Effect of an Increase in Free Testosterone Brought About by Nettle Root or Activate

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    Question Effect of an Increase in Free Testosterone Brought About by Nettle Root or Activate


    Does anyone know if a product like DS Activate or highly concentrated Nettle Root extract by increasing free testosterone:

    1. Reduces the off-time needed between AAS cycles to make the next cycle effective and/or
    2. Increases the effectiveness of a cycle particularly in the latter stages.


    --------------------------------------------------------------------------------------------
    ** The following reference material on Nettle Root was taken from Life Extension's article "Male Hormone Modulation Therapy" which is itself based on Dr. Eugene Shippen's book entitled The Testosterone Syndrome

    Nettle
    About 90% of testosterone is produced by the testes; the remainder is produced by the adrenal glands. Tes-tosterone functions as an aphrodisiac hormone in brain cells and as an anabolic hormone in the development of bone and skeletal muscle. But testosterone that becomes bound to serum globulin is not available to cell receptor sites and fails to induce a libido effect. It is therefore desirable to increase levels of "free tes-tosterone" in order to ignite sexual arousal in the brain.

    As discussed already, a hormone that controls levels of free testosterone is called SHBG. When testosterone binds to SHBG, it loses its biological activity and becomes known as "bound testosterone," as opposed to the desirable "free testosterone." As men age past age 45, SHBG's binding capacity increases almost dramatically--by 40% on average--and coincides with the age-associated loss of libido.

    Some studies show that the decline in sexual interest with advancing age is not always due to the amount of testosterone produced, but rather to the increased binding of testosterone to globulin by SHBG. This explains why some older men who are on testosterone replacement therapy do not report a long-term aphrodisiac effect. That is, the artificially administered testosterone becomes bound by SHBG and is not bioavailable to cellular receptor sites where it would normally produce a libido-enhancing effect.

    It should be noted that the liver also causes tes-tosterone to bind to globulin. This liver-induced binding of testosterone is worsened by the use of sedatives, antihypertensives, tranquilizers, and alcoholic beverages. The overuse of drugs and alcohol could explain why some men do not experience a libido-enhancing effect when consuming drugs and plant-based aphrodisiacs. An interesting review entitled "How Desire Dies" (Nature, 381/6584, 1996) discusses how frequently prescribed drugs, such as beta-blockers and antidepressants, cause sexual dysfunction. Prescription drugs of all types have been linked to inhibition of libido.

    Logically, one way of increasing libido in older men would be to block the testosterone-binding effects of SHBG. This would leave more testosterone in its free, sexually activating form.

    A highly concentrated extract from the nettle root provides a unique mechanism for increasing levels of free testosterone. European research has identified constituents of nettle root that bind to SHBG in place of testosterone, thus reducing SHBG's binding of free testosterone (309-313). As the authors of one study stated, these constituents of nettle root "may influence the blood level of free, i.e., active, steroid hormones by displacing them from the SHBG binding site."

    The prostate gland also benefits from nettle root. In Germany, nettle root has been used as a treatment for benign prostatic hyperplasia (enlargement of the prostate gland) for decades. A metabolite of testosterone called dihydrotestosterone (DHT) stimulates prostate growth, leading to enlargement. Nettle root inhibits the binding of DHT to attachment sites on the prostate membrane.

    Nettle extracts also inhibit enzymes such as 5-alpha reductase that cause testosterone to convert to DHT. It is the DHT metabolite of testosterone that is known to cause benign prostate enlargement, excess facial hair, and hair loss at the top of the head.

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    Quote Originally Posted by meowmeow
    Does anyone know if a product like DS Activate or highly concentrated Nettle Root extract by increasing free testosterone:

    1. Reduces the off-time needed between AAS cycles to make the next cycle effective and/or
    2. Increases the effectiveness of a cycle particularly in the latter stages.


    --------------------------------------------------------------------------------------------
    ** The following reference material on Nettle Root was taken from Life Extension's article "Male Hormone Modulation Therapy" which is itself based on Dr. Eugene Shippen's book entitled The Testosterone Syndrome

    Nettle
    About 90% of testosterone is produced by the testes; the remainder is produced by the adrenal glands. Tes-tosterone functions as an aphrodisiac hormone in brain cells and as an anabolic hormone in the development of bone and skeletal muscle. But testosterone that becomes bound to serum globulin is not available to cell receptor sites and fails to induce a libido effect. It is therefore desirable to increase levels of "free tes-tosterone" in order to ignite sexual arousal in the brain.

