Is methandienone the king of anabolic steroids or is this claim exaggerated? The following story will show you that there may be something rational about it. In any case, this steroid compound, created supposedly on purpose for athletic purposes, has started something that will be very difficult to stop.
The genesis of methandrostenolone/methandienone
There are several stories about the origin of the testosterone analogue methandrostenolone, which is often referred to in the literature by its second generic name, methandienone. Beware, it is exactly the same substance. Trade names are then invented by each pharmaceutical company independently after the period protected by the inventor’s patent application has expired. But one thing these stories have in common is that they always feature the name of the inventor, Johnny Ziegler. This story is based on the description of the event as published by columnist Nelson Montana on the “Testosterone” website. The description is reportedly based on an interview Ziegler himself gave just before his death in 1983.
The origins date back to 1940, the location being Nazi Germany. The main character is Adolf Hitler, who decided to take over the world with the help of his nation. In order to realise his twisted dreams, Hitler needed, in addition to advanced combat technology, an army of extremely fit men who would be strong, fast, aggressive, and who would recover quickly from any injuries. In other words, they would be invincible supermen. The Nazi medical establishment decided to create a cure that would enable men to cope with the harsh conditions of war, including overcoming the effects of food shortages. It did not matter whether the soldiers would later suffer any health damage as a result of taking this medicine. The goal was victory at any cost. What did human health mean in war? Fortunately for the Nazi scientists, their plan did not fully succeed, which may also have contributed to their ultimate defeat.
It was not known at the time that there was another state, the Soviet Union, which had similar plans. By the end of the Second World War. World War II, Russian scientists successfully produced a synthetic form of testosterone, and started an entirely different form of war, this time fought on the sports field. By the end of the 1950s, it was clear that the athletes of the former Soviet Union had dominated the sporting disciplines requiring strength as the main criterion. The performance dominance of USSR athletes was, of course, not to the liking of the Americans. The U.S. government reportedly asked weightlifting team doctors to investigate the seemingly inexplicable domination of the USSR’s super athletes. One of the doctors, then working for the American weightlifting team, was a young Johnny Ziegler, who saw no problem with it.
American scientists were investigating a group of Russian athletes who had emigrated to the US at the time. They noted hypertrophied prostates and elevated concentrations of the 5α reduced testosterone metabolite dihydrotestosterone in the young men. From this finding, they deduced that exogenously administered synthetic testosterone would be the cause of both the health abnormalities and the excellent athletic performance. Once again, for prestigious political reasons, it was about winning at all costs. Who cared about the health of athletes? In Germany, the trials of the responsible sports officials of the former GDR are still going on today. This is always the case when historical memory and the willingness to deal with the past are lost. I can understand it, many high-ranking people are involved in this, who of course have no desire to clarify things.
American scientists, headed by Johnny Ziegler, have, based on the quoted findings, tried to find a testosterone analogue that would have accentuated anabolic effects while suppressing or at least reducing undesirable androgenic characteristics. It was allegedly Johnny Ziegler who, in 1956, came up with a proposal for a molecule which, as it was later to be shown, met the scientists’ expectations to some extent. Ziegler reportedly offered his discovery to the pharmaceutical firm CIBA, which, according to rumour, was to pay him $100 for it. Even from this sum you can guess what was going on. Let’s be realistic, without extensive research over several years, costing tens of thousands of dollars, nothing worthwhile can be invented and implemented. By the 1960s, CIBA then marketed the substance under the trade name Dianabol in the USA. Very soon, athletes of all disciplines, not excluding bodybuilders of course, became interested in this substance and its effects.
Gentleman’s two-pill deal – truth or fiction?
Nelson Montana describes another shocking story in his article. This one is directly related to bodybuilding. As I have already stated, the introduction of Dianabol to the pharmaceutical market has caused its abuse by athletes, including bodybuilders. Soon the negative health consequences of such actions became apparent. This alarmed some of the top bodybuilding figures at the time to the extent that they considered it necessary, in view of the possible damage to health, to take protective measures. The then bodybuilding guru and mentor of top bodybuilders, Vince Gironda, called a meeting which, in addition to himself, was to be attended by Larry Scott, Don Howorth, Dave Draper and perhaps others. Vince Gironda was opposed to exogenous hormone manipulation, on the other hand he understood the needs of professional bodybuilders who had to maintain, with a view to impressive presentation, a certain muscular development. They agreed together on a compromise, which was not to exceed 2 Dianabol tablets a day. Larry Scott went on to become Mr Olympia twice in 1965 and 1966. We can only guess if he kept this two-pill agreement? It has to be said that there was no ban on doping at the time, so it was truly a chivalrous affair that can hardly be judged today. “Those directly involved in the meeting swear that this is true,” says Montana.
