Primobolan Information
Primobolon

Understanding Primobolan

At first glance, the term Steroidal Aromatase Inhibitor sounds like a complex trio of words describing some powerful pharmaceutical agent or enzymatic process. In reality, it merely represents a group of hormonal related compounds that inhibits the enzyme in the human body responsible for the conversion of male hormones into female hormones. More specifically, it inhibits whats called the aromatase enzyme, which converts androgens into estrogens. The normal metabolism of male androgens includes two main byproducts, female estrogens and male dihydrotestosterone (DHT).


If androgen metabolism is functioning normally, why would we want to inhibit the enzyme responsible for this function? The reason is that, under certain circumstances the body can produce too much estrogen or DHT, which can lead to a number of negative side effects. These side effects include decreased natural testosterone production, reduced sperm count, loss of muscle mass, and decreased strength.



Unique Functions


Steroidal aromatase inhibitors are compounds that decrease estrogen and DHT while at the same time producing a signal that stimulates natural androgen production. Thats right, they increase (natural) total and free testosterone concentrations by decreasing estrogen and DHT. Keep in mind that, not all steroidal aromatase inhibitors decrease DHT, but they all attempt to decrease total circulating estrogen levels.


Primobolan does not need to directly convert into another hormone in order to be active. It is active in its initial state. It simply stimulates the body to produce more total and active testosterone. It does this by promoting luteinizing hormone (LH) and decreasing (SHBG) in order to increase natural production of testosterone while simultaneously increasing free or active testosterone. Keep in mind that other pro steroids only convert into a form of testosterone, which can shut down natural testosterone production and they do not increase both natural total and free testosterone levels. Now while Primobolans dual effects are super charging your natural testosterone production, it is also decreasing female estrogen and androgenic DHT levels. Thats why Primobolan is a must for those on andro or steroids.






Quest For The Best Chemical Variation Of Steroidal Aromatase Inhibitors.

There are several different chemical variations of steroidal aromatase inhibitors. Some of these androstene related compounds are patented by pharmaceutical companies and more recently by supplement companies. The most familiar pharmaceutical aromatase inhibitor has been shown to increase androgen levels in males.


Sounds great, right, well thats what a supplement company thought when it planned to release this compound until it found that was patented by pharmaceutical giant Schering and then decided to drop it. The only other known aromatase inhibitor currently on the dietary supplement market is 5a-androstanedione. Now while this compound can inhibit estrogen biosynthesis it does not decrease DHT in fact, it has a weak conversion into DHT and it does not support natural testosterone production. Therefore this leaves Primobolan in a class of its own.

Benefits of Sports Nutrition Enthusiasts



The Sports Nutrition market should benefit the most from this type of compound. Serious and weekend athletes could receive increased muscle mass, recovery, strength and decreased body fat. Natural increases in total and free testosterone concentrations while simultaneously decreasing estrogen and DHT make this the single most important ergogenic compound in an athletes arsenal. The weekend athlete can effectively utilize these compounds in conjunction with creatine and protein in order to improve their physiques and or performance. The serious athlete may do the same or use these compounds in conjunction with other performance enhancing compounds. The serious athlete could also use some of these compounds to jump start natural androgen production after a cycle of anabolic steroids. Anabolic steroids tend to shut down natural androgen production and increase estrogen levels, which can cause an androgen deficiency. Steroidal aromatase inhibitors could be used to counter these negative side effects. Bodybuilders use drugs like Clomiphene citrate (Clomid) in order block estrogen absorption and increase natural androgen production, but this is a powerful prescription pharmaceutical with its own set of side effects.


So where can you find some of these legal compounds that lower both estrogen and DHT while increasing natural androgen production? The compound is currently referred to as Primobolan. It is an analog or derivative of a naturally occurring compound. It exerts all of the previously mentioned positive benefits associated with steroidal aromatase inhibitors and provides a mild anabolic effect without leaving banned metabolites in the system!


In The Raw
by Sal Abraham M.S. R.D. L.D.N.