    As discussed already, a hormone that controls levels of free testosterone is called SHBG. When testosterone binds to SHBG, it loses its biological activity and becomes known as "bound testosterone," as opposed to the desirable "free testosterone." As men age past age 45, SHBG's binding capacity increases almost dramatically--by 40% on average--and coincides with the age-associated loss of libido.

    Some studies show that the decline in sexual interest with advancing age is not always due to the amount of testosterone produced, but rather to the increased binding of testosterone to globulin by SHBG. This explains why some older men who are on testosterone replacement therapy do not report a long-term aphrodisiac effect. That is, the artificially administered testosterone becomes bound by SHBG and is not bioavailable to cellular receptor sites where it would normally produce a libido-enhancing effect.

    It should be noted that the liver also causes tes-tosterone to bind to globulin. This liver-induced binding of testosterone is worsened by the use of sedatives, antihypertensives, tranquilizers, and alcoholic beverages. The overuse of drugs and alcohol could explain why some men do not experience a libido-enhancing effect when consuming drugs and plant-based aphrodisiacs. An interesting review entitled "How Desire Dies" (Nature, 381/6584, 1996) discusses how frequently prescribed drugs, such as beta-blockers and antidepressants, cause sexual dysfunction. Prescription drugs of all types have been linked to inhibition of libido.

    Logically, one way of increasing libido in older men would be to block the testosterone-binding effects of SHBG. This would leave more testosterone in its free, sexually activating form.

    A highly concentrated extract from the nettle root provides a unique mechanism for increasing levels of free testosterone. European research has identified constituents of nettle root that bind to SHBG in place of testosterone, thus reducing SHBG's binding of free testosterone (309-313). As the authors of one study stated, these constituents of nettle root "may influence the blood level of free, i.e., active, steroid hormones by displacing them from the SHBG binding site."

    The prostate gland also benefits from nettle root. In Germany, nettle root has been used as a treatment for benign prostatic hyperplasia (enlargement of the prostate gland) for decades. A metabolite of testosterone called dihydrotestosterone (DHT) stimulates prostate growth, leading to enlargement. Nettle root inhibits the binding of DHT to attachment sites on the prostate membrane.

    Nettle extracts also inhibit enzymes such as 5-alpha reductase that cause testosterone to convert to DHT. It is the DHT metabolite of testosterone that is known to cause benign prostate enlargement, excess facial hair, and hair loss at the top of the head.

    Since DHT is actually a stronger androgen that test, the effectiveness of this product should be in terms of gains can be debated...
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    My theory is that it gives you more usable test to help during pct but will take longer to recover because the increased free test levels.
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    Interesting discussion here about same subject:



    http://forum.avantlabs.com/index.php?showtopic=20085
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    8 week log with bloodwork


    here was pretest:

    red and white cell count = ok, bilirubin 1.5 (elevated) ast 28, alt 24 (both normal)
    Estradiol = 38 normal
    Lipids = hdl 46, ldl 68, tri 106
    igf = 129 normal
    thyroid = tsh 1.737, thyrox 7.6, t3 32, free thy 2.4
    prostate = .5
    test = 612, free 12.6 (8.1-25.1 is normal)

    Final Results:

    red and white cell count = ok, bilirubin 1.1 (ok) ast 25, alt 24 (both normal)
    Estradiol = 20 normal
    Lipids = hdl 39, ldl 68, tri 146
    igf = 100 LOW WTF?
    thyroid = tsh 3.046, thyrox 7.2, t3 34, free thy 2.4
    prostate = .5
    test = 632, free 20.3


    20 pills per day, DS beta tester
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    20 pills/day? The reccomended dose is 4! There are 120 in the bottle - thats not even a weeks worth!

    Anyhow it works as advertised it seems.

    What type of effect did it have on your gym gains and libido?
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    KD1, that is b/c it was the beta. They didn't have the final potency down yet. One bottle had 300 caps.
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    Quote Originally Posted by KD1
    20 pills/day? The reccomended dose is 4! There are 120 in the bottle - thats not even a weeks worth!

    Anyhow it works as advertised it seems.

    What type of effect did it have on your gym gains and libido?

