FormaSurge a lil info on Formestane and Resveratrol

MrKleen73

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This article was written by L. Rea from MesoRX, this guys has experience with all kinds of AAS, research chems and all kinds of stuff that is used in the bodybuilding world. All of his articles are legit, they all have reliable references and have excellent details on what you need to know.


Nothing in this article is intended to take the place of advice from a licensed health professional. Consult a physician before taking any medication.

Q: I already read your awesome book Chemical Muscle Enhancement and ordered your new one Building The Perfect Beast today. Thanks for a no Bullpoo source of in the trenches information!

My question is about anti-estrogens. I read where you said some of them can really shut down IGF-1 in the body. I am pre-contest and need to keep all the muscle I can while cutting the fat. What is the best anti-estrogen and what makes the others good or bad?

A: Thank you for reading CME and I hope that you enjoy Beast. It is always great to know people benefit from my efforts!

Most of the available studies on anti-estrogens (aromatase inhibitors and estrogen receptor antagonist) are performed upon breast cancer patients. As such, to some extent, the results may vary in regard to healthy male athletes. Personally I have always found this boarder-line idiocy due to the fact that there are millions of males with gynecomastia (female dog tits) and corresponding inhibition of HPTA function (the body’s androgen producing system) that would crawl over glass to participate in medical studies of this nature.

A Very Quick Physiology Lesson
The male body uses an enzyme called aromatase to convert a percentage of susceptible androgens into estrogens. Naturally this includes both those the body produces and those introduced from outside the body such as AAS (Anabolic Androgenic Steroids). In most cases the result is predominantly a very powerful estrogen called estradiol.

Aromatase is present in most body tissues and the circulatory system. Unfortunately fat cells produce a scary amount of this man-altering enzyme…which of course explains why fat guys get boobs. (Yikes!)

When we think of aromatase inhibitors we often assume that they are all the same with various levels of results…depending upon dosages. While the latter may be true, the prior statement certainly is not.

Aromatase Inhibitor "Types"?
Let’s do a quick review of the types of aromatase inhibitors that are available. These include type 1, or steroidal inactivators, and type 2, or nonsteroidal inhibitors. The type 1 aromatase inhibitors include exemestane and formestane and are actually androgen analogues (cool stuff if applied right!). The type 2 inhibitors include aminoglutethimide, anastrozole, letrozole, and vorozole.

There are both similarities and differences between the type 1 and 2 aromatase inhibitors. Their similarities include the fact that both inhibit aromatase in a very specific fashion and reduce endogenous or circulating estrogens. On the other hand, the steroidal inhibitors are rather better classified as inactivators, in that they bind to the aromatase molecule in an irreversible fashion (they hold on and do not let go). Because aromatase is rapidly replaced within the body, however, the significance of this property in terms of clinical benefit is unclear in some ways. In addition, the "inactivators" have a structure quite similar to that of androgens and may, in higher doses, have anabolic steroid or androgen-type properties.

Of the type 2 agents, letrozole tends to be more potent than anastrozole and both are more potent than aminoglutethimide in regard to estrogen production. Of the type 1 agents, exemestane is considerably more potent than formestane. But again in each case this may be dose dependant more so than a question of effectiveness of the drug itself. In vivo (tested in live subjects rather than a test tube), the aromatase inhibitors can be graded as shown in the basic table below.

Relative Potency of Type 1 and Type 2 Aromatase Inhibitors

Product Aromatase Inhibition (%) Residual Aromatase (%)
Formestane/
4-Androstenoldione 91.9 8.1
------------------------0---------------------------------------0--------------------------------------0
Aromasin/
Exemestane 97.9 2.1
------------------------0---------------------------------------0--------------------------------------0
Cytadren/
Aminoglutethimide 90.6 9.4
------------------------0---------------------------------------0--------------------------------------0
Arimidex/
Anastrozole 96.7 3.1
------------------------0---------------------------------------0--------------------------------------0
Femara/
Letrozole 98.7 1.3

-----------------------0---------------------------------------0---------------------------------------0

So far it would appear that Letrozole is the leader, huh?

Anti-Estrogens And IGF-1 Production
GH (Growth Hormone) is like a master hormone for tissue growth and fat regulation due to its own intrinsic qualities and its propensity to be converted into or trigger the production and release of Growth Factors. Of these Growth Factors, one of the best known in regard to muscle growth is IGF-1 (Insulin-Like Growth Factor-1).

