Mestanolone DDR steroid substanz 646

Mestanolone (STS646 )

Methyldihydrotestosterone (methyl-DHT; 17alpha-methyl-17beta-hydroxy 5alpha-androstane-3-on (mestanolone) is a steroid that has characteristics similar to those of DHT (dihydrotestosterone), but unlike DHT is orally bioavailable [1]. Methyl-DHT was the second most commonly used steroid by German athletes in decades past, who were among the best in the world largely because of widespread steroid use [2]. There is comparatively little information, either scientific or anecdotal, on methyl-DHT, although there is a wealth of information on DHT. This article will discuss the information on methyl-DHT and what can be expected from this compound.

One common way of characterizing steroids is by their relative anabolic (muscle-building) and androgenic effects. Androgenic effects refer primarily to secondary sex characteristics: increased body hair, deeper voice, balding, and so on. Androgenic compounds characteristically also have strong psychological effects, such as increased aggressiveness and concentration. Among bodybuilders, highly androgenic compounds are commonly used pre-contest or during cutting cycles for increasing muscle hardness and decreasing water retention and also to provide stimulation and increase concentration and performance in the gym. They also typically have anti-estrogenic effects.

The anabolic and androgenic effects of methyl-DHT were compared to testosterone and methyltestosterone in some early animal studies [1]. In tests of its androgenic potency (total of five tests), methyl-DHT ranged from 20-255% as androgenic as testosterone or testosterone propionate, with a per study average of 70%. In terms of anabolic effects relative to testosterone, the range was 25-105% with an average at 55%. One study also compared the effects of methyl-DHT to methyltestosterone, and it measured as ~60% as androgenic and 25% as anabolic. The large differences in these values are due to multiple differences in experimental design, not to mention the problems with extrapolating animal research to humans, but this research does give a general idea of what the potency and effects of this compound might be.

Although some scattered small-scale research does appear to exist, there is very little published information on the use of methyl-DHT in humans. Observations in Germany by scientists indicated that it is effective at increasing athletic performance [2]. There is also a patent that describes some of the effects of methyl-DHT administration on humans [3]. According to the patent, methyl-DHT is anabolic in humans, but not with the same potency of other commonly used steroids. However, this was with only 10-20 mg daily. They also reported a strong anticatabolic effect (in other words, it inhibited lean tissue breakdown) in a study of 54 "physically highly stressed test persons."

Most notable in the patent, however, were comments regarding the psychological effects of methyl-DHT. To quote from the patent:

"This research completely unexpectedly and surprisingly discovered a hitherto unknown further action of mestanolone [methyl-DHT], namely the supply thereof led to an optimization of the central nervous system activation during preparation for the task and to a maintaining of this optimum activation even under high stresses. Thus, there was an increase [in] psychophysiological capacity.

"...The test persons performed difficult exercises requiring high physical capacities linked with high intellectual concentration and muscular coordination with far fewer errors. Complicated movement sequences with a high degree of stressing did not lead to a reduction in the degree of activation and instead the increased capacity remained after several repeats."

A final effect indicated in this application was that after 20 mg for six weeks, natural testosterone production was not affected. It should not be counted on for this effect to be reliable, as it could have been a function of dose or the way that testosterone regulation was measured. All steroids should be cycled on and off, with the employment of proper post-cycle therapy.

There is also another study, published in the early 1960's, in which women with tuberculosis were given 100 mg daily of methyl-DHT sublingually. Compared to control, the women given methyl-DHT had increased body weight and nitrogen retention [4].

Although user feedback is generally unreliable, it is the next best thing given the low amount of published information on the effects of methyl-DHT in humans. In general, reports from users are in line with what should be expected given the characteristics of this steroid: the perception of muscle hardening, decreased appearance of body fat, strength increases, muscle preservation while dieting (but no pronounced muscle building effect), increased sex drive, and increased confidence and concentration in the gym. In terms of side effects, some report an increased rate of hair loss, while others do not note this effect.

We now have information on the historical use of this compound in Germany, animal studies, a human study (albeit from a patent application, which is far from ideal), and user feedback. Putting this all together, we find that the information is generally consistent, and the following conclusions can be drawn:

Methyl-DHT has a strong psychological component, increasing aggression, concentration, strength, stamina, and athletic performance. It is ideal for use pre-workout.

Methyl-DHT will build muscle, but not nearly to the same degree as potent muscle builders such as methyl-1-test or many other commonly used steroids. However, it will help preserve muscle during periods of high stress or dieting.

