Designer Steroid Discussion

I’m sure many readers will be aware that the term “prohormone” is now used somewhat euphemistically in the bodybuilding supplement industry to describe a wide range of what are essentially anabolic steroids, albeit ones that have yet to be scheduled or added to any list of controlled drugs. Governments around the world are slowly reacting to the widespread use – and abuse – of these compounds, by adding them to existing legislation in place to prevent the proliferation of steroids for non-medical (cosmetic or athletic) uses.

The scheduling process is a demanding and time-consuming one, with legislators operating years behind the grey market they are trying so hard to govern. No sooner has a compound been legislated against than several new ones appear, leaving the authorities playing a perpetual catch-up game.

For example, the designer steroid “methasterone”, commonly known as “superdrol”, has been sold online since 2005 – yet one of the first manufacturers to sell it was only prosecuted in November 2011. [1]

Despite the product being an “unapproved drug”, due to the less-than-watertight definition of an anabolic steroid in the US Controlled Substances Act it isn’t actually considered a controlled drug until it’s added manually to the list of Schedule III drugs – a laborious process of red-tape which only began in November 2011 [2] and may well not even be completed by the end of this year (2012), judging by the time similar previous amendments have taken to get passed. [3]

In the 1960s a lot of research was going on into steroids, in the search for compounds with strong anabolic effects, but low androgenic (or secondary sex characteristic) effects that could be used to prevent muscle-wastage in weakened medical patients (the results of which also found adherents in millions of bodybuilders worldwide). Today research in that field has all-but stopped because the public and governmental attitude is that “steroids” is something of a dirty word, carrying far too many negative connotations. In some cases existing steroids are being “rebranded” as “SARMs” (Selective Androgen Receptor Modulations), possibly in order to avoid the prejudices associated with anabolic androgenic steroids. [4]

In December 2009, a number of steroids and “steroidal precursors” (prohormones) were added to the UK’s Misuse of Drugs Act, making them Class C Controlled Drugs, [5] and detailed above are the ongoing efforts to schedule “Superdrol” and “Prostanozol”. So are the days of the over-the-counter steroids nearly over? Not necessarily.

A number of specific steroids are already legislated against, however with a slight chemical adjustment the resulting compound is very similar, but no longer illegal. The compound known as “Halodrol” for example, differs from the (illegal) Oral Turinabol only in that it has a hydroxyl group at the 3 position instead of a ketone. Small changes to the structure like this, for example by substituting functional groups, or the introduction of a covalent double bond between two carbon atoms, can allow cunning Chinese chemists to continue providing what the market demands: muscles in a bottle, a credit card away.

There are many such potential variations on existing steroids that could be synthesized and released in order that the community reliant on them stays one step ahead of the legislative process, one of which is illustrated below.

Desoxymethyltestosterone

One of the recently banned compounds was DMT, a.k.a. desoxymethyltestosterone (commonly known as “phera” or “pheraplex”; also referred to as “Madol”), a steroid made famous by its use to circumvent doping restrictions by athletes in the BALCO scandal. [6][7] This is now a Class C drug in the UK, [5] and a Schedule III controlled substance in the US. [3]

1a,17a-dimethyl-17b-hydroxy-5a-androst-2-ene

Among the compounds synthesized and discarded during the 1950s/60s “gold rush” on steroids was the compound above – 1a,17a-dimethyl-17b-hydroxy-5a-androst-2-ene. Although it closely resembles desoxymethyltestosterone, it is different enough to slip through the loopholes of the US Controlled Substances Act, in much the same way many of the synthetic “legal highs” of recent years did.

By adding a methyl group at the 1a position, a completely new steroid is created, with electronic androgen receptor binding properties that are distinct from the illegal desoxymethyltestosterone. 1-methylation of 5a-androstanes tends to reduce androgenic activity and favour anabolic activity, [8][9] and this steroid appears to also follow that trend.
According to the 60s research, “desoxydimethyltestosterone” is less anabolic than desoxymethyltestosterone (roughly half as anabolic), though since it’s androgenic effects were much less (around a quarter of the effects of desoxymethyltestosterone), it actually presents an improved A:A ratio (or “Q value”) of around 10, whereas desoxymethyltestosterone has an A:A ratio of around only 6.5. [10]

This positive ratio of high anabolic effect to relatively low androgenic effect, although only demonstrated in castrated rats, would seem to make it an attractive prospect both for those unscrupulous companies looking to resurrect designer steroids that have yet to be legislated against, and the guinea pigs who line up to take them.

With minor structural changes like these providing new, highly-profitable compounds to an eager – and growing –  market, and the lax controls on the pharmaceutical labs in China providing a cheap source of raw materials, there appears to be no end in sight for the availability of over-the-counter designer steroids.

References:
[1] FDA Press Release: Supplement Manufacturers Plead Guilty to Selling Products Containing Unapproved Drugs
[2] Classification of Two Steroids, Prostanozol and Methasterone, as Schedule III Anabolic Steroids Under the Controlled Substances Act
[3] Classification of Three Steroids as Schedule III Anabolic Steroids Under the Controlled Substances Act
[4] Steroids. 2010 Jun;75(6):377-89.
[5] The Misuse of Drugs Act 1971 (Amendment) Order 2009
[6] Toxicol Lett. 2007 Feb 28;169(1):64-71
[7] Rapid Commun Mass Spectrom. 2005;19(6):781-4.
[8] Steroids. 1966 Aug;8(2):209-18
[9] Steroids. 2009 Feb;74(2):172-97
[10] Acta Endocrinologica 1966, Vol 53, Issue 4, 635-643