rats have reactions unique to this (ie, effects that aren't given to them by other idealab sups)? And in general, how have your rats been affected by this?
     
  5. DankMemes

    DankMemes Member

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    Haidut congrats on the new product.

    How does this compare to 11 keto dht? What benefits could it provide that dht can't and vice versa?
     
  6. Laurence

    Laurence Member

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    Can you elaborate on any testing to show that this is androsterone and not the beta isomer epiandrosterone?

    Androsterone vs Epiandrosterone

    Patrick Arnold:
     
  7. cats

    cats Member

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    What is the potential for endogenous shutdown with this, given alone or in combination with DHEA and/or 11keto-DHT?
     
  8. haidut

    haidut Member

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    The most pronounced effects I noticed were anti-depressant (almost immediate), sedative and anxiolytic (immediate) and anti-stress. I'd say it is a lot better as a neurosteroid and metabolism booster than 11-keto DHT.
     
  9. haidut

    haidut Member

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    Can't really separate effects of 11-keto DHT from androsterone. We don't know how much of 11-keto DHT effects are really its own effects or effects from downstream metabolism into androsterone.
     
  10. haidut

    haidut Member

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    Patrick is right, and I specifically avoided epiandrosterone since it is not only inactive as an androgen but also as an aromatase inhibitor. I have the certificate of analysis from the vendor, so I guess that's my proof. Also, I tested both androsterone and epiandrosterone and the difference is immense. Whoever has access to epiandrosterone can try it and the compare to our androsterone. The difference is night and day. Epiandrosterone has a mild fever producing effect, which feels quite annoying and not like the metabolism boost that androsterone provides. If Patrick wants to get a bottle from us and test it, I'd be happy to provide it. I won't say no to free chemical analysis :)
     
  11. DaveFoster

    DaveFoster Member

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    @haidut Any possibility for shutdown of the HPTA at doses >10 mg?
     
  12. Pet Peeve

    Pet Peeve Member

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    Dammit! Illegal in Norway...
     
  13. mirc12354

    mirc12354 Member

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    What dosages have you used?

    You have written that it is "a potent thyroid mimetic / surrogate and as such to increase basal temperature, oxygen consumption and lower lipid levels in humans." Do you think it is safe to use if one has a rather low cholesterol levels and a good thyroid function (at least according to body temperature and TSH being under 1)? I am interested in anti-cortisol action mainly.
     
  14. Laurence

    Laurence Member

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    Also in Australia :(
     
  15. Rand56

    Rand56 Member

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    What is the half life of androsterone?

    Would it be wise if I wanted to experiment on rat with this who is already taking a low dose of 11-keto DHT <2 drops per day>, to stop the application of 11-keto?

    Pardon my lay person question here, and I could be wrong, but if something is anti-adrenaline, does this mean it also lowers dopamine?
     
  16. haidut

    haidut Member

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    Doubt it, as some human studies used several hundred milligrams daily and found no ill effects on HPTA. But it always helps to keep an eye out for side effects.
     
  17. haidut

    haidut Member

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    I posted the thyroid effects mainly as an indication that thyroid manifests its effects through downstream hormones like androsterone. If you cholesterol is low and thyroid function is good then there is probably no need to add another variable. A combination of androsterone and progesterone would probably be best for cortisol management. Androsterone and DHEA may also work as DHEA inhibits cortisol synthesis as well.
     
  18. haidut

    haidut Member

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    Adrenaline is downstream from dopamine, so inhibiting it does not mean dopamine will also go low. There animal studies showing androsterone opposes prolactin effects, and that would not have happened if androsterone was lowering dopamine somehow. I think androsterone can replace 11-keto DHT in doses about twice as high. So, if a single dose for you of 11-keto DHT was say 2 drops, I'd try 4 drops androsterone as a replacement.
     
  19. Rand56

    Rand56 Member

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    Thanks Haidut! Got it on order already.
     
  20. whereismyOJ

    whereismyOJ Member

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    So, if a male rat is trying to raise testosterone (currently using injections, but we believe most of it's converting to estrogen), as well as trying to improve thyroid function, increase energy, lower stress, would this new Androsterone work better than the 11 keto DHT, or would using both be better?

    Our original plan was to get the 11 keto DHT, TyroMix, and maybe Energin and Estroban.
     
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