Side effects will be primarily androgenic in nature, and estrogenic side effects (gyno, water retention) are very unlikely. Concurrent use of other substances to prevent hair loss, acne, or prostate enlargement (note that whether or not DHT causes this is a point of debate) is something to consider. Also, women should not use methyl-DHT.

It may be that methyl-DHT is best used as a supplement to a more potent substance while on a cycle. By using this strategy, one could have the muscle building effects of one compound and the psychological benefit of methyl-DHT at the same time.

In terms of dosage, 20-50 mg is recommended. Generally, people will take a dosage on the higher end of this range as a standalone, or a lower dose when stacking. Since this compound is methylated, liver toxicity is a potential concern. Not taking more than 50 mg, limiting cycle length to a month or less, avoiding alcohol, other methyls, and other drugs that may compromise the liver, and taking a supplement to protect the liver are all recommended. And, as with any steroid or prohormone, a cycle should be followed up with post-cyle therapy.

References

1. Vida, Julius A. Androgens and Anabolic Agents: Chemistry and Pharmacology. Academic Press 1969.

2. Franke WW, Berendonk B. Hormonal doping and androgenization of athletes: a secret program of the German Democratic Republic government. Clin Chem 1997 Jul;43(7):1262-79.

3. Mattern et al. Medicament for influencing the degree of activation of the central nervous system. US Patent #5591732, Jan 7 1997.

4. Harris LH. Protein anabolic action of mestanolone. J Clin Endocrinol Metab 1961;21:1099.

This application is a 371 of PCT DE 93/00473, filed May 28, 1993.

The invention relates to a medicanent which, apart from its already known action in the metabolism, is able to positively influence the activation state of the central nervous system or physiologically optimize the same and/or is active in the prophylaxis and therapy of osteoporosis.

Apart from other factors, the psychophysiological and psychic capacity of the human being is significantly determined by the state of activation of the central nervous system. This activation can be evaluated by means of the shift of the average alpha-frequency in the electroencephalogram. Each physical or psychic stress to the human being leads to an increase of approximately 4 to 6 Hertz of the frequency as compared with the individual starting value. This increase is linked with an improvement to the psychophysiological capacity. If the stressing is excessive or cannot be adequately controlled, the alpha-frequency decreases after passing through an optimum. As a result the psychophysiological capacity drops and can sink below the starting value prior to the start of stressing.

Research carried out on top sportsmen proved that the increase of the alpha-frequency is triggered by mental concentration connected with completing the task. An appropriate physical activity before controlling the actual stress has the same effect. If the optimum of the activation is exceeded by false preparation, overstressing, fear situations or disturbing external influences, the capacity decreases, errors increase, corrections are associated with more psychic and physical effort. The degree of exhaustion on completing the task is higher.

In middle and old age a cause of the decreasing capacity is an inadequate stress activation of the central nervous system. In phases of longer-term and high psychophysiological stressing and particularly with restricted activation, the setting and maintaining of an optimum activation state of the central nervous system acquires particular significance at this age for maintaining and optimizing capacity.

Through changes in the hormonal balance as from an age of 45 to 50 years there can be a catabolic situation in the calcium metabolism of the bone, which leads to calcium depletion (osteoporosis). A substitution of this function without disturbing the endogenic control system is necessary. For woman in the menopause therapeutical schemes have been tested, but there is no satisfactory solution for men. All the steroid hormones and derivatives tested up to now have revealed clear negative influencing of the endogenic control system.

It has now surprisingly been found that both an optimum activation state of the central nervous system and also (simultaneously or separately therefrom) an activity during prophylaxis and therapy of osteoporosis can be obtained by the application of a medicament having a content of mestanolone and/or Oral-Turinabol.

The medicament can be used as a controlled-release dragee, depot form or buccal tablet, or in the form of a galenic formulation, which permits pernasal application by means of a nasal spray. Preference is given to a content of mestanolone and/or Oral-Turinabol of 5 to 20 mg per ingestion unit.

Mestanolone (STS 646, 17.beta.-hydroxy-17-methyl-5.alpha.androstan-3-one) is a testosterone derivative. As a result of the chemical modification the prevailing androgenic activity of the active ingredient is reduced and the anabolic activity increased. Mestanolone is authorized in Greece under the indication "anabolic/androgen".

It has surprisingly been found that, compared with other anabolically acting steroids (e.g. methandrostenolone), which can be therapeutically used, the anabolic activity of mestanolone is much lower. When administering the same dose (e.g. 10 to 20 mg daily) under mestanolone there is a reduction of the urea concentration in the blood and at 4% it is much lower than with the other steroids (up to 30%).

