Dianabol (Methandrostenolone)

Overview and History of Dianabol

Methandrostenolone is the chemical name for Dianabol, which is the brand/trade name provided to the drug by the pharmaceutical company Ciba, which originally initially manufactured the drug. Dianabol is known as literally the number one most popular and widely used anabolic steroid in existence, with the second most popular being Nandrolone Decanoate (Deca Durabolin), and third being Stanozolol (Winstrol). Dianabol was also essentially the second anabolic steroid synthetically created, and is the first analogue of Testosterone to ever be developed (discounting Methyltestosterone, which is essentially orally active Testosterone). The development of Dianabol for all intents and purposes sparked the beginning of the anabolic steroid development boom, which began in the 1950s. Dianabol was developed by Dr. John Ziegler whom led a scientific team in the mid-1950s[1] in response to the Soviet domination of the Olympic Games. With the Americans at a massive disadvantage, an investigation had been initiated into how the Soviet athletes were vastly superior, and various Soviet Olympic athletes that had defected to America had been studied. Shortly afterwards, it was discovered that these Soviet athletes had been administered supraphysiological amounts of Testosterone via intramuscular injection. It was this administration of Testosterone that was discovered to be a major changing factor in enhancing athletic ability, specifically in the areas of muscular strength. The American response to this was the development of Methandrostenolone by Dr. John Ziegler and his team. This newly created anabolic steroid, which was an orally active chemically altered Testosterone, would be the United States’ response to the use of Testosterone in the Soviet Union’s Olympic athletes. The pharmaceutical company Ciba then marketed and released Methandrostenolone onto the market as Dianabol when the FDA approved its use.

Dianbolic 25As mentioned, this compound is a chemically modified Testosterone. This modification was an attempt at reducing the androgenic strength (and associated side effects) of Testosterone while simultaneously maintaining or even increasing the anabolic muscle building effects of the compound. The result, of course, was Dianabol. It turned out that the modifications granted it less androgenicity than its parent hormone Testosterone, but the androgenic strength of the compound was not completely eliminated – it still maintained some measure of androgenic activity. D-Bol is an orally bioavailable anabolic steroid, meaning it can be ingested orally and can survive metabolism through the liver with a high percentage of it reaching the bloodstream. Although it is primarily an oral anabolic steroid, it is fairly well known that even some injectable preparations exist, but are rarely seen or used. They can still be located fairly easily, however. As this anabolic steroid is literally the most popular anabolic steroid, it is almost universally known at least by name in all circles of gym culture, athletics, and/or anybody involved in these scenes. Even Arnold Schwarzenegger has been quoted at one point in time during his bodybuilding career as saying that “Dianabol is the breakfast of champions”. The fact of the matter as well is that it had provided plenty of medical use from assisting patients with bone weaknesses, restoring atrophied muscle, and treating anemic patients to treating pituitary-deficient dwarfism. However, Dianabol’s main niche was far more commonly found in its ability to enhance athletic performance and doping in sports in relation to the medical applications. Unfortunately as a result of this, American and Western pharmaceutical corporations slowly scaled back production of Dbol until it was halted in the late 1980s. Dr. John Ziegler as well became increasingly disillusioned with the vast amounts of abuse and overuse, and eventually became strongly opposed to anabolic steroid use in professional sport and athletics.

