In Pursuit of the Holy Grail

You are about to be introduced to the future of prohormones. It is called 1-AD, and it is without a doubt the single most amazing prohormone to be synthesized and sold as a nutritional supplement.

For the past 18 months Patrick Anold has been feverishly working — almost exclusively — on one project. While scores of less knowledgeable people in the industry periodically made occasional lame, foul ball attempts at finding the “latest, greatest” prohormone, Patrick kept quiet and worked on the development of what essentially could be called the “holy grail” of prohormones.

Patrick wanted this prohormone to have all the attributes most critical to the perfect prohormone. It had to be:

• Orally Active
  
• Completely Non-Aromatizable to Estrogens
  
• Extremely potent
  
• Naturally occurring
  
• Non-toxic

After months of scouring every book and journal he could locate, including those in foreign languages (i.e. German), Patrick discovered a compound that seemed to be the perfect candidate. That was the easy part. It then took Patrick almost one whole year to figure out how to manufacture the compound cheaply enough for sale as a supplement. Patrick’s lab took on the appearance of ground zero at Hiroshima as he endlessly did reaction after reaction in pursuit of the perfect manufacturing recipe.

We understand that not everyone buying our products has a chemistry or biology degree, but we do know that people appreciate being treated with respect and honesty. They want to know they are being told the straight story, even if they don’t have the background to understand every facet of the presentation.

Introducing 1-AD

It’s time to introduce what Patrick refers to as “the crown achievement” of his career. The formal chemical name of the compound Patrick developed is 1-androstene-3beta, 17beta-diol. We nicknamed this compound “1-AD” which is a shortened acronym of its chemical name. Its chemical structure is shown here.

This compound is truly unique amongst other prohormones in a variety of ways. Let’s look specifically at 1-AD and what it does.

The Power of 1-Testosterone

You probably are familiar with the “Andro” prohormones, and the “Norandro” prohormones. The former convert to testosterone and the latter to 19-nortestosterone. 1-AD, however, does not fit into either of those categories. That is because 1-AD converts to a relatively unheard of hormone called 1-testosterone. 1-testosterone is what is known as a “double bond isomer” of testosterone.

Although chemically the only difference between testosterone and 1-testosterone is the position of the double bond, pharmacologically the two products are quite different. According to research done by the pharmaceutical giant G.D. Searle and published in the 1960s, 1-testosterone is over 7 times as myotrophic (anabolic) as testosterone(1). That makes 1-testosterone a phenomenally potent compound, surpassing even most synthetic anabolic steroids.

No Aromatization

1-testosterone differs from testosterone in another way as well. Being a 5alpha-reduced androgen (a DHT derivative) it simply cannot aromatize to estrogens. The same goes for 1-AD itself — no estrogen transformation can occur. This makes 1-AD unique compared to other prohormones — all of which can either aromatize directly, convert to a product that aromatizes, or both. So what does this mean in the real world? It means that your chances of getting gynecomastia (bitch tits) from 1-AD is essentially zero, and that water retention side effects are vastly reduced compared to other prohormones.

The Only Truly “Orally Active” Prohormone

Natural androgenic steroids are normally not very active orally. Large amounts have to be taken orally to see biological effects. This is because the first pass through the liver causes a massive deactivation of the compounds, primarily through the oxidation of the 17beta-hydroxyl to a 17-keto group. Chemists long ago found that by adding an alkyl (methyl or ethyl) chemical group to the alpha position of the 17 carbon, this oxidation can be prevented. However, this alkyl derivatization also greatly increases the liver toxicity. Therefore the usage of such synthetically altered compounds (methyltestosterone, oxymetholone, stanozolol) are not without substantial risk.

Luckily, there are other ways to render a steroid orally active, and do so without making the compound toxic to the liver. Certain structural modifications can alter the metabolism of steroids making them resistant to liver breakdown. One of these modifications is unsaturation (presence of a double bond) in the 1-position. One steroid that has this structural modification and is orally active is the anabolic steroid Methenolone, also known as Primobolan.

As you may have noticed, this double bond position that makes Primobolan orally active is the same one found in 1-AD, which, by the way, is also orally active. Steroids with this particular double bond characteristic are known as 1-dehydroandrostanes.

During the 60’s and 70’s some papers were published describing the phenomenon of oral activity seen with 1-dehydroandrostanes, including 1-testosterone and 1-AD. What was discovered was that these compounds resist metabolic deactivation by profoundly shifting what is known as the “17-keto redox potential” towards the formation of active 17beta-hydroxyl steroids(2,3). What does this mean? It means that when you take 1-AD, the liver serves primarily to activate the compound, rather than break it down and excrete it as it does with other prohormones and testosterone. It means that 1-AD is “orally active,” yet it does not impart the liver toxicity that 17alpha-alkylation does.

A Natural Hormone Made in the Body

One of the beautiful things about 1-AD is that in addition to its impressive pharmacological activity, it is also a natural androgen made in the human body(4) . This means that it is not foreign to your body, and that it can legally and openly be sold as a nutritional supplement. Furthermore, 1-AD’s high rate of active conversion after oral administration is not just a theory, it has been demonstrated and published in a highly reputable peer reviewed journal.