Research carried out on physically highly stressed test persons revealed that on supplying mestanolone the protein metabolism remains in equilibrium and neither during, not after stressing catabolic situations occur. However, a marked accentuation of the anabolic situation was not detected.

This research completely unexpectedly and surprisingly discovered a hitherto unknown further action of mestanolone, namely the supply thereof led to an optimization of the central nervous activation during preparation for the task and to a maintaining of this optimum activation even under high stresses. Thus, there was an increases psychophysiological capacity.

54 test persons highly stressed for a long period of time had, after the administration of 10 mg of mestanolone daily, a marked increase of the alpha-frequency by up to 4 Hertz. With this was associated a regularizing and optimizing of the frequency rise under stress. The test persons performed difficult exercises requiring high physical capacities linked with high intellectual concentration and muscular coordination with far fewer errors. Complicated movement sequences with a high degree of stressing did not lead to a reduction in the degree of activation and instead the increased capacity remained after several repeats.

Therefore the supply of mestanolone is suitable in high stress phases and particularly in human beings in middle and old age with activation deficiencies is able to trigger and support stress-adequate optimization of the central nervous activation state.

Due to these results comparative tests were carried out on 10 test persons, which were subject to exhausting physical stresses for 4 to 6 hours daily. Five of the test persons were given for six weeks on a daily basis between 5 and 10 mg of Oral-Turinabol, in order to ensure an adequate restoration and stressability. The other five test persons were given a placebo. The anabolic action of the medication was, as expected, detectable by means of the concentration of myoalbumin and urea in the serum. However, compared with the test persons who received the placebo, there was surprisingly also a clear increase of the central nervous activation of most of the test persons treated with Oral-Turinabol. This side effect of Oral-Turinabol was not hitherto known.

The application of the active substance can take place in the form of delayed-action dragees, depot forms or buccal tablets. However, it is particularly advantageous for a pernasal application of the medicanent in the form of a nasal spray. It would appear that this pernasal application facilitates passage through the blood-brain barrier. Therefore the active ingredient passes more rapidly and bypassing the first-pass metabolism in the liver to the effector organ, or organ, the steroid receptors present in the central nervous system. Associated with this bypassing action the necessary dose per individual application can be reduced to approximately 5 rag. By reducing the dose and bypassing the liver negative influences on the liver metabolism which, according to the literature could be caused by 17-alpha-methylation, are avoided.

A further, particularly advantageous characteristic of the further medical indication of mestanolone and Oral-Turinabol according to the invention is that these substances, unlike other anabolically active steroids, even in the case of administration over a longer period of time (20 mg daily for six weeks) have no negative reactions on the endogenic regulation of the testosterone level. This is also a surprising observation in view of the known behaviour of other anabolics.

The supply of mestanolone and/or Oral-Turinabol leads to an optimization of the central nervous activation without any negative influencing of the endogenic regulation of the testosterone level and therefore the individual anabolic/catabolic equilibrium in the metabolism. In addition, these substances offer the advantage of a mild anabolic action and therefore of favouring the calcium incorporation into the bone without disturbing the endogenic regulation. This makes it possible to use the stabilizing action on the metabolism also for the prophylaxis and therapy of osteoporosis. It is particularly important that a long-term application is possible without any harmful reactions. The above-described positive effect on the central nervous system has an additional advantageous action. However, naturally both effects can be individually used.

The features of the invention described in the description and in the claims can be essential both individually and in random combinations for the realization of the different embodiments of the invention.

Dihydrotestosterone (Transdermal, I.M.)

DHT has proven effective in the treatment of microphallus, applied topically,37 and has been shown to be of value in the treatment of elderly hypogonadal men. Within the prostate, exogenously supplied testosterone is enzymatically converted to DHT, a more potent agonist of the AR, and also to estradiol. Prostate enlargement is a common side effect of testosterone use, perhaps for these reasons. However, it has been found that when DHT itself is supplied to elderly hypogonadal men, reduction of prostate size occurs.38 This appears to be due to inhibition of endogenous testosterone, estradiol, and aromatase. Furthermore, DHT is more potent than testosterone in most tissues (perhaps excepting muscle, as a result of enzymatic conversion to the diol) whereas testosterone is effectively less potent to those tissues lacking 5a-reductase. DHT can therefore be given in a lower dose than testosterone to achieve the same effect in target tissues, and therefore, less DHT, less testosterone, and less estradiol reach the prostate when DHT itself is given as the drug. However, DHT has not been studied much for use in replacement hormone therapy.

(Choi SK et al. J Urol (1993) 150 657

deLignieres B. Ann Med (1993) 25 235)