    I dont think it had any real affect at all on libido or strength.

    the bump is pretty small and probably about the same as ZMA.

    maybe im just used to using gear, though.


    i wont buy it again, but the guys at DS treated me well and I like their supps
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    Quote Originally Posted by x_muscle
    Interesting discussion here about same subject:

    http://forum.avantlabs.com/index.php?showtopic=20085
    Thanks for alerting me to the discussion over there. I've been looking through posts on body building forums , male health and life-extension type forums from users of Nettle Root and Avena Sativa. Accounts are anectdotal and of limited use but still interesting like this one from the Anabolex forum where a multi-year long cycle user with few breaks attributes his good mood, libido, sexual function and continued muscle tone to Nettle & Avena Satvia. http://www.anabolex.com/forums/showp...2&postcount=23
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    Quote Originally Posted by momod
    I dont think it had any real affect at all on libido or strength.

    the bump is pretty small and probably about the same as ZMA.

    maybe im just used to using gear, though.


    i wont buy it again, but the guys at DS treated me well and I like their supps
    A raise from 12 to 20 in free testesterone is a pretty significant increase. Maybe someone else can chime in, but Im pretty sure that kind of increase is definitely something to at least be a little excited about. Im using activate with my PCT right now and am so far in love with it. I think it has helped dramatically. I had to take a week off due to sickness one week into PCT, and now on my fourth week into PCT Ive not only retained, but gained as well. That is not usual for me at all.
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    I beta tested Activate as well. IMO, it should only be used with an effective testosterone booster (ATD).

    I didn't see any increased gains on it with Bobo's bulking program.
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    Quote Originally Posted by Lakevillethor
    Since DHT is actually a stronger androgen that test, the effectiveness of this product should be in terms of gains can be debated...
    This is actually one of the reasons it works so well at the end of a cycle and during PCT. You don't sound like you really understand androgens that well.
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    Quote Originally Posted by adrenalinaddict
    A raise from 12 to 20 in free testesterone is a pretty significant increase. Maybe someone else can chime in, but Im pretty sure that kind of increase is definitely something to at least be a little excited about. Im using activate with my PCT right now and am so far in love with it. I think it has helped dramatically. I had to take a week off due to sickness one week into PCT, and now on my fourth week into PCT Ive not only retained, but gained as well. That is not usual for me at all.
    I would definately think so, and agreee with you. that is almost a 2X increase in free test, which should definately do something I would think!
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    Quote Originally Posted by swole210
    I would definately think so, and agreee with you. that is almost a 2X increase in free test, which should definately do something I would think!
    Of course it will do something when you double free test! That's how it works. The amazing part is that the estro stays low in spite of the elevated test. That's why it's such a great bridger for PCT. It's almost like cheating, but good for the cardiovascular, prostate, etc. at the same time! This is an awesome product. I was one of the first to alpha test it.
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    Does that make you an alpha male?

    hehe

    I'll give Activate a try next pct. I really seem to have trouble hanging onto gains and my libido really takes a long time to recover after these last few cycles. ATD did seem to help the last pct but if I can make it even better..then why not?


    I may do a Raloxifene/ATD/Activate pCT this time. ALthough Nolva works, it's a little lackluster for me.
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    posted by rrgg over avalabs forum:


    From reading the attached link, SHBG binds to a lot more DHT than testosterone (3.4 times as much). I think this means that when ActivaTe releases bound testosterone, it will also release 3.4 times as much DHT. The article also implies androgenic alopecia can result from low SHBG. Increasing DHT might be great for some, but could be a concern for others.

    ------------------------------------
    rrgg brought up very interesting point. SHGB binding affinty to DHT is highier than testosterone. so nettle roots extract will compete to bind SHBG, which release more free test and DHT."

    So in theory more free test dosnt mean more anabolic effects, unless we found a way to supress DHT levels. maybe nettel with ATD + plant sterols extract will replace excessive DHT and favore more anabolic effect. Otherwise i dont think there is any benifit from taking activate on its own.



    but again Nettle root i used to treat prostate problems so i dont know if has stimulatory effects on free dht.

    I would be interested to see blood work showing DHT levels.
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    Quote Originally Posted by x_muscle
    posted by rrgg over avalabs forum:


    From reading the attached link, SHBG binds to a lot more DHT than testosterone (3.4 times as much). I think this means that when ActivaTe releases bound testosterone, it will also release 3.4 times as much DHT. The article also implies androgenic alopecia can result from low SHBG. Increasing DHT might be great for some, but could be a concern for others.