Primobolan acetate orals Patent Pending

(4-Androsten-4-ol-3,17-dione Acetate)

(4-HydroxyAndrostene-3, 17-dione acetate)
(4-OHAA)

Novel Compound


What if I was to tell you that I know of a compound that can dramatically increase natural production of total and free testosterone while simultaneously inhibiting estrogen and DHT formation? Dare I say a good for you steroid? Lets see, a steroid that has all of the positive strength and muscle building effects of

testosterone but none of the negative side effects associated with androgen metabolites. Sounds too good to be true, right? Wrong!! Now while some steroids and pro-steroids are designed to produce less estrogen and DHT, they still do and can produce significant amounts of estrogen if taken in excess. This new compound raises testosterone by decreasing estrogen levels and longer you take it the better it works. This is truly the next great breakthrough in legal supplemental hormones.



Orally Active Pro-Steroid Or Steroid?

To my surprise, this hormonal analog doesnt convert or change into another hormone in order to be active. In other words, this compounds potency is not limited to the amount of liver converting enzyme found in the body. It is active in its original form. There are methods to modify the base compound such as the chemical addition of ethers and esters. The addition of an acetate ester was utilized for this compound since acetate and deconate esters have been shown to enhance oral absorption of certain compounds.




Similar Concept but Real World Results.

This might sound somewhat similar to an old concept once described by Dan Duchaine with a little well known compound Flavone X (Chrysin). Although, Chrysin (plant aromatase) never panned out because it had almost zero oral bioavailability and was only a mild aromatase inhibitor. To be honest this is probably a bad example since Chrysin doesnt even come close in action to this new compound. Chrysin was thought to only shift the estrogen testosterone ratio slightly in favor of testosterone. This new compound dramatically inhibits estrogen formation and also stimulates the production of total and free testosterone, not just shifting the ratio.





New Class - Steroidal Aromatase Inhibitors



If you take this same concept with an orally bioavailable compound, lets say a Steroidal aromatase inhibitor with very potent aromatase inhibition, then you start to see real world results. Steroidal aromatase inhibitors are a class of steroidal nutrients that have been shown to inhibit estrogen formation and stimulate androgens or natural production of total and free testosterone levels in males. 3,4




Total and Free Testosterone


Just in case youre not familiar with the terms Total and Free testosterone I will briefly explain their relevancy. Testosterone and dihydrotestosterone (DHT) circulate in plasma either unbound (free approximately 2 - 3%) or bound to plasma proteins. 5 The binding proteins include sex hormone-binding globulin (SHBG) and albumin. SHBG is a -globulin that has a low capacity for steroids, but binds with high affinity. SHBG has its highest affinity for DHT and its lowest affinity for estradiol. In men, circulating testosterone is bound 44-65% to SHBG and 33-54% to albumin, whereas in women, testosterone is bound 66-78% to SHBG and 20-32% to albumin.Blood testosterone levels are dependent on many different factors. In aging men, total serum testosterone is often normal while free testosterone or bioavailable testosterone is low. Because SHBG is often low in women with hirsutism, free testosterone is elevated while the total testosterone concentration is normal. This means the free testosterone portion is responsible for muscle mass, strength, recovery and male characteristics. Just an increase in free testosterone with no increase in total testosterone can produce significant results. So raising both total and free testosterone should result in dramatic effects.







People who can Benefit



Who can benefit from this product? Well the main groups of individuals who will benefit the most are 1) anyone using prohormones, 2) anyone using steroids, and 3) anyone who doesnt use prohormones or steroids. Did I miss anyone? Anyway, people using this new compound in conjunction with prohormones would receive much greater benefits, as compared to using prohormones by themselves, due to the increase in natural testosterone production coupled with the synthetic conversion of the prohormone. There would then be no concern over estrogen accumulation resulting in harder gains. As a result, natural testosterone production would not shut off. Lastly it has been shown that this compound has the ability to increase the amount of liver enzyme responsible for the conversion of prohormones. 6 This means you get a greater amount of testosterone or nor-testosterone prohormone conversion resulting in greater gains. Steroid users would receive the same benefits but on a somewhat larger scale since, side effects are more prevalent with actual steroids. So the anabolic pharmaceutical user could take this in an attempt to prevent testicular shut down, prevent an accumulation of estrogen, inhibit DHT formation, and to solidify any gains from the steroids due to no hormonal drop in natural testosterone after the cycle.