However, a new generation of bodybuilders came along who were completely alien to the sentiments of their predecessors, and so the usual merry-go-round began. Four Dianabol pills work better than 2 pills, 8 work better than 4, etc. Later, 10, 20 or 50 tablets in combination with several other preparations became the norm. What kind of bodybuilding experience have I had? No matter where you step, you will always come across anabolic steroids.
Mechanism of action of methandrostenolone
Mauro G. Di Pasquale, an associate professor at a Canadian university, writes the following in his 1984 book on the mechanism of action of anabolic steroids: “All anabolic steroids have a common mechanism of action that requires the binding of the steroid hormone to a specific receptor in the target tissues. This hormone-receptor complex then stimulates RNA production, which further increases protein synthesis”.
This may be because the book was written in 1984, but the citation is highly misleading and in many ways inaccurate. First of all, you must not think that this receptor to which the steroid binds must be an androgen receptor. In many cases, it will be another protein of another signaling system, such as some growth factor. It should therefore be plural and omit the term specific. It can be stated today that each so-called anabolic steroid has its own specific set of mechanisms of action, about which, unfortunately, we do not know much. It is no longer true at all to claim that all anabolic steroids increase protein synthesis (at least not muscle protein). The only oral synthetic steroid for which this property has been demonstrated in humans is oxandrolone. It should also be noted that in this case it was pure muscle protein synthesis.
Also, Grundig in his anabolic manual “World Anabolic Review 1996” states the following: “The effect of Dianabol promotes protein synthesis”. I really don’t know where these people go for this information? Regarding methandrostenolone specifically, it is difficult to assess its effects, let alone its mechanisms. Research is scant in this regard.
I’m going to attempt to do so without guarantee. The first thing to note is that methandrostenolone has a very low relative binding affinity (henceforth RBA) for androgen receptors, at least in the animals studied. In one 1984 study, the RBA of methandienone for both rat and rabbit muscle was only 2% of the binding of methyltrienolone, which was and still is the reference steroid with excellent affinity for this protein. Furthermore, radiolabelled dihydrotestosterone and mibolerone are sometimes used as a reference steroid for these purposes. By comparison, for testosterone, this RBA in the cited study is 23 % for rat muscle and 7 % for rabbit muscle. I state this for those who take pride in the binding affinity of steroids. However, binding alone is not a guarantee for the effectiveness of an anabolic steroid, for that further steps are required, the explanation of which is beyond the scope of this article. Even antiandrogens (now more recently referred to as SARMs – selective androgen receptor modulators) have quite good binding affinity for androgen receptors, and yet subsequent androgenic effects do not occur.
The low binding affinity of most synthetic anabolic-androgenic steroids is quite logical. Try taking a file or a welder to your apartment key and make a shape change. Chances are you won’t insert the key into the lock at all, otherwise you will insert but not turn. This is exactly what scientists have done with the molecule in an attempt to dissociate androgenic effects from anabolic ones. It was a mere experiment or game of chance which, due to ignorance of the mechanism of action, failed completely, although partial success must be admitted. Today, perhaps scientists with their more advanced methodology and technique would be more successful, but for the sake of bodybuilders, no one will bother with it. Anabolic steroids, as drugs, are already passé, so there is no one to pay for it. In any case, it is desirable for many reasons to clarify the mechanisms of action of each class of anabolic steroids. For example, in 1998, research was published on stanozolol, which discovered a completely unique mechanism of action for this substance, but more on that some other time.
The anabolic effect of methandrostenolone was demonstrated in 6 trained athletes even after administration of only 15mg/day of this substance for 2 months. There was a significant increase in body weight. However, the study was aimed in a different direction and so the abstract does not include specific figures on body composition.