Chemical Properties of Dianabol

Dianabol is methylated at carbon 17-alpha on its structure (this is simply the addition of a methyl group at the 17th carbon). This process, known as C17-Alpha Alkylation, allows the anabolic steroid to be administered orally and still have a measurably strong effect on the body. Without this modification, it is impossible for any anabolic steroid to survive liver metabolism in significant enough quantities to promote any measurable effects in the body – the result is that extremely miniscule amounts of the anabolic steroid reaches the bloodstream to perform its job. It also possesses a double-bond between carbons 1 and 2. This modification in particular is what grants it a ‘milder’ androgenic strength in comparison to its parent hormone Testosterone. This double-bond is what limits Dianabol’s affinity to bind to the androgen receptor in different tissues in comparison to Testosterone. It is these modifications that also allow Dianabol’s half-life to exceed that of Testosterone (Dianabol’s half-life is 4.5 – 6 hours). An additional benefit of these chemical modifications is Dianabol’s lower affinity for binding proteins to bind to it, such as Sex Hormone Binding Globulin (SHBG). These binding globulins (in this case SHBG), which are proteins, bind to sex hormones such as Testosterone, Estrogen, Dianabol, etc. and render them inactive temporarily. What results is essentially a bound hormone that floats around in the bloodstream and does nothing – it cannot bind to receptors or do anything – and is essentially useless. These are the chemical features are that grant it its status of being a significantly potent anabolic steroid. One interesting point to note, however, is that it possesses a weaker interaction with the androgen receptor in comparison to Testosterone and many other anabolic steroids, yet it is a very strong and potent hormone in comparison. It is therefore speculated that much of Dianabol’s activity is that of non-receptor mediated activity. With this being said, Dianabol’s anabolic rating is known to be a rating of 210 in contrast with Testosterone’s anabolic rating of 100. What can be seen here is it possesses slightly over double the anabolic strength of Testosterone, and this is because of the described structural modifications it possesses.

dianabol tabletsThe Effects of Dianabol’s Modifications

Dianabol does succumb to some limitations of its own, with the first being its C17-Alpha Alkylated property. As previously mentioned, C17-Alpha Alkylation allows an anabolic steroid to become orally active and bioavailable – without it, the anabolic steroid would not survive liver metabolism. However, the negative downside in this case is that of increased hepatotoxicity (increased liver toxicity). C17-Alpha Alkylation allows an anabolic steroid to become more resistant to hepatic breakdown, and any compound that is further resistant to hepatic breakdown with always have greater hepatotoxicity associated with it. As a result, it is a smart choice to run this oral for periods no greater than 4-6 weeks at any given time in a cycle. This is to ensure healthy liver function, and for proper liver recovery following the cycle. It is because of the risk of hepatotoxicity that Dianabol’s main function in a cycle is to serve as a supportive kickstarting compound. Dbol, nor any oral anabolic steroid, should ever be run solitarily on its own. Testosterone in some form no lower than a TRT (Testosterone Replacement Therapy) dose should always be run with an oral anabolic steroid.

Dianabol contains moderate Estrogenic activity[2], and is a compound that is exposed to aromatization by the aromatase enzyme, which is the enzyme responsible for converting androgens into Estrogen. This is why its commonly known for its Estrogenic side effects of water retention, risk of gynecomastia, elevated blood pressure (often as a result of water retention), and possible fat retention/gain due to Estrogen. It has been mentioned already that Methandrostenolone expresses far less androgenic strength and activity than does Testosterone, but it is important to understand that androgen-related side effects and issues are still a concern, although they are not as pronounced as Testosterone. Dbol possesses an androgenic rating of 40-60, and when compared to Testosterone’s androgenic rating of 100, we can see there is quite a significant reduction – however, the risk of androgenic side effects can still be prominent especially in those individuals sensitive to androgenic side effects. Androgenic side effects can include: increased risk for male pattern baldness (MPB) if the individual possesses the genetic trait responsible for it, increased sebum secretion (oily skin) and associated acne, and increased facial hair and bodily hair growth. In addition, the 5-Alpha Reductase enzyme which is the enzyme responsible for converting Testosterone into the much stronger androgen Dihydrotestosterone (DHT) does also interact with it. In this case, Dihydrotestosterone is not created but instead Dianabol’s own more androgenic metabolite is the result. A positive note on this issue, however, is that it possesses a lower binding affinity for the 5-Alpha Reductase enzyme[3].

DianabolMethandrostenolone (AKA Dianabol)
Chemical Name: 17a-methyl-17b-hydroxy-1,4-androstadien-3-one
Molecular Weight: 300.441 g/mol
Formula: C20H28O2
Original Manufacturer: Ciba (originally)
Half Life: 4.5 – 6 hours
Detection Time: 5 – 6 weeks
Anabolic Rating: 90 – 210
Androgenic Rating: 40 – 60


Dianabol References:

[1] Vischer E, Meystre C, Wettstein A. Helv Chim Acta 38 (1955):1502

[2] Kruskemper, H L, Anabolic Steroids, Academic Press, New York, 1968

[3] Relative importance of 5alpha reduction for the androgenic and HL-inhibiting activities of delta-4-3-ketosteroids, Steroids 29 (1997):331-48.