The non-prohormone or non-steroid user can also receive great benefits from this compound. The inhibition of estrogen formation and the stimulation of total and free testosterone can impart extensive physique altering benefits. This hormonal alteration can promote solid gains in muscle mass and strength. The inhibition of estrogen biosynthesis would provide a decrease in excess extra cellular water and promote a better environment for fat burning. The stimulation of total and free testosterone promotes muscle mass, strength, and recovery. This is due to the fact that testosterone output is now greater with a higher free or active portion of testosterone.




Metabolism

Another interesting note is that this new compound does not break down into banned substances or metabolites. One of the metabolites is the direct 4-O-glucuronide. The other two represent 3-O-sulfates of the exocons 3beta,4beta-dihydroxy-5alpha-androstane-17-one and 3alpha,4beta-dihydroxy-5alpha-androstane-17-one, their ratio being 7:3. These exocons are formed by stereoselective 3-keto reduction, accompanied by reduction of the 4,5-enol function. 7 Now while the actual compound does not metabolize into a banned substance, the natural increase of total testosterone could cause a positive test result. So it would be probably wise to stop taking the product at least 2-4 weeks prior to testing in order to bring testosterone levels back to normal.



Chemical & Physiological Info



Figure 1



The chemical term 4-Androsten-4-ol-3,17-dione acetate refers to the isomer:
4-Androsten-4-ol-3beta,17beta-dione Acetate. 4-Androsten-4-ol-3,17-dione acetate is an analog or derivative of the naturally occurring precursor hormone 4- Androstenedione. 2 4-Androsten-4-ol-3, 17-dione acetate is a steroidal aromatase inhibitor that inhibits estrogen biosynthesis, stimulates natural production of total and free testosterone, and may inhibit DHT formation. 8, 9 It does this by inhibiting the Cytochrone P-450 enzyme which converts testosterone to estrogen. Once estrogen levels fall a signal is sent to the hypothalamic pituitary axis to produce (LH) luteinizing hormone and decrease (SHBG) steroid hormone binding globulin. LH then stimulates the testes to increase total testosterone production, in which a large portion is free or active testosterone due to the decrease in SHBG. This elevated amount of testosterone is then metabolized with less estrogen and DHT conversion. The total estrogen conversion is decreased by the aromatase mechanism while the DHT inhibition is site specific. It appears that the 5-alpha reductase isoenzymes are inhibited resulting in less DHT formation from testosterone. Another interesting note is the ability of 4-Androsten-4-ol-3, 17-dione acetate to directly stimulate testosterone whether in the presence of LH or not. Researchers examined the effects of placebo, luteinizing hormone (LH), 4-acetoxy-4-androstenedione, and luteinizing hormone (LH) plus 4-acetoxy-4-androstenedione on rat follicles in vitro. In regards to testosterone they found that within the first 8 hours 4-acetoxy-4-androstenedione had the ability to directly stimulate testosterone alone and greatly stimulate testosterone in combination with luteinizing hormone (LH). Interestingly enough within the next 16 hours they discovered 4-acetoxy-4-androstenedione alone was stimulating testosterone 3 times as much as luteinizing hormone (LH) while the combination also continued to stimulate testosterone. 10



Patent Info

This new compound is currently patent pending at the United States Patent & Trademark Office. This invention relates to a method of administering ether and ester derivatives of 4-Androsten-4-ol-3,17-dione. The oral daily doses can be between 20 to 1000mg, but preferably 100 to 600mg. The preferred daily dosing schedule should be divided into 3-6 sub dose applications per day in order maintain adequate blood hormone concentrations. 11 This compound is currently provided by Promatrix . Which is an international joint venture between well established pharmaceutical companies, home and abroad.

Summary

In summary, this new patent pending compound is truly an essential supplement for anyone concerned
with physique, strength, and recovery and libido enhancements. It is a must use product for several population segments including: 1) anyone using prohormones, 2) anyone using steroids, and 3) anyone who doesnt use prohormones or steroids. Its orally bioavailable with no down regulation. This means no cycling is required and long term use is recommended. This compound is a naturally occurring hormonal analog that stimulates natural production of total and free testosterone while simultaneously inhibiting estrogen formation.

Primobolan

*These statements about Primobolan have not been evaluated by the Food and Drug Administration. Primobolan is not intended to diagnose, treat, cure, or prevent any disease.