The battle of OTC Anti-Estrogens! 6OXO or Formasin??

windwords7

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Formasin(????) Formastane(Bill L.)/4-hydroxyandrostenedione or  6OXO(Patrick Arnold)/3,6,17-androstenetrione

Formasin

<P id=details1>Prototype Nutrition introduces a powerful anti-estrogen to the market in their product Formasin™, which contains the suicide aromatase inhibitor formestane (4-hydroxyandrostenedione). Formestane has been shown to be far more potent than any existing anti-estrogen supplement (5-alpha-androstanedione, chrysin, etc). Formasin™ contains the only active ingredient proven by numerous placebo-controlled human medical studies, which is effective enough to battle breast cancer via perscription in numerous foriegn countries.

<B>Suicide Inhibitor </B>
Formasin works by attaching to the active binding site of the aromatase enzyme, and hence, preventing the receptor from converting other androgens to estrogen. With the aromatase enzyme binding site occupied, the receptor becomes inactive. Because of this, formestane will dramatically suppress estrogen concentrations if it is present in a high enough concetration in the blood. Unlike existing inhibitors, Formasin™ binds permanently with the aromatase enzyme, rendering it useless until the body actually replaces it. Therefore, formestene is called a suicide or irreversible aromatase inhibitor; it also is both highly selective in its action on estrogen and has a long-lasting in effect.

Formestane has successfully treated breast cancer patients in many countries including Germany, England, Switzerland, Australia, Spain,  New Zealand, and Italy. After tamoxifen, an estrogen receptor antagonist, has failed to elicit a positive response, formestane has been shown to be an effective option that produces a response statistically similar to tamoxifen. Now, atheletes who would like to hinder the actions of estrogen can use a substance so powerful that it is often obtained through a prescription.

<B>Dosage and Effects </B>
Peak levels of 4-hydroxyandrostenedione are detected in the blood at approximently an hour and a haf after oral administration, and the substance ellicits a half-life of approximately 3 hours. Because it is an irreversible inhibitor, the estrogen-suppressing activity outlives the actual presence in the bloodstream. It has been shown that maximum estrogen suppression is achieved with an oral dose of only 250mg a day.  An increase in this dose does not cause any significant rise in inhibition.

<B>Estrogen Maintenance In Men </B>
Estrogen increases muscle glucose utilization, supports HDL cholesterol, and even increases androgen receptor concentrations. In contrast to past beliefs, estrogen serves many useful purposes in men and is particularly important in rapid muscle mass gain. Hence, those bulking would not immediately need estrogen maintenance compounds until post-cycle. Aside from the numerous  benefits of estrogen, there still remains a long list of negative effects. Firstly, estrogen increases water retention and fat buildup, which can hide muscle definition. Estrogen can also promote the development of female breast tissue (gynecomastia) in men. When dieting and  cutting are goals, or when there is a potential for gynecomastia development, it is often beneficial to maximize the ratio between androgens and estrogens.

<B>Anabolic Stimulation </B>
Formestane has been shown to be lesser prohormone to the anabolic steroid 4-hydroxytestosterone; aside from aromatase inhibitition, 4-hydroxyandrostenedione also has notable testosterone stimulating properties. Although this conversion rate is low, it is greatly amplified by its ability to inhibit estrogen. By doing so, the testosterone-suppressive signal estrogen sends to your brain is greatly reduced, thus increasing testicular output of testosterone. It has been demostrated by in-vivo human studies  that 4-hydroxyandrostenedione will suppress estrogen levels to such a point that they were not high enough to suppress gonadotropins [1]. An amount of only 250mg to 500mg of formestane injected every 2 weeks, or oral doses as high as 1000mg daily, have not shown any significant testosterone suppressive effect [2]. When given to men in oral doses as high as 500mg, there has been a great  increases in serum testosterone concentrations [3 4 5].

<B>Post-Cycle Estrogen Maintenence </B>
Formasin™ can offer a very unique additional benefit, when used during the recovery window after a cycle of androgens. At this time, one must minimizw post-cycle hypoandrogenic state by restoring the natural production of testosterone. Often, some type of anti-estrogen is used to accomplished the stated task. Since Formasin™ is also converts to 4-hydroxytestosterone, it allows for continued supplementation of androgens during this window, while also suppressing estrogen. Normally, androgens are usually suppressive towards testosterone production. However, with Formasin, its weak androgenic activity is compensated for by its estrogen suppression. Hence, it can basically serve as a small bridge to full testosterone recovery. Other aromatase-inhibitors cannot offer this anabolic stimulation.