    ------------------------------------
    rrgg brought up very interesting point. SHGB binding affinty to DHT is highier than testosterone. so nettle roots extract will compete to bind SHBG, which release more free test and DHT."

    So in theory more free test dosnt mean more anabolic effects, unless we found a way to supress DHT levels. maybe nettel with ATD + plant sterols extract will replace excessive DHT and favore more anabolic effect. Otherwise i dont think there is any benifit from taking activate on its own.



    but again Nettle root i used to treat prostate problems so i dont know if has stimulatory effects on free dht.

    I would be interested to see blood work showing DHT levels.
    This is wrong. Nettle root will compete with both DHT and Test for the SHBG. Since DHT has more affinity to SHBG than Test, DHT and nettle root will both "win more" the honor of binding to SHBG while test will have the dirty job of being free to bind with the muscle receptors.
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    Quote Originally Posted by Grunt76
    This is wrong. Nettle root will compete with both DHT and Test for the SHBG. Since DHT has more affinity to SHBG than Test, DHT and nettle root will both "win more" the honor of binding to SHBG while test will have the dirty job of being free to bind with the muscle receptors.

    Well unless we know the ki value or binding affinity values for nettle root and DHT to SHBG,there will be more speculation about this issue.

    Biding proteins will bind to the ligand with highier affinit first, the remaining unbound protein will bind to the lower affinity ligan. Now if neetle root has highier affinity to SHBG than DHT (which we dont know), then more DHT will be released also.
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    Quote Originally Posted by bioman
    Does that make you an alpha male?

    hehe...
    Haha, I guess it does!

    You're gonna love it bro, makes PCT so much smoother and productive. You know mods get the hook-up on new stuff for free, so hit DS up on a PM for some and use it in your next PCT.
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    Quote Originally Posted by x_muscle
    Well unless we know the ki value or binding affinity values for nettle root and DHT to SHBG,there will be more speculation about this issue.

    Biding proteins will bind to the ligand with highier affinit first, the remaining unbound protein will bind to the lower affinity ligan. Now if neetle root has highier affinity to SHBG than DHT (which we dont know), then more DHT will be released also.
    No need to speculate.. DVTHF displaces DHT @ 95% +/- 5%. That means the binding affinity is practically the same. The difference is not statistically significant when calculating effects. It doesn't really matter because the elevated DHT/test will not be able to bind AR's in the prostate and only the test will in muscle. It's all good.
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    Dr.D how about Avena Sativa as a replacement for Nettle Root extract? It seems to have the same propensity for freeing globulin-bound testosterone. In bloodwork people report higher free testosterone & anecdotally they report higher libido and strength especially if used with tribulus.
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    Meowmeow,

    Like you say, the mode of action is very similar with A. Sativa. I think it's more of a quantitative difference. Sativa elevates my libido no doubt (combined with maca, fen and longjack) when used regularly, but it doesn't feel as powerful as nettle. The nettle does it solo. It also kicks in hard after just a few days. It's like comparing tribulus and fenugreek. Tibulus works, just not as thoroughly as fenugreek does. It's the same when comparing AS and ActivaTe. Qualitatively, it is likely superior also, due to it's level of sterols and other constituents that provide additional benefits and synergy to compound the effects.
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    Dr.D do you think increasing free testosterone with Activate post cycle will decrease the amount of off-time needed before entering another cycle?

    To use a prohormone example, I've noticed that some who immediately start a second SD cycle after a short PCT fail to benefit to the degree that they should had they taken more time off. Do you think Activate would increase their second cycle benefit?
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    Quote Originally Posted by meowmeow
    Dr.D do you think increasing free testosterone with Activate post cycle will decrease the amount of off-time needed before entering another cycle?

    To use a prohormone example, I've noticed that some who immediately start a second SD cycle after a short PCT fail to benefit to the degree that they should had they taken more time off. Do you think Activate would increase their second cycle benefit?
    Yes, I do. However, in the case of your example (or any oral), this effect may be less dramatic. I am only talking about decreased time to refreshen the anabolic response to a new cycle. I am not suggesting that liver regeneration and cholesterol metabolism will have necessarily been improved by then. But yes, theoretically you could cheat your PCT with it. You could start 1-2wks before the end of a cycle, go 2-3 more wks, and start a new cycle. This is in the case of an abrupt cycle with no long-chain esters still floating around to complicate the numbers.
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    Dr.D I want to thank you for your response. In the few months I've been on this board you've been very generous with your time and knowledge. You strike me as an intellectually curious guy especially in the area of biochemistry. Just as importantly you try things out for yourself and then you're willing to share your knowledge. Thanks to you my PCT is never toxic to my liver. So I do appreciate you.