In rats fed a legume diet (beans) plus Dianabol, there was a significant decrease in non-protein nitrogen in skeletal muscle and a significant increase in the myofibrillar nitrogen fraction of that muscle. I would characterize this manifestation, in bodybuilding jargon, as an increase in muscle density. Undoubtedly something every bodybuilder strives for, and which has been proven in practice. By the way, the dose of Dianabol was 1 mg per 100g of diet. It gets worse with proof of how these manifestations occurred. Anabolic effect, anti-catabolic effect, satellite cell stimulation, etc.
I found one study that examined the effect of methandrostenolone, methylandrostenediol and Retabrol on muscle protein synthesis in rats. I only have the abstract, which does not give the results of this investigation. Otherwise, it is concluded that anabolic steroids increased skeletal muscle protein content: myosin, myofibrillar and sarcoplasmic fraction. Again, at least an increase in muscle density can be discussed. Otherwise, however, this may have been due to suppression of proteolysis. This hypothesis of mine is supported by the findings of research that investigated the effect of exercise and Dianabol on the rate of myofibrillar protein degradation in the heart and three muscle types in female hamsters. Conclusion: myofibrillar protein degradation was reduced in all muscles in the training group on Dianabolol and in the heart of the non-training group on Dianabolol.
Understanding these effects is important for designing combinations of multiple steroids. Substances with different mechanisms of action should always, if ever, be combined. Thus, additive or even synergistic effects can be achieved with relatively small doses. I can characterise the synergistic effect succinctly with the mathematical expression: 1+1=3. Just don’t say it in school math classes if you want to graduate. Instead of, say, 30 mg of one substance, it is better to apply 2 times 15 mg of two different substances. I say this to those who will not be deterred from steroids even at the cost of endangering their lives. Moreover, this is merely a hypothesis for which I have no solid scientific evidence.
Something from practice about dosage
First of all, it should be said that therapeutic doses of methandrostenolone are usually set by various manufacturers in the range of 2.5 to 10 mg/day for adults. Thus, from the perspective of today’s bodybuilding, ridiculous doses. But keep in mind that even these therapeutic doses have irreversibly damaged health many times. After all, even Aspirin, containing acylsalicylic acid, can do that. By the way, with the ephedrine, caffeine, Aspirin™ combination, the combination used for sculpting, it is the latter that bothers me the most. Finally, all drugs have adverse health effects, but anabolic steroids occupy a special place among them, given their steroid structure. Whoever does not believe this is his problem and life’s mistake.
It seems to me that every new generation of bodybuilders comes up with higher doses of steroids, not to mention other doping.
I find the answer of English steroid guru Brian Batcheldor to the question interesting: “What’s the highest dose you’ve heard of someone taking?” The answer can be found on the website of the magazine “Testosterone” on the Internet. The answer is a lot. However, most reports on the subject are grossly exaggerated. Take the case of the unfortunate Andreas Muntzer, who made it into the medical literature for his unprecedented withdrawal, based on a cycle written on a scrap of paper found on him. However, those who knew him know that this was merely a commonly used trick to partially protect the person concerned in case he was caught with large quantities of steroids, indicative of trafficking.” He goes on to say, “In fact, some of the most extreme cases of abusers that I am aware of took place in the late 1970s and early 1980s. I personally know two powerlifters and 5 top bodybuilders (two Olympia level) who admitted to taking anywhere between 50-100 Dianabols™ a day during the 70’s”. Elsewhere he continues. ” I also know of one powerlifter who admitted to regularly taking 100 Dianabolol™ a day and adding a total of 10,000 mg of testosterone a week in the weeks leading up to a competition”. Don’t be scared off by the zeros, it’s actually 10g.
Next. “The most extreme case I have heard of was confirmed to me by a certain English Olympia competitor. He was taking 2 Anadrol, 10 Dianabol, 6 Halotestin and 100 Anavar a day in preparation for his last competition in the 80s. To this he injected 4000 mg of Deca, 2000 mg of Testosterone Cypionate, 400 mg of Winstrol and 400 mg of Primobolan per week”. So much for Brian Batcheldor.
If someone asked me the same question, I would have to answer “60 methandrostenolone tablets and 2g of testosterone per week”. This was in the Central European area and I have the information second hand.
I was going to mention the health implications, but the article dragged on and I have to finish. More about health next time. Otherwise, I don’t recommend even small doses. Know that negative consequences cannot be avoided. What Brian describes then is insane.