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26.04.2009

Anabolic effect of giant Egyptian androgens exceeds that of testosterone

You don't come across that many publications on new anabolic steroids these days. Not since chemists have managed to kid each other that SARMs are hip and good old androstanes not. In this article however, researchers at the Egyptian Natural Compounds Department National Research Center and Hi-Care Pharmaceutical describe how they synthesised a new class of anabolic steroids and tested them for week long on rats.

It's a factual article, with information on synthesis routes and the biological activity of the new compounds. The most successful, in terms of the anabolic-androgen ratio, is compound 5a. Full name: 17-cyano-17alpha-(N-methyl-trifluoroacetamido)-androst-5-en-3beta-trifluoroacetate.

It's shown in the diagram below. Beware, though: it bites.

The researchers gave experimental animals a daily 0.1 mg per kg bodyweight of the steroid for a week. At the end they measured how much the sphincter muscle and the prostate had grown in the rats. These are markers respectively for the [desired] anabolic and [undesired] androgenic effects of the new steroids.

The table below shows the performance of testosterone and component 5a. The ratio between the anabolic and the androgenic working of testosterone is 0.05. The ratio of compound 5a is enough to make your flesh creep.

Another steroid with a comparable effect mentioned in the publication is steroid 1a, with an anabolic-androgenic ratio of 2.20. Steroid 1a is shown below.

The chemists we consulted doubt whether the compounds mentioned in this article really do have the effects measured in the animal tests. They criticise the Egyptians, saying they have assumed that the steroids administered are the active components.

"I can't imagine that most of these compounds would interact so well with the androgen receptor", says Professor of Organic Chemistry Aede de Groot. "They are so big that they probably wouldn't fit on the receptor. I suspect that they have been metabolised, and that it's the metabolites that cause the effects that the Egyptians measured."

Which metabolites these might be is not clear from the article. "The acetates and trifluoracetates will be the first to hydrolyze at any rate," predicts De Groot.

When the new steroids described in the article metabolise, poisonous compounds could in theory be created. But when the researchers pumped megadoses of the new steroids directly into the gut of rats, however, there were few signs of acute poisoning.

The LD50 of the new steroids is comparable to that of testosterone and DHEA.

Source:
Acta Pharm. 2008 Mar 1;58(1):43-59.