    Quote Originally Posted by DR.D
    decreased time to refreshen the anabolic response to a new cycle.
    If you have the time I would appreciate it if you could elaborate on refreshing the anabolic response. Author L. Rea touched on this in his book but I can not find any science to back up his use of controlled catabolism. However as it pertains to increasing free testosterone as we have discussed in this thread there is some science to show an increase in androgen receptors.

    "In fibroblasts cultured from human genital skin which contained very low amounts of 5-alpha reductase, 2 nanomolar tritium-labeled testosterone (free testosterone 40x normal human level) produced a 34% increase in androgen receptors (ARs)as measured by specific AR binding, the best assay method known and 20 nanomolar tritiun-labeled testosterone produced an increase of 64% in number of SRs." - Endocrinology (1990)
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    Did you guys ever see this:

    Gansser D, et al. Plant Constituents Interfering with Human Sex Hormone-binding Globulin. Evaluation of a Test Method and Its Application to Urtica dioica Root Extracts. Z Naturforsch.[C]. 1995;50(1-2):98-104.

    Author: Gansser D, Spiteller G
    Date: 1/1995
    Journal: Z Naturforsch

    A test system is described, which allows the search for compounds interfering with human sex hormone-binding globulin (SHBG) even in complex plant extracts. The method has been evaluated and applied to Urtica dioica root extracts. The lignan secoisolariciresinol (5) as well as a mixture of isomeric (11 E)-9,10,13-trihydroxy-11- octadecenoic and (10 E)-9,12,13-trihydroxy-10-octadecenoic acids (3 and 4, resp.) were demonstrated to reduce binding activity of human SHBG. Methylation of the mixture of 3 and 4 increased its activity about 10-fold.
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    In laymans terms that would be methylation of the Nettle Root BV??
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    Yeah, or at least methylation of some of the constituents in nettle root extract
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    Quote Originally Posted by BigVrunga
    Yeah, or at least methylation of some of the constituents in nettle root extract
    Wouldn't you have to extract a pure sample or synthesize the active from scratch to methylate it like that? If it translated to real world results that'd be an interesting product to use in and of itself, but once you've got the methylation to deal with why not simply do an AAS cycle though, you know? Unless it was for some reason significantly easier on the liver than existing AAS I wouldn't see the point, at least for using it on cycle. For PCT again it'd be interesting but probably only good for transdermal and injectable cycles. The last thing I'd want to do after an oral cycle is take a methylated PCT supplement.
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    Not at methylation correlates to toxicity of the liver.
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    Quote Originally Posted by 3clipseGT
    Not at methylation correlates to toxicity of the liver.
    (at=all) and exactly. Take caffeine for example. Maybe one day, people will understand this.....
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    good info here bros. thanks doc d for breaking out your knowledge.
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    Wouldn't you have to extract a pure sample or synthesize the active from scratch to methylate it like that? If it translated to real world results that'd be an interesting product to use in and of itself, but once you've got the methylation to deal with why not simply do an AAS cycle though, you know? Unless it was for some reason significantly easier on the liver than existing AAS I wouldn't see the point, at least for using it on cycle. For PCT again it'd be interesting but probably only good for transdermal and injectable cycles. The last thing I'd want to do after an oral cycle is take a methylated PCT supplement.
    Yeah, you'd have to isolate those compounds via fractional distillation or something similar. Like mentioned above, not all methylated compounds mean undue liver stress. I just thought it was interesting - something like that could mean a serious boost in test levels when combined with an anti-e like ATD. Especially for an older athlete.

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    Quote Originally Posted by Max32
    (at=all) and exactly. Take caffeine for example. Maybe one day, people will understand this.....

    Hahaha thanks bro for the spelling correction, got a little ahead of myself!

    Yea caffiene was what i was referring too as well.
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    On another note, Alris ATD is methylated as well, i havnt heard anything but im pretty sure that wouldnt cause liver toxicity either would it?

    I mean on the other hand RXT has been noted to negatively effect lipid profiles as well so whats up with alris methylated ATD?
    E-Pharm Rep... PM me with any questions or concerns
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