Monthly Archives: February 2012

Modifications explained

Many people asked me about the meaning of “modifications“ of tocopherol, tocotrienol and nicotinamide – the substances used in production of xenoandrogens we are using as performance-enhancing drugs.

Frankly, until now I was not able to answer such questions. I do have some background in biology but let’s admit that manipulating non-hormonal substances to make them resemble hormones is not exactly what they teach you at the university.

While the producer is somewhat secretive about this, the scientists developing xenoandrogens are not.

So here is what I learned:

Many naturally occurring substances can exist in various different forms which will then have a different impact on human organism. One has to bear in mind that many such substances are actually very complicated molecules. They can either naturally occur in several structural variations or can be artificially modified.

This is confusing for those who are used to deal with steroids, as they know many testosterone-derivates which have all different names – and on top of that, come esterified by various esters.

This is because it is well known in medicine that a slightly different version of a hormone can have significantly different action in the body.

The situation is different with many other molecules. As they were usually not used as “serious” drugs, the classification is much more liberal. It means that you can twist and tweak, say, tocopherol and its name will be the same.

An example? Take vitamin B. You can call it vitamin B and you’ll be right. Then, you can be more specific and distinguish between B1, B2, B3, B6, B12 etc. OK, so let’s take one of them, for instance vitamin B6.

Here we are quite specific. If you produce dietary supplements and add vitamin B6, it is perfectly OK to describe it as such. But in fact, it can come in forms known as pyridoxine, pyridoxine 5’-phosphate, pyridoxal, pyridoxal 5’-phosphate, pyridoxamine, pyridoxamine 5’-phosphate, 4-pyridoxic acid.

And what about pyridoxine subgroups? Well, they don’t have specific names.

In theory, we could create countless subgroups of such substances, but the food-labels would still describe them as vitamin B6 or, say, pyridoxamine, at best.

In the case of tocopherol, the existing MegaGear anabolic steroid-clones are based on modifications of all-rac-alpha-tocopheryl acetate. How are those modifications different from their “parent substance”? Here is an excerpt from a scientific study published in 1989:

The biological activity of the tocopherols vary greatly, and this variation is only partly correlated with the antioxidant activity of the tocopherols when this is studied in a lipid medium. A number of features of the tocopherol molecule evidently contribute to the biological activity, and this may be compared with the activity of either synthetic all rac-alpha-tocopherol or to the natural RRR-alpha-tocopherol. The features causing alterations in biological activity may include (1) the presence or absence of ring methyl groups in the 5, 7, and 8 positions; (2) the number of carbon atoms in the side chain; (3) the stereaspecificity of the carbon atoms 2, 4’, and 8’; (4) the branching of the side chain; (5) the chromanol ring as compared to a furanol ring; and (6) the point of attachment of the side chain to the ring structure.  The work described in the present paper is a systematic study in which the effect on growth and on prostaglandin E2 synthesis was measured on a comparative basis for a range of structurally modified compounds.

If you are really interested in the stuff, you can read the whole article here: http://onlinelibrary.wiley.com/doi/10.1111/j.1749-6632.1989.tb14909.x/abstract

As you can see, the differences can be quite significant. It is really like calling nandrolone, trenabol, oxandrolone and boldenone just “testosterone modifications”…

In fact, the structural difference between nandrolone and testosterone is smaller than between all-rac-alpha-tocopheryl acetate and its various modifications.

By playing with the rings, sidechains and their positions, the computer program can create virtually countless modifications. Some of them are then evaluated as promising and undergo further testing.

254 modifications and counting

The recently published overview shows there are no less than 254 various xenoandrogens that can be potentially used as performance-enhancement drugs.

Of course, not all of them are fit for human use and some may – in theory – prove rather harmful.

But how you create a modification of an existing substance and how can you test its effects on human body?

Unlike the drugs of yesteryear, huge deal of designing and testing a new substance is today done in the memory of a computer only. Millions and millions of variables must be changed until there is hope that the resulting modification will have the wished-for effects.

Still, even the fastest computer is not a match to in-vivo testing: using the substance in living organisms. First, rodents are the victims. Then, some larger animals and ultimately the humans will use the substance (if safe…of course).

Every newly designed modification is tested on influencing the testosterone production, anabolic activity, protein synthesis stimulation (which is basically the same), androgenic activity etc.

Of the 254 computer-designed modifications, 47 have been tested in laboratory conditions and out of these 47, 12 eventually made it to commercial production.

The choice of those 12 modified tocotrienols and nicotinamides had been done purely on commercial base: namely, the producer was interested in substances showing close resemblances to previously known anabolic steroids.

But what about the rest? Maybe, there is a new super-stimulant that will outdo all we have ever known? Imagine sort of Oxymetholone/Dianabol/Nandrolone stack that would cause no testosterone retention and no liver damage J

Having used the xenohormones for the past several months I strongly believe such a substance is near. One reason is that I never experienced any serious side-effect and neither did my fellow-bodybuilders. And this is quite something.

To be sure, not every athlete using xenoandrogens will experience huge muscle gains. We’ve seen some who had to try several different products to feel at least some improvement. But they never had acne, shrinking testes, baldness, liver problems. Not to speak about being tested positive on steroids or just doing something that can easily land you in jail.

Another huge advantage of androgens is that they are produced and sold legally, and here I mean that you know who really produced them and under what hygienic conditions. Because this is the real problem with steroids today.