<B>Supplement Facts</B>
90 Capsules per Container
Amount per Serving
4-hydroxyandrostenedione 50mg

<B>Directions: </B>
Take 1-5 capsules per day, depending on the level of effect desired. Do not exceed 12 weeks of continuous use. Not recommended for women, especially if pregnant or nursing. Consult your doctor before using if you have or at risk for high blood pressure, heart disease, diabetes or are taking any medications. This product is not intended to treat, cure, prevent or diagnose any disease.

<B>References: </B>
[1] Aromatase inhibitors and hormone-dependent cancers. Brodie AM, Banks PK, Inkster SE, Dowsett M, Coombes RC. J Steroid Biochem Mol Biol 1990 Nov 20;37(3):327-33

[2] Dose-related endocrine effects and pharmacokinetics of oral and intramuscular 4-hydroxyandrostenedione in postmenopausal breast cancer patients. Dowsett M, Cunningham DC et al. Cancer Res 1989 Mar 1;49(5):1306-12

[3] Comparison of the pharmacokinetics and pharmacodynamics of unformulated and formulated 4-hydroxyandrostenedione taken orally by healthy men. Dowsett M, Lloyd P. Cancer Chemother Pharmacol 1990;27(1):67-71

[4] Pharmacokinetics of 4-hydroxyandrostenedione in man after intramuscular injection of different formulations and the effect of this drug on plasma aromatizable androgens and 17beta-estradiol concentrations. Danza G, Muratori M, Guarna A, Occhiato EG, Sadri R, Serio M. J Steroid Biochem Mol Biol 1993 Sep;46(3):373-9

[5] Aromatase inhibition: 4-hydroxyandrostenedione (4-OHA, CGP 32349) in advanced prostatic cancer. Davies JH, Dowsett M, Jacobs S, Coombes RC, Hedley A, Shearer RJ. Br J Cancer 1992 Jul;66(1):139-42
 

windwords7

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Part 2

<DIV align=justify>For athletes familiar with prohormones and steroids, the female hormone estrogen is undoubtedly a familiar enemy. While most of us understand that estrogen is not necessarily always a harmful and worthless substance to men (in the right amounts it is necessary and beneficial), we still are aware that it must be kept under control or some pretty undesirable conditions may arise in the body.
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<DIV align=justify>
<B>The Evils of Estrogen </B>
In males, higher than normal estrogen levels (or estrogen levels that are out of balance with androgen levels) can lead to several physiological disturbances. The most well known estrogen induced malady is, of course, <B>gynecomastia</B> (aka <B>gyno</B> or bitch tits). Gyno, simply put, is the growth of breast tissue in men. Usually gyno is a benign growth that is little more than a cosmetic nuisance, however it occasionally (rarely) can become malignant and lead to male breast cancer. Either way, it is something than definitely is anathema to any guy that takes pride in his physical appearance and musculature. Rock hard pecs topped off with puffy cone shaped girlie lumps are simply not for showing off - at least not in <I>my</I> neighborhood.

High estrogen can also promote excessive water and sodium retention, resulting in a bloated, puffy, and smooth appearance. Steroids that aromatize heavily (such as testosterone and Anadrol) are renowned for putting on lots of bodyweight. However, that body weight usually is in large part estrogen induced water retention, and certainly not all muscle.

If all this is not enough then there is the potent inhibitory effect of estrogen on the hypothalamus, resulting in a shutdown of testicular testosterone production. Science has demonstrated that perhaps the most important regulator of testosterone production in males is estrogen - produced by the conversion of testosterone (and other androgens) to estrogen in the body and the brain. Estrogen sends a signal to the hypothalamus to shut down production of a substance known as <B>GnRH.</B> GnRH is a hormone that stimulates the pituitary to produce <B>luteinizing hormone (LH)</B> which is the signal that tells the testicles to produce testosterone. Therefore, men with elevated estrogen levels will have suppressed testosterone levels and perhaps even atrophied testes. Not a pretty picture, eh?