As most are aware by now, IGF-1 is a powerful anabolic and anti-catabolic hormone. Whether in pre-contest mode or packing on the mass, the amount of circulating and stored IGF-1 an athlete maintains plays a powerful role in the results achieved. Obviously as IGF-1 levels decrease so does the potential for packing on the beef, and the amount of lean tissue lost during calorie-restricted periods increases as well. (Not good)

Estrogen, and more so estradiol, can trigger GH release from the pituitary gland. Aromatase inhibitors decrease the amount of circulating estrogen/estradiol and estrogen receptor antagonist keep estrogen out of the specific pituitary receptors. So in many regards the use of anti-estrogens can effect IGF-1 production and in some cases affect the number of IGF-1 receptors our tissues posses.

Product Effect Percentage
Formestane/
4-Androstenoldione Increases IGF-1 26%
-------------------------0----------------------------------0-----------------------0
Femara/
Letrozol Increases IGF-1 24%
-------------------------0----------------------------------0-----------------------0
Arimidex/
Anastrozole Decreases IGF-1 18%
-------------------------0----------------------------------0-----------------------0
Nolvadex/
Tamoxifen Decreases IGF-1 23.5%
-------------------------0----------------------------------0-----------------------0
Faslodex/
Fulvestrant Decreases IGF-1 70%
-------------------------0----------------------------------0-----------------------0
Cytadren/
Aminoglutethimide Increases IGF-1 27%
-------------------------0----------------------------------0-----------------------0
Aromasin/
Exemestane Increases IGF-1 28%
-------------------------0----------------------------------0-----------------------0

Hmmm, so now we have some major points in favor of Cytadren, Aromasin and Formestane.

Other things to consider pre-contest or simply as a matter of achieving desired results at any point in the pursuit of freak status include…
When attempting to evaluate "the best" choice for any item, the question of specific-intent should come into play first. If you asked for solely my opinion, then I would choose the product that covered the greatest number of needs for specific-intent or goal(s). Personally I prefer Formestane (under whatever name the product is provided, in the purest most active form).

Why?

Formestane ----increases IGF-1 secretion and activity.

Formestane ----decreases the number of progesterone receptors (inhibits the trenbolone and "deca-dick" type side effects and increases fat loss)
Formestane ----inhibits 91.9% of aromatase enzyme production
Formestane ----increases HPTA activity similar to HCG and Clomid together
Formestane ----is anabolic and androgenic (At 500mg weekly the product is similar in effects to 250mg of Primobolan Enanthate)
Formestane ----is a "suicide inhibitor" of aromatase. Specifically this means that it will irreversibly bind to the aromatase enzyme and permanently deactivate it
Formestane ----(The sterile injectable form) possesses a 4-day half-life
Formestane ----decreases SHBG 34% thus increasing androgen activity.
Formestane ----inhibits DHT (dehydrotestosterone) formation and activity.
Formestane ----possesses 1% of the binding affinity of DHT to DHT receptors
Formestane ----has been shown to decrease prostate concerns such as BPH.
Formestane ---- has been shown to continue to increase HPTA function above natural levels even after 22 weeks of continuous administration.
 
MrKleen73

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Reveratrol Benefits

This information copied from http://www.benefits-of-resveratrol.com/benefits-of-resveratrol.html[h=1]The Health Benefits of Resveratrol: Antioxidants Benefits and More[/h]
The health benefits of resveratrol (commonly misspelled reservatrol) can be heard far and wide. 60 Minutes, Barbara Walters, John Hopkins University and the USDA have all reported great benefits from this newly discovered compound. It’s almost common knowledge now that the health benefits of drinking red wine stem from resveratrol, a compound found in the skin of grapes – but what isn’t common knowledge is the specific benefits one gains by consuming resveratrol.
Just recently, in fact, Emma Wightman from the University of Northumbria, discovered that resveratrol helps you think. Seriously. One of the benefits of resveratrol is it helps you think. 24 adults took a series of mental tests before which they were given either resveratrol or a placebo. The results showed significant improvements in cognitive performance in the participants who took resveratrol!
[h=2]The Life Extending Benefits of Resveratrol[/h] The most famous resveratol health benefit, due to 60 Minutes and Barbara Walters is its ability to extend life in mice, yeast and rats – in the laboratory. In addition to extending their lives, the application of resveratrol proved to be an anti-inflammatory, it lowered blood sugar, prevented cancer and other cardiovascular positives. Recently scientists identified the genes they believe to be associated with the length of life. These longevity genes are activated during times of survival and have been labeled sirtuins. Once sirtuins are engaged by the body, they put into action measures to help lengthen life like slowing the metabolism and respiration rate.
Scientists started to look for non-perilous triggers that would activate the sirtuins in the body and discovered Resveratrol to be very effective.
Researchers found that resveratrol could activate the sirtuin in yeast cells and they would live 60 to 80 percent longer. Researchers duplicated their results with mice, which is what spawned 60 Minutes and Barbara Walters Specials.


