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28.05.2016

Mesterolone as an anti-depressant and pep pill

The German hormone manufacturer Schering did tests in the seventies on an injectable analogue of the anabolic steroid mesterolone, the active substance in Proviron. We, the industrious compilers of this free webzine, discovered this friday afternoon when we were browsing through patents. Researchers at Schering gave mesterolone cypionate and classic mesterolone to men suffering from depression – and the results were promising.

Mesterolone
Mesterolone resembles DHT, the androgen metabolite of testosterone. The difference with DHT is that mesterolone has a methyl group on C1 and DHT does not. The methyl group makes mesterolone into a very mild steroid. So mild that, according to studies done in the 1970s, oral doses of 75-150 g daily have a negligible effect on the body's own testosterone synthesis. [Andrologia. 1974;6(2):111-8.]

At the same time the 1-alpha-methyl group inhibits enzymes that neutralise mesterolone in the body. That's why mesterolone can be taken orally.

Most handbooks say that mesterolone is too mild for male steroids users. In the past steroids users have taken mesterolone as an anti-oestrogen but without much success, and to restart the body's own testosterone production after a course of steroids - with even less success.

Mesterolone as an anti-depressant
In the 1980s researchers at Schering published a couple of studies in which they had got small groups of men suffering from depression to take 300-450 mg mesterolone daily for a period of six weeks. [Methods Find Exp Clin Pharmacol. 1984 Jun;6(6):331-7.] This treatment was successful in most of the subjects.

In another study the researchers compared mesterolone with the anti-depressant amitriptyline. [J Clin Psychiatry. 1985 Jan;46(1):6-8.] According to the researchers both substances were equally effective, but mesterolone had fewer side effects.

Mesterolone cypionate
Schering's research on the anti-depressive effect of mesterolone started in the 1970s, as the discovery of a patent dating from 1974 shows. [US Patent 3,908,007.] In that patent the researchers explicitly mention mesterolone and its esters, one of which was named mesterolone cypionate [structural formula shown below].

According to the patent, mesterolone cypionate is particularly suitable for oral use, but can be injected too.

The patent also happens to cover the use of nearly all possible analogues of mesterolone as anti-depressants. The figure below gives an idea of the dosages that the researchers used.

Mesterolone as a stimulant
According to the patent, the researchers administered mesterolone and its esters to subjects in both low and high dosages. The high dosages, shown above, had an anti-depressant effect, and the low dosages a stimulatory effect. The stimulatory dose for mesterolone administered orally lies somewhere between 1 and 20 mg, according to the patent.

"It has now been found that mesterolone and its esters exhibit a psychostimulating effect at lower doses", the researchers wrote. "The desired psychotropic and CNS-stimulating effects of mesterolone occur within 2-3 hours after administration."

Source:
US Patent 3,908,007.

More:
Of Proviron and mice - and jogging 01.10.2008

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