<B>Controlling estrogen in males </B>
Bodybuilders who use steroids caught on years ago to drugs that control estrogen in the body. The first drugs to be utilized were <B>estrogen receptor antagonists</B> such as tamoxifen and clomiphene. These drugs worked by binding to the estrogen receptor like estrogens do, but unlike estrogens they are unable to translocate to the nucleus and activate estrogen responsive genes. While these drugs are somewhat effective in countering gynecomastia and testicular shut down, they still retain some estrogenic activity in certain tissues such as the liver. The result of this residual estrogenic activity can be a reduction in <B>IGF-1</B> production and an increase in<B> sex hormone binding globulin (SHBG)</B> production. These are both undesirable side effects.

Later on, bodybuilders discovered <B>aromatase inhibitors</B>. These drugs work by blocking the production of estrogens in the body through binding to the enzyme <B>aromatase.</B> Aromatase catalyzes the transformation of aromatizable androgens (i.e. androstenedione, testosterone) into estrogens such as estrone and estradiol. By actually blocking the production of estrogens altogether, aromatase inhibitors do not share the undesirable estrogen agonist activity of estrogen receptor blockers. Instead they function as true anti-estrogens, and because of this have arisen as the most preferred compounds for combating estrogen.

<B>6-OXO™, the first effective all natural aromatase inhibitor </B>
Before I go into detail about 6-OXO™, I would like to give a very brief review and commentary on the current variety of estrogen blocking supplements.

The first estrogen blocking supplement to be introduced, and perhaps the most popular one to date is the isoflavone <B>chrysin</B>. Yes, chrysin has some good in-vitro (“test tube”) research on it that demonstrates it blocks aromatase. However, for years many experts including myself have contended that it suffers from very poor bioavailability, and therefore is ineffective in-vivo. Recently, an article has been published in a very reputable journal that substantiates this suspicion.<!a href="#_edn1" name="_ednref1" title=""> [1][/URL] So chrysin, as promising as it once seemed, unfortunately appears to be a total bust.

After chrysin there was <B>Indole-3-carbinol</B> and <B>Di-indoylmethane</B> . These related compounds work by shifting the metabolism of estrogens away from strong estrogen compounds (16-hydroxylated) and towards weaker estrogens (2-hydroxylated). This can have benefits for women prone to breast cancer as 16-hydroxylated estrogens are quite notorious for promoting estrogen dependent breast cancer. However, there has never been any benefit demonstrated in men for reducing estrogen related effects or for increasing androgen levels. In fact, these compounds may actually REDUCE androgen levels.<!a href="#_edn2" name="_ednref2" title=""> [2][/URL] So for males looking to reduce estrogen and raise testosterone, I-3-C and DIM are poor choices.

In addition to these aforementioned compounds there have been a slew of other compounds sold for estrogen control purposes. These include bioflavonoids such as quercitin, herbs such as Vitex Agnus Castus, and phytochemicals such as resveratrol (3,5,4’-trihydroxystilbene). None of these has ever been substantiated by any research to reduce estrogen levels or to increase testosterone levels.

<B>6-OXO™ </B>
After years of research into natural estrogen blockers I finally discovered a compound that really truly works, in males, to both reduce estrogen and increase testosterone. Its called 6-OXO™, which is short for <B>3,6,17-androstenetrione.</B>

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<DIV align=center><IMG alt="" src="http://www.1fast400.com/store/images/ep-6-oxo1.gif">
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<DIV align=justify>
6-OXO™ is what is known as a <B>suicide inhibitor</B> of aromatase. This means that 6-OXO™ binds to the aromatase enzyme in a permanent and irreversible manner, rendering it inactive. The result of this is an eventual diminishment of aromatase enzyme in the body and a concomitant reduction in estrogen levels.<!a href="#_edn3" name="_ednref3" title=""> [3][/URL] <!a href="#_edn4" name="_ednref4" title="">[4][/URL] <!a href="#_edn5" name="_ednref5" title="">[5][/URL] <!a href="#_edn6" name="_ednref6" title="">[6][/URL] <!a href="#_edn7" name="_ednref7" title="">[7][/URL] A corresponding increase in testosterone production is usually experienced as well.<!a href="#_edn8" name="_ednref8" title="">[8][/URL]

It is important to note here that this deactivation of aromatase enzymes by 6-OXO™ does not mean that your body becomes permanently deficient in the ability to synthesize estrogen. Your body will react to the deficiency of enzyme by producing more enzyme to replace that which has been deactivated. Therefore, when you stop taking 6-OXO™ your aromatase enzyme level will quickly catch up to normal and full estrogen production will resume.