[h=2]The Antioxidant Benefits of Resveratrol[/h]


Antioxidants are nature's youth protectors. There are lots of things out there that destroy healthy cells. That destruction is what we call aging. Injured skin cells make the skin look leathery and wrinkled. Damaged artery wall cells allow clotting to take hold and begin. The antioxidants are our defense. One of the benefits of resveratrol is that it acts like a true antioxidant. Like antioxidant molecules, resveratrol molecules can donate electrons to unstable free radicals and still remain stable themselves. (Read more about the science of antioxidants).
Resveratrol has been found to be more powerful and effective than Vitamins C and E (the most famous antioxidants). As an antioxidant, Resveratrol inhibits the degredation of lipids and LDL cholesterol – thus resveratrol helps lower the bad cholesterol. And like an antioxidant, resveratrol protects cells from oxidative damage caused by free radicals.
This cellular damage has been implicated in the development of cancer – but is most commonly associated with aging. Damaged cells manifest themselves as aged cells – thus resveratrol prevents the signs of aging and can make you look and feel younger.
[h=2]Anti Cancer Benefits of Resveratrol[/h] Another of the health benefits of resveratrol is its anti-cancer attributes. An ideal anti-cancer compound would naturally adhere to certain properties. It would have to be low-cost and something able to be consumed or applied. It would need to have a high efficacy amongst users and have little to no adverse side effects. Finally, it would need to be presented in a vehicle people were comfortable with and otherwise felt as safe. Resveratrol is this compound.
Resveratrol research has shown resveratrol to induce the deaths of tumor and cancer cells. These effects were confirmed in several in vitro studies, and were successful in every type of human cancer that was tested, including: breast, prostate, esophagal, cervix, ovary, lung and skin cancer. It was also shown to inhibit tumor growth in the development of colon cancer by blocking the building enzyme Cox-2.

Read More on Resveratrol and Cancer!
[h=2]Probiotics Move Over, Resveratrol Can Help[/h] Researchers at Clemson University found that the compounds in grapes, like resveratrol inhibit the bad bacteria growing in your digestive system. Most health practitioners speak of the health benefits of the good bacterias found in yogurt and probiotics, but use drugs to treat the bad. Helicobacter pylori, which you may have heard as H.Plyori, is the main culprit. Using resveratrol to stop the growth of H.plyori could prevent gastritis, and more importantly your body won't become immune to grapes - like it would for drugs.
[h=1]More Fantastic Benefits of Resveratrol[/h] Resveratrol is beneficial in:
  • protecting the central nervous system, by increasing the levels of heme oxygenase (an enzyme known to protect nerve cells) in the brain.
  • regulating hormones
  • acting as blood thinning agent, minimizing the formation of clots and alleviating the damage to blood vessels, and suppressing platelet aggregation.
  • acting as an anti-inflammatory, anti-infective (against fungi and viruses)
  • controlling cravings leading to weight loss
  • shielding against hearing loss
  • increasing and reducing estrogen excess in men (and in women who require aromatase in the treatment of cancer).
  • reducing the risk of Alzheimer’s disease.
 
MrKleen73

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From http://www.ncbi.nlm.nih.gov/pubmed/15795430 PubMed site.

[h=1]trans-Resveratrol, a natural antioxidant from grapes, increases sperm output in healthy rats.[/h]Juan ME, González-Pons E, Munuera T, Ballester J, Rodríguez-Gil JE, Planas JM.
[h=3]Source[/h]Departament de Fisiologia, Facultat de Farmàcia, Universitat de Barcelona, E-08028 Barcelona, Spain.