Summary

Let’s put it all together and see what 1-AD has to offer:

• High oral activity
  
• Conversion to a hormone 700% more potent than testosterone
  
• Absolutely NO aromatization to estrogens
  
• Natural and safe
  

There can be no argument that this is the ultimate prohormone. Believe us, there simply are no natural compounds out there that can come close to what 1-AD does, so don’t even bother looking.

1-AD FREQUENTLY ASKED QUESTIONS (FAQ)

What do you mean specifically when you say that 1-AD converts to a hormone that is over 7 times as anabolic as testosterone?

1-AD converts to an isomer of testosterone known as 1-testosterone. The anabolic potency of 1-testosterone and testosterone were determined (Counsel et al., Anabolic Agents. Derivatives of 5alpha-Androst-1-ene, J. Org. Chem., 27 (1962), 248-251) by the rat levator ani assay, which is the way that steroids have traditionally been tested for muscular anabolic activity.

In this study, testosterone was assigned a myotrophic potency of 26, while 1-testosterone was given a myotrophic potency of 200. These potencies were determined by measuring the minimal doses from which significant increases in muscle weight were observed. It took over 7 times LESS 1-testosterone than testosterone to produce the same increases in muscle weight.

To sum it up, this means that it should take much less 1-AD to stimulate your muscles to grow than with a testosterone precursor like 4-androdiol (4-AD) — and this is without taking into consideration 1-AD’s oral bioavailabilty advantage over traditional prohormones.

1-AD sounds good in that it doesn’t convert to estrogen, but what about DHT? Is this going to have the same effects as Andro on my prostate?

While 1-testosterone can convert to DHT through an unusual pathway, the extent of that conversion is unknown. The extent of 1-tesotsterone’s impact on the human prostate is unknown as well. According to assays on rats, prostate growth is similar to that with an equal dose of testosterone. But this is in castrate rats that have underdeveloped prostate glands to begin with. This kind of prostate growth (developmental growth) is in no way the same thing as benign prostate hypertrophy (BPH), the kind that can be damaging in humans.

Since BPH is estrogen dependent, there is a possibility that 1-AD is in fact very prostate friendly. In case you do not know, DHT given by itself can actually reduce BPH because it reduces serum estrogen (US patent# 5,648,350, Dihydrotestosterone for use in androgenotherapy). The same may be true for 1-AD — at this point we don't really know.

Are you saying that 1-AD is as potent as trenbolone?

I said that 1-AD’s effects were qualitatively similar to trenbolone’s. Unfortunately I assumed that everyone understood what the term qualitative means. I meant to express that 1-AD’s effects are of the same type and character as trenbolone (i.e. increased strength, increased hardness, low water retention). This does not mean that it is just as potent ‘milligram per milligram”. By the way, for those who are not familiar with trenbolone, it is a very potent anabolic steroid primarily used today to beef up cattle. Trenbolone was at one time a popular pre-contest anabolic agent used by bodybuilders.

I know you say that a lot of this makes it past the liver, can you give a rough percent?

All I can say is that more gets through than for other prohormones. I base this on data examining the recovery of active 17-beta hydroxy steroids from the urine of subjects given various steroids including 1-AD (Galletti and Gardi, Metabolism of 1-Dehydroandrostanes in Man, J Steroid Biochem, 3 (1972), 933-936).

Currently there is insufficient evidence to estimate the percentage that makes it into the bloodstream however. We can just say that it is considerably more than other prohormones.

Is there going to be a spray version or an intra-oral version of 1-AD? I like the sprays because they’re timed released.

1-AD is going to only be sold orally for now. It has slight irritant properties on the skin and mucous membranes that make it poorly suited for topical spray or intra-oral applications.

What do you mean specifically that 1-AD is not outstanding for mass gains?
1-AD can put bodyweight on you, but if you compare the strength and pure muscle gains to the overall bodyweight increase it is less than what you would see associated with an aromatizing steroid like testosterone (for the same given amount of strength and pure muscle gains). This is because the mass gains seen with 1-AD are not associated with water retention.

This is considered by many to be a very desirable property in an anabolic agent. It is for this reason that strong anabolic steroids such as Trenbolone, Halotestin, and Winstrol are so treasured for pre-contest usage. These steroids are not noted for promoting great body weight increases, but they increase pure muscle mass considerably and without definition-obscuring water.

Would 1-AD be a good product to use for losing fat or cutting up?? I assume it would be anabolic enough to counteract some of the catabolic effects of an aggressive dieting program.

1-AD can be extremely useful for cutting up, and this is probably its most valuable use. While 1-AD will not impart any direct fat burning effects like you would get from a thermogenic product, it can assist in losing fat indirectly. 1-AD can minimize the loss of lean body mass (LBM) while dieting, aiding in the maintenance of a high basal metabolic rate.