<DIV align=center>
<TABLE id=solidborder cellSpacing=2 cellPadding=2 align=center border=0>
<TBODY>
<TR>
<TD>
<DIV id=details1 align=justify>6-OXO™ is all natural as it is known to be an androgen metabolite formed in the adrenal<!a href="#_edn9" name="_ednref9" title=""> [9][/URL] and placenta<!a href="#_edn10" name="_ednref10" title=""> [10][/URL]</DIV></TD></TR></TBODY></TABLE></DIV>


<DIV align=justify><B>When and how you should use 6-OXO™ </B>
There are two main situations where 6-OXO™ can come in useful. The first situation is in combating estrogen elevation while taking aromatizable prohormones or steroids. Aromatizable prohormones/steroids include testosterone, testosterone precursors (4-androstenedione, 4-androstenediol), nortestosterone, nortestosterone precursors (19-nor-4-androstenedione, 19-nor-4-androstenediol), and synthetic anabolic steroids such as oxymetholone (Anadrol) and methandrostenolone (Dianabol).

The second situation where 6-OXO™ stands very useful is in restoring full endogenous testosterone production after a cycle of prohormones or steroids. Prohormones and steroids act as replacements for natural testosterone, and as a consequence, prolonged usage of these substances results in the body resetting the level of its own natural testosterone production. Your body does this by adjusting the activity of the <B>hypothalamic pituitary testicular axis</B>, or <B>HPTA</B>. The HPTA acts like a thermostat that constantly adjusts the body’s production of testosterone to maintain a certain level in the blood. The <B>hypothalamus</B> is the primary sensor in this system, and it responds to both androgens (i.e. testosterone, DHT) and estrogens (derived from aromatization of androgens). The hypothalamus is so sensitive to estrogens in fact that administration of an estrogen blocker can often result in a very substantial surge in testosterone production. This is why steroid using bodybuilders take products such as <B>Clomiphene</B> (an estrogen receptor antagonist) and <B>Anastrazole</B> (an aromatase inhibitor) after cycles to jump-start their suppressed testicular testosterone production. Now, with the introduction of 6-OXO™, there is a natural - over the counter alternative available to these prescription only drugs.

Okay, am I saying that one has to be a prohormone or steroid user to find 6-OXO™ useful? Certainly not! Even if you never touch prohormones/steroids you can obtain a very substantial and beneficial increase in <I>natural</I> testosterone production by taking nothing but 6-OXO™. For those that are wary of hormonal supplements and their effects on the bodies endocrine balance, yet still want to obtain the benefits of increased testosterone levels, 6-OXO™ offers a very safe and effective alternative.

So how does one use 6-OXO™? If you are using it to combat estrogen during a cycle of aromatizable steroids then you can take it every day of your cycle, once a day (preferably with your evening meal) at a dosage of 200-600 mg. If you are using it to jump-start your testosterone production after a cycle of prohormones (or just to increase your own natural production in a clean state) then you would also take 200-600mg of 6-OXO™ once a day, for a period of 3-6 weeks.

<B>6-OXO™ finally available </B>
As of the writing of this piece, the first batch of 6-OXO™ is being encapsulated. After many trials and tribulations on the manufacturing end (the compound is very difficult and somewhat hazardous to produce) leading to delays in the marketing introduction, we now have enough highly pure product to fill the pipeline.

If you are a prohormone user, or even a steroid user, I doubt I have to entice you anymore than I have to give this stuff a try. The research is solid, and the product is affordable. This is the first new product that Ergopharm has introduced in over a year, and I am sure you will soon discover for yourselves that 6-OXO™ is a product well worth the wait!!