[h=3]Abstract[/h]trans-Resveratrol was reported to have health benefits including anticarcinogenic effects and protection against cardiovascular disease. One of the mechanisms by which it exerts its action is through modulating the estrogen response systems. Because estrogen is involved in male reproductive biology, we investigated the effect of trans-resveratrol on testis and spermatogenesis. Adult male rats were divided into 2 groups. The treated group was administered by gavage 20 mg/(kg . d) of trans-resveratrol suspended in 10 g/L of carboxymethylcellulose for 90 d, whereas the control group received only carboxymethylcellulose during the same period. The relative weight of testes did not differ between the groups. However, the diameter of the seminiferous tubules was significantly reduced from 437.5 +/- 0.1 mum in the controls to 310.9 +/- 0.1 mum in the resveratrol-treated rats. This decrease was accompanied by a significant increase in tubular density, from 3.20 +/- 0.18 in controls to 6.58 +/- 0.18 tubules/mm(2) in the treated group. Moreover, sperm counts were significantly greater in the resveratrol-treated rats (24.8 +/- 3.30 x 10(7)) than in the control group (14.1 +/- 0.80 x 10(7)), but sperm quality did not differ. Serum concentrations of gonadotrophins and testosterone were significantly higher in the resveratrol-treated group. We identified a novel activity of trans-resveratrol. The daily oral administration of this phytochemical to adult male rats enhanced sperm production by stimulating the hypothalamic-pituitary-gonadal axis, without inducing adverse effects.
 
Celorza

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Formestane ----increases IGF-1 secretion and activity.

Formestane ----decreases the number of progesterone receptors (inhibits the trenbolone and "deca-dick" type side effects and increases fat loss)
Formestane ----inhibits 91.9% of aromatase enzyme production
Formestane ----increases HPTA activity similar to HCG and Clomid together
Formestane ----is anabolic and androgenic (At 500mg weekly the product is similar in effects to 250mg of Primobolan Enanthate)
Formestane ----is a "suicide inhibitor" of aromatase. Specifically this means that it will irreversibly bind to the aromatase enzyme and permanently deactivate it
Formestane ----(The sterile injectable form) possesses a 4-day half-life
Formestane ----decreases SHBG 34% thus increasing androgen activity.
Formestane ----inhibits DHT (dehydrotestosterone) formation and activity.
Formestane ----possesses 1% of the binding affinity of DHT to DHT receptors
Formestane ----has been shown to decrease prostate concerns such as BPH.
Formestane ---- has been shown to continue to increase HPTA function above natural levels even after 22 weeks of continuous administration.


Benefits of this plus Dermacrine please? :D! It is easier to understand with your breakdowns and explanations MrKleen!! :D!
 
MrKleen73

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As you already know DHEA is converts to the androgens, androstenediol, androstenedione and testosterone. The enzymes responsible for this are largely located in the skin and more specifically in the shoulders and upper back. This is why you want to rub Dermacrine on your shoulders and upper back where the highest concentration of the enzymes is in the skin. However it also converts to Estrogen and estrogen like metabolites via another avenue at a decently high rate. Dermacrine already uses Resveratrol, and Chrysine to lower the conversion rate to estrogen to a more balanced level however many people tend to retain water and what not when on Dermacrine due to it's conversion. Simply adding in the FormaSurge will cause a marked increase in not only tightness due to the lack of conversion to estrogen but also the amount of DHEA avaialable to be converted into the more androgenic compounds mentioned above.

So to put it simply the combination would be synergistic, as the FormaSurge would compliment the androgenic effects of Dermacrine while negating any possible negative effects including limiting shut down due to lower estrogen and the SERM like properties of having a high dose of resveratrol between the two products.
 
Celorza

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Thanks brother :) , will be referring to this post for future advice on Forma and Dermacrine :D!
 
oufinny

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As you already know DHEA is converts to the androgens, androstenediol, androstenedione and testosterone. The enzymes responsible for this are largely located in the skin and more specifically in the shoulders and upper back. This is why you want to rub Dermacrine on your shoulders and upper back where the highest concentration of the enzymes is in the skin. However it also converts to Estrogen and estrogen like metabolites via another avenue at a decently high rate. Dermacrine already uses Resveratrol, and Chrysine to lower the conversion rate to estrogen to a more balanced level however many people tend to retain water and what not when on Dermacrine due to it's conversion. Simply adding in the FormaSurge will cause a marked increase in not only tightness due to the lack of conversion to estrogen but also the amount of DHEA avaialable to be converted into the more androgenic compounds mentioned above.