While all prohormones can help maintain LBM, most of them also convert to estrogens. Estrogens promote fat gain and therefore their elevation is counterproductive while dieting. 1-AD does not increase estrogen levels making it a superb prohormone choice for cutting-up.

Furthermore, since 1-AD has little associated water retention, your muscle definition will not be adversely affected. You will maintain a lean, hard look to your physique.

What about stacking 1-AD with other types of prohormones? Is this advisable? Would this help mass gains??
Stacking 1-AD with 4-AD (Androdiol®) or nor-4-AD (Norandrodiol®) prohormone products can be of value. You can get the mass gain benefits of the diol prohormones combined with the strength benefits of 1-AD.

In particular, stacking 1-AD with one of the topical spray prohormone products should be very effective. Such a stack would include a sustained release component with an oral, fast acting component. This would be pharmacokinetically similar to a traditional “injectable/oral stack”.

Can women take 1-AD?

1-AD is significantly androgenic, which means that it will put women at risk for virilizing effects much more so than a low virilizing product such as Norandrodiol®. For that reason, it would probably be advisable for most women to avoid 1-AD. Some women may be able to tolerate one capsule a day perhaps, but certainly for the majority of women it is just a better idea to take a Norandrodiol product.

What can you tell me about the prohormone 5alpha-androstandiol? It is supposed to be a Masteron precursor. Is this the same thing as 1-AD?

No. This is certainly not the same thing as 1-AD. 5alpha-androstandiol (I will call it 5-AA) is the 5alpha-reduced version of 4-AD (4-Androstenediol or Androdiol). It is produced by the catalytic hydrogenation of the prohormone 5-AD (5-androstenediol). As a result, it is quite inexpensive to manufacture. The retail price of the stuff unfortunately does not reflect this however.

In the body, 5-AA is supposed to convert to DHT. It does NOT convert to Dromostanolone (Masteron). Masteron is 2alpha-methyl DHT. There is no 2alpha methyl group on 5-AA. Now if they made a 2methyl-5-AA, then they could claim it's a Masteron precursor. But that would not be a nutritional supplement now would it? Anyway, I digress. The point is that this prohormone only converts to plain old DHT.

Anabolically speaking, DHT simply cannot be compared to Masteron, or any other DHT derivative (winstrol, anadrol) for that matter. DHT has relatively slight anabolic activity compared to these compounds because of its quick breakdown by 3alpha-hydroxysteroid dehydrogenase in the muscle. Synthetic derivatives of DHT on the other hand are resistant to this breakdown, so they are able to bind and activate androgen receptors in the muscle.

Let's not write off DHT however. DHT has positive effects on the central nervous system, which lead to increased neurological efficiency (strength), and increased resistance to psychological and physical stress - not to mention optimal sexual function and libido.

But just how good a precursor to DHT is 5-AA? To tell you the truth, I scoured the literature thoroughly all the way back to the 1930's and could not find any studies that quantified this. 5-AA definitely should convert to DHT because there is a pathway in the body, however, there is no direct research that indicates the extent to which this happens.

What there is data on are the effects of 5-AA on androgen dependent organs. DHT is a very active androgen, so the influence of 5-AA on androgen dependent organs should give a decent indication of whether a lot of 5-AA is being converted or not.

Ruzicka et.al. found that its activity in the capon comb test was approximately 35 times less than that of testosterone (Helv Chim Acta 19, 357-362). Also in the capon comb test, Heusser et.al. found 5-AA to be a little less than 4 times as active as 4-androstenedione (Androstenedione or Androstene). Finally, Cavallero et.al. found that its activity on the exorbital lacrimal gland of the castrated rat was less than 20 times that of testosterone (Acta Endocrin. 55, 131-135).

Obviously 5-AA is not converting very much to DHT, otherwise you would see much more stimulation of these organs. So my conclusion is that this prohormone is not very effective, and certainly not worth the prices it is being sold for by some companies. As far as the advertising claims being made for the stuff - well - they obviously are a far, far cry from the truth.

Are there any other potential side effects?

Do not take 1-AD if you have any liver dysfunction or if you are taking medicine that effects liver function. Higher dosages of 1-AD (more than 600mg/day) may result in elevated readings of ALT (SGPT) in liver enzyme tests. These readings return to normal soon after discontinuation.

A minor percentage of early 1-AD (1-androstenedione) users experienced gastric upset, and/or urinary irritation from the product. These effects are dose dependent. Users should take this product exactly as indicated. That is, always take with a meal. Furthermore, one should start off at the lower end dose and slowly increase, so as the body has a chance to adjust to the product. Always drink plenty of water throughout the day as well. Most users that experienced these problems find that the effects subside over time if they follow this advice. This is no longer a problem with the current 1-AD.

This irritation was due to intrinsic properties of 1-androstenedione. It was NOT due to any impurity in the product. 1-androstenedione has peculiar properties similar to chili pepper (capsaicin), in that it is an irritant to mucous membranes, but not harmful. We have solved this problem by switching to an alternative 1-testosterone precursor, 1-androstenediol. As a result, current batches of the product have been improved in potency as well as side effect profile.