</DIV>
<SMALL><!a href="#_ednref1" name="_edn1" title="">[1][/URL] </SMALL><SMALL>Saarinen N et.al., “No evidence for the in vivo activity of aromatase-inhibiting flavonoids.” J Steroid Biochem Mol Biol. 2001 Sep;78(3):231-9. </SMALL>
<DIV id=edn2><SMALL></SMALL><SMALL><!a href="#_ednref2" name="_edn2" title="">[2][/URL] </SMALL><SMALL>Wilson, V.S., et al., “Alteration in sexually dimorphic testosterone biotransformation profiles as a biomarker of chemically induced androgen disruption in mice.” Environ Health Perspect, 1999. 107(5):377-384. </SMALL></DIV><SMALL><!a href="#_ednref3" name="_edn3" title="">[3][/URL] </SMALL><SMALL>Covey DF, Hood WF, “Enzyme-generated intermediates derived from 4-androstene-3,6,17-trione and 1,4,6-androstatriene-3,17-dione cause a time-dependent decrease in human placental aromatase activity” Endocrinology. 1981 Apr;108(4):1597-9. </SMALL>
<DIV id=edn4><SMALL></SMALL><SMALL><!a href="#_ednref4" name="_edn4" title="">[4][/URL] </SMALL><SMALL>Numazawa M, Mutsumi A, Tachibana M, “Mechanism for aromatase inactivation by a suicide substrate, androst-4-ene-3,6,17-trione. The 4 beta, 5 beta-epoxy-19-oxo derivative as a reactive electrophile irreversibly binding to the active site” Biochem Pharmacol. 1996 Oct 25;52(8):1253-9. </SMALL></DIV>
<DIV id=edn5><SMALL></SMALL><SMALL><!a href="#_ednref5" name="_edn5" title="">[5][/URL] </SMALL><SMALL>Numazawa M, Midzuhashi K, Nagaoka M, “Metabolic aspects of the 1 beta-proton and the 19-methyl group of androst-4-ene-3,6,17-trione during aromatization by placental microsomes and inactivation of aromatase” Biochem Pharmacol. 1994 Feb 11;47(4):717-26. </SMALL></DIV>
<DIV id=edn6><SMALL></SMALL><SMALL><!a href="#_ednref6" name="_edn6" title="">[6][/URL] </SMALL><SMALL>Numazawa M, Tsuji M, Mutsumi A, “Studies on aromatase inhibition with 4-androstene-3,6,17-trione: its 3 beta-reduction and time-dependent irreversible binding to aromatase with human placental microsomes”.J Steroid Biochem. 1987 Sep;28(3):337-44. </SMALL></DIV>
<DIV id=edn7><SMALL></SMALL><SMALL><!a href="#_ednref7" name="_edn7" title="">[7][/URL] </SMALL><SMALL>Marsh DA, Brodie HJ, Garrett W, Tsai-Morris CH, Brodie AM, “Aromatase inhibitors. Synthesis and biological activity of androstenedione derivatives” J Med Chem. 1985 Jun;28(6):788-95. </SMALL></DIV>
<DIV id=edn8><SMALL></SMALL><SMALL><!a href="#_ednref8" name="_edn8" title="">[8][/URL] </SMALL><SMALL>Booth JE “Effects of the aromatization inhibitor androst-4-ene-3,6,17-trione on sexual differentiation induced by testosterone in the neonatally castrated rat” J Endocrinol. 1978 Oct;79(1):69-76. </SMALL></DIV>
<DIV id=edn9><SMALL></SMALL><SMALL><!a href="#_ednref9" name="_edn9" title="">[9][/URL] </SMALL><SMALL>Levy H et.al, “The inhibition by metopirone of 11beta and 19-hydroxylations of androst-4-ene-3,17-dione in bovine adrenal perfusion” Steroids. 1965; 5:479-493 </SMALL></DIV>
<DIV id=edn10><SMALL><!a href="#_ednref10" name="_edn10" title="">[10][/URL] </SMALL><SMALL>Tan L et al., “De novo biosynthesis of 6 beta-hydroperoxyandrostenedione in human placental microsomes.” Biochem Biophys Res Commun. 1984 Feb 14;118(3):805-13.</SMALL> </DIV></DIV>
 

windwords7

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Let's get some good conversation going on this subject bros!
 
pogue

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1-5 capsules per day? That's kind of an odd suggested serving.

