Methylestradiol
Looking at the aromatization of methyltestosterone, we see an irrefutable example of just how methylation can increase the potency of a steroid, despite decreasing its receptor binding. We start by noting that there is little argument among bodybuilders today that methyltest is much more estrogenic than testosterone milligram for milligram. In fact, it’s known as one of the worst offenders in this regard, and most bodybuilders don’t go near it for this reason. In my first book, Anabolics 2000, I mistakenly attributed this to a greater rate of aromatization (estrogen conversion). Why else would it be so bad? It must be that more estrogen is produced with methyltestosterone, naturally. I was, however, making very much the same mistake as the proponents of the Class System. I was making assumptions without looking at the whole picture. Upon further investigation, my theory of course crumbled, as I found that methytestosterone is aromatized at only 44 percent the rate of testosterone.  It is a much less active estrogen producer, which at first glance didn’t make sense. How can this be possible if it is so much more estrogenic? I needed an explanation, and wasn’t resting until I had one.
The answer, I later found, lies in the fact that methyltestosterone converts to a completely different estrogen than does testosterone. Because its added 17alpha-methyl group cannot be removed metabolically, it aromatizes to 17-alpha-methylestradiol (17ME) instead of regular estradiol. 17ME is clearly a much more potent estrogen in comparison, which obviously explains the more problematic nature of methyltestosterone regarding estrogenic side effects. The truly enlightening thing, however, comes in understanding exactly why 17ME is such a potent estrogen. It’s not because it binds the estrogen receptor more avidly than estradiol. In fact, it was shown to be weaker in studies.  It is more potent for some of the very same reason that our Class II androgens are. Methylation had, again, dramatically increased the half-life of the steroid hormone, and presumably its affinity for serum binding proteins, creating a much more active hormone despite weakening its ability to bind the estrogen receptor. The relationship to our Class II steroids is obvious. 

In Conclusion
I’m not disputing that there are non-androgen-receptor mediated activities inherent in many, or possibly all, anabolic/androgenic steroids. More research needs to be done, but clearly there are other mechanisms involved in muscle growth, such as those that may be mediated through glucorticosteroid displacement, estrogen conversion, or the level or activity of other hormones and proteins. I do, however, dispute the broad classification system discussed here. When held up to the light, the whole theory falls apart. We can clearly see, and explain away, the logic that went into its inception. Early proponents had mistaken poor binding and obviously high potency to indicate that certain steroids worked primarily through different pathways. Steroid half-life, serum binding protein affinity, and the potency of active metabolites all failed to be taken into account. When these factors are examined, we no longer see any true Class II steroids. We are left only with a collection of misunderstood oral steroids, and a theory that doesn’t hold water.

References
Steroid Profiles: Dianabol. Mesorx.com

  Pharmacokinetics of plasma and urine clenbuterol in man, rat, and rabbit. Yamamoto I, Iwata K, Nakashima. J Pharmacobiodyn 1985 May;8(5):385-91

  Metabolism of Anabolic Androgenic steroids. V. Rogozkin. 1991 CRC press.

  Sublingual and Oral Administration of Methyltestosterone. A comparison of Drug Bioavailability. Alkalay et al. J Clin Pharm April 1973 p 142-51

  Relative binding affinity of anabolic-androgenic steroids: Comparison of the binding to the androgen receptor in skeletal muscle and in prostate, as well as to Sex Hormone-Binding Globulin. Endocrinology 114 (1984) 2100-06

  Binding of 17a-methyltestosterone In Vitro to Human Sex Hormone Binding Globulin and Rat Ventral Prostate Androgen Receptors. Wiita, Artis et al. Ther Drug Monit 17 (4) 1995 p 377-80

  Estrogen Formations by the Human Placenta: Studies on the Mechanism of Steroid Aromatization by Mammalian Tissue. K. J. Ryan. Acta Endocrinol 35 (suppl. 51) 1960 p 697-8

  Estrogen Receptor Binding Radiopharmaceuticals: II. Tissue Distribution of 17a-Methylestradiol in Normal and Tumor-Bearing Rats. Feenstra, Vaalburg et al. J Nuclear Med 24 (6) 1983 p 522-28

Black Market Update
By William Llewellyn
There is a new counterfeit testosterone cypionate on the market of which bodybuilders should be aware. This latest one is a copy of Upjohn’s Depo-Testosterone. The fake vial is actually a very good attempt at duplicating the unique appearance of this American testosterone product, so take note. You can see in the picture that both the real and fake Depo-Testosterone vials have a similar small neck and stopper. These vials and tops are somewhat unusual for counterfeit and underground steroids, and no doubt were specifically sought after by the illicit manufacturers. Furthermore, the real vial bears a very non-distinct screen-printed expiration date, making the duplicate that much harder to discern. The fake, however, stands out for two very important reasons. First, the vial is much shorter than the one used to make our real product. No doubt these exact vials were harder to get than the tops. Secondly, the label is in classic “bogus product” style, peeling right off the vial. Real U.S. drug products adhere to strict FDA manufacturing requirements, which do not allow for labels that are easily removed or replaced.
Growth hormone is an extremely expensive drug, and consequently a big target for counterfeit manufacturers. Fakes of the popular U.S. growth hormone product Serostim, for example, are currently a big problem on the black market. At $600-$700 a box, it’s no wonder there are so many illegitimate kits around these days. Over the years, many other brands fell, and will continue to fall, victim to counterfeiters, as well. GH is an item simply too profitable for them to ignore. With the high costs involved, some bodybuilders are opting to avoid the common products altogether. Fearing they might not be able to spot fakes, they are instead holding out for the more obscure GH products they hope haven’t been copied yet. This particular box of Norditropin is a good example of such an item. It is manufactured in the Eastern European country of Slovenia, and contains 10 milligrams (approximately 30 IU) of synthetic human growth hormone. It is not a common find on the black market at this time, and no fakes are known to exist. Likewise, on the rare occasion it is located, the buyer can be confident he’s getting a legitimate product. It may even provide a more economical alternative to many other products, as pharmaceuticals in general tend to be much cheaper in this area of the world.