So to put it simply the combination would be synergistic, as the FormaSurge would compliment the androgenic effects of Dermacrine while negating any possible negative effects including limiting shut down due to lower estrogen and the SERM like properties of having a high dose of resveratrol between the two products.
This is about as effective a test boosting stack as you can get in regards to transdermals; you can also replace dermacrine with EndoSurge if you want to only use one topical. Either way, win win for the users. Plus, you can run dermacrine safely for 8 weeks and formasurge you can run at least 8 weeks if not longer.
 
Resolve

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This is about as effective a test boosting stack as you can get in regards to transdermals; you can also replace dermacrine with EndoSurge if you want to only use one topical. Either way, win win for the users. Plus, you can run dermacrine safely for 8 weeks and formasurge you can run at least 8 weeks if not longer.
And Formasurge and Endosurge make a great PCT for Dermacrine too.
 

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Interested in Formasurge and Dermacrine, but I am hesitant on using topicals. Has anyone used these products that also has a family with children? I know it clearly states avoid contact with young children after application so it seems like something for me to avoid. If someone has run these or any other topicals in the same household as children please let me know their regimen and how comfortable they felt doing so. Thank you.
 
MrKleen73

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Interested in Formasurge and Dermacrine, but I am hesitant on using topicals. Has anyone used these products that also has a family with children? I know it clearly states avoid contact with young children after application so it seems like something for me to avoid. If someone has run these or any other topicals in the same household as children please let me know their regimen and how comfortable they felt doing so. Thank you.
I have an 8 year old daughter and here is what I do. I use my formestane products on the spot between my collarbone and my neck where the skin is extremely thin. I do it when I get out of the shower and let it dry for a couple minutes then once dry I put my shirt on and the area it is applied is covered. I also put it on my inner thigh where it is also very thin skin and well my daughter NEVER gets in that area.

The Dermacrine is best on your shoulders, traps and back and if you let it dry then put your shirt on you should be okay. Just be conscious of where you are applying it and that it is covered once dry. After about 5 hours most of everything is soaked into the skin and transfer is extremely unlikely even with skin to skin contact. Other than that make sure to wash your hands after application or even go so far at to apply with rubber gloves then discard the gloves if that makes you feel safer.

My daughter nor wife have ever shown any signs of virilization, or any other effects from either product. Just use your head and keep the areas applied to covered during contact withing the first several hours after application. I would not recommend putting on the forearms if you have small children that you will be playing with unless you always wear long sleeves.
 
oufinny

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I have an 8 year old daughter and here is what I do. I use my formestane products on the spot between my collarbone and my neck where the skin is extremely thin. I do it when I get out of the shower and let it dry for a couple minutes then once dry I put my shirt on and the area it is applied is covered. I also put it on my inner thigh where it is also very thin skin and well my daughter NEVER gets in that area.

The Dermacrine is best on your shoulders, traps and back and if you let it dry then put your shirt on you should be okay. Just be conscious of where you are applying it and that it is covered once dry. After about 5 hours most of everything is soaked into the skin and transfer is extremely unlikely even with skin to skin contact. Other than that make sure to wash your hands after application or even go so far at to apply with rubber gloves then discard the gloves if that makes you feel safer.

My daughter nor wife have ever shown any signs of virilization, or any other effects from either product. Just use your head and keep the areas applied to covered during contact withing the first several hours after application. I would not recommend putting on the forearms if you have small children that you will be playing with unless you always wear long sleeves.
I was just going to say forearm application is out for sure with kiddos. I love that but I have none so its a non-issue for me now. Great recommendations Kleen!
 

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Thank you very much for the detailed response. A lot of supplements tear my stomach up so topicals have greatly interested me as of late and the price for Formasurge and Dermacrine are very appealing.
 
MrKleen73

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Thanks Oufinny, and Paul the products will amaze you. They are much more bioavailable through trandermal use. Please keep us updated if you use them and feel free task any questions you have. We have an extremely good Rep team here.
 

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