Can someone look up the studies and see how much was used per serving in the studies?


Also what is 4-hydroxytestosterone? What steroid is that?

It looks to be cheaper than 6oxo from 1fast, I guess we'll have to see how it pans out.

Here's a discussion on Avant about it:

http://forum.mindandmuscle.net/index.php?act=ST&f=12&t=1371&st=0
 
wojo

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OK I THINK ON MOLECULARNUTRITION.NET THE DOSE LISTED IN THE STUDIES IS 250 MGS..WHICH WOULD BE 5 CAPS
 

windwords7

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In both of these kind of supps you only take once a day wich intrigues me but apparently they are so effective that it'a all you need to do.
 
wojo

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Dose and Pharmacokinetics

After oral administration peak levels of 4-hydroxyandrostenedione are reached in the blood at approximately 1.5 hours , and the drug is cleared from the body with a half-life of approximately 3 hours . Due to its nature as an irreversible inhibitor, its estrogen-suppressing activity outlives it actual active lifespan in the bloodstream. Studies have demonstrated that maximum estrogen suppression is achieved with an oral dose of only 250mg per day12 . Doubling this dose to 500mg, or even quadrupling it to 1000mg, was shown to have no effect on aromatase inhibition or estrogen levels appreciably different from the 250mg dose.

http://www.molecularnutrition.net/formastat.htm
 

windwords7

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Originally posted by wojo
Dose and Pharmacokinetics

After oral administration peak levels of 4-hydroxyandrostenedione are reached in the blood at approximately 1.5 hours , and the drug is cleared from the body with a half-life of approximately 3 hours . Due to its nature as an irreversible inhibitor, its estrogen-suppressing activity outlives it actual active lifespan in the bloodstream. Studies have demonstrated that maximum estrogen suppression is achieved with an oral dose of only 250mg per day12 . Doubling this dose to 500mg, or even quadrupling it to 1000mg, was shown to have no effect on aromatase inhibition or estrogen levels appreciably different from the 250mg dose.
 

Good Stuff bro! Karma for you!
 

bpdaddy

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Who the heck is Protype Nutrition?

I can't say which is better, nor can anyone else at this point.  Until there is feedback it all here say on Formastain.  We all knowthat 6OXO works.

I agree Formastatain looks like a better anti-e, but it's all about T recovery!
 

Aztec42

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Prototype Nutrition is Pat Arnold's new company. Him and Bill L. are fighting about it on BB.com
 

windwords7

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Originally posted by bpdaddy
Who the heck is Protype Nutrition?

I can't say which is better, nor can anyone else at this point.  Until there is feedback it all here say on Formastain.  We all knowthat 6OXO works.

I agree Formastatain looks like a better anti-e, but it's all about T recovery!
 

Were not trying to decide which is "better" really. One will be better than the other depending on the circumstance IMO. But I would like to have some good discussion about it. There are some cases that can be made that one is better overall but we will see. I cant wait to see what kind of testimonies we get from the 4HYD.
 
Supa Freek 420

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There was a great discussion about this a month or so back between Bill and Pat over at bb.com. Remember it Jake? :)

I'll try to dig up the link.
 

bpdaddy

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  1. ergopharm
  2. supertech
  3. LPJ
  4. Prototype
Anymore this guy deals in?
 

1Fast400

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PA has nothing to do with Supertech. Supertech just buys the raws of 1-AD from them. Just like HDT used to do.
 

bpdaddy

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Originally posted by 1Fast400
PA has nothing to do with Supertech. Supertech just buys the raws of 1-AD from them. Just like HDT used to do.
 

HDT :eek:
 
thundergod

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Windwords7--- I see you criticize resveratrol as being ineffective. Then you praise 6-oxo. Don't you know that 6-oxo extreme has it in it?? Surprised? I am!!! It looks like ergopharm thinks it is effective as an anti-e. I agree with ergopharm.
 
john123131

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Windwords7--- I see you criticize resveratrol as being ineffective. Then you praise 6-oxo. Don't you know that 6-oxo extreme has it in it?? Surprised? I am!!! It looks like ergopharm thinks it is effective as an anti-e. I agree with ergopharm.
dude this thread is 5 years old..lol...there was no 6 oxo extreme back then brah.
 

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