Aromatization of testosterone
Testosterone – the primary substrate in the male body, which serves for the synthesis of estrogen (estradiol), the main female sex hormone. Despite the fact that the presence of estrogen may seem quite uncommon in men, this hormone is structurally very similar to testosterone. With a slight change in the enzyme aromatase, estrogen and can be produced in male organism. Aromatase activity in various parts of the body man, including adipose tissue, liver, sex organs, the organs of the central nervous system and in skeletal muscle tissues. The average number of healthy male estrogen produced usually not particularly affect the body, and may even be beneficial due to its effect on cholesterol levels. However, large amounts of it really has the potential for side effects, including such as water retention, the development of breast (gynaecomastia) and fat accumulation. For these reasons, many people prefer to minimize the intake of estrogenic activity of aromatase inhibitors such as Arimidex and Cytadren , or anti-estrogens such as Clomid or Nolvadex , especially when gynecomastia is a cause for concern, or in cases where an athlete wants to increase muscle mass. However, it is impossible to believe that estrogen does not benefit the body. In contrast, the hormone is useful in many ways. Athletes use estrogenic steroids in order to set the masses, but has only recently begun to understand the mechanisms underlying this effect. It seems that the reasons go beyond simply increasing the size, weight and power that can be attributed, and by maintaining the water in the body associated with estrogen influence and form the basis of a direct influence on the process of anabolism. These processes are associated with increased glucose utilization, sekretsiiey growth hormone and distribution of androgen receptors.
Utilization of glucose and estrogen
Estrogen may play a very important role in the development of an anabolic effect affecting glucose disposal in muscle tissue. This is due to a change in the level of available glucose-6-phosphate dehydrogenase, an enzyme directly related to the use of glucose for growth and repair of muscle tissue. Particularly, G6PD (glucose-6-phosphate degidronaza) is a vital part of the pentose phosphate pathway, required to limit the levels of lipids and nucleic acids used in the synthesis in cells for tissue repair. During the recovery period after skeletal muscle damage levels of G6PD increases sharply, that serves as a mechanism to enhance the body’s ability to recover. Surprisingly, estrogen is directly related to the level of G6PD available to cells in the recovery period. In studies that demonstrate increasing levels of the enzyme dehydrogenase after administration of testosterone propionate, it established a connection between estrogen and G6PD. Studies have also shown that the increase is directly responsible for no androgenic activity of this steroid and aromatization of testosterone to estradiol. Do not expose the flavoring steroids DHT and fluoxymesterone have been tested along with testosterone propionate, but were unable to reproduce the effect of testosterone. Furthermore, the positive effect of testosterone propionate was blocked by adding an aromatase inhibitor 4-gidroksiandrostenediona ( formestane ), while the 17-beta-estradiol, testosterone caused to close prorionatu increase G6PD. Inactive isomer estrogen 17-alpha-estradiol, not having the ability to bind to estrogen receptors, could not give any result. Further tests using testosterone propionate and anti-androgen flutamide showed that this preparation also acts as a blocker of the positive action of testosterone, which depends on androgen receptors.
Estrogen and GH / IGF-1
Estrogen may also play an important role in the production of growth hormone and IGF-1 . IGF-1 (insulin-like growth factor) – anabolic hormone produced in the liver and in various peripheral tissues by stimulating growth hormone . IGF-1 is responsible for the anabolic activity of growth hormone , for increasing nitrogen retention, protein synthesis and cell hyperplasia (distribution). One of the first studies demonstrated the overwhelming influence of anti-estrogen tamoxifen on IGF-1 levels. The second, perhaps more notably, a study conducted in 1993, considered the effects of testosterone replacement therapy and its impact on the levels of GH and IGF-1 in combination with tamoxifen. If you are using Tamoxifen GH and levels of IGF-1 were significantly suppressed, but their value rose in the appointment of testosterone enanthate. Another study showed that the use of 300 mg of testosterone enanthate per week in healthy men causes a slight increase in the level of IGF-1. Here, 300 mg of testosterone ester caused an increase in the level of estradiol, which is quite expected for this dose. The compound was compared with the same dose of nandrolone decanoate; however, this is not a steroid produced the same effect. This result is quite interesting, especially when you consider that the application of compounds to reduce estrogen levels. Another study showed an increase in the secretion of GH and IGF-1 using testosterone male delayed puberty, whereas dihydrotestosterone (aromatizing) tended to suppress the secretion of GH and IGF-1.
Estrogen and androgen receptors
It has also been shown that estrogen can increase the concentration of androgen receptors in certain tissues. It has been shown in rats, considering the effects of estrogen on cellular androgen receptors in animal studies, subjected to orchiectomy (removal of testicles to reduce the production of endogenous androgens). According to the study, the appointment of estrogen resulted in a dramatic 480% increase in binding methyltrienolone (a powerful oral androgen often used in research as a connecting link with the receptors) in the muscle, the levator anus. The proposed explanation for this is the fact that estrogen has to either directly stimulate the production of androgen receptor, or to reduce the rate of decay of receptors. Growth of the erector muscle of the anus, typically used as a base to support the activity of anabolic steroid compounds. However, actually this muscle is muscle genitals, and differs from skeletal muscle tissue in that it has a much higher concentration of the androgen receptor. The study, however, examines the effects of estrogen in tissues of fast-twitch skeletal muscle (tibialis anterior and extensor muscles of the fingers), but such an effect on the muscle that lifts the anus, was observed. Discouraging at first glance, the fact that estrogen can increase the binding of the androgen receptor in all tissues, remains extremely important discovery, especially in light of the fact that androgens have a positive impact on the growth of muscle, mediated by factors that go beyond the muscle tissue.
Estrogen and fatigue
Recently, a well-known term becomes “tired steroids” with reference to another important estrogen function in both male and female body – namely, its ability to promote wakefulness and mental activity. According to the builders, the third generation of potent aromatase inhibitors is much more extreme suppression of estrogen than it did in the past. Often associated with the suppression of fatigue. In such circumstances, an athlete, although the application of drugs to the production cycle, can not make the most of their own capabilities because of the inability to train in full force. This effect is also sometimes referred to as “steroid lethargy.” The reason that estrogen plays such an important supporting role in the activity is serotonin. Serotonin is one of the main neurotransmitters in the body, which are vital for mental alertness, and sleep / wake cycles. Malfunctions of this neurotransmitter is also associated with chronic fatigue syndrome. Inhibition of estrogen at menopause is also associated with fatigue, and are clinically used new (more powerful), aromatase inhibitors such as anastrozole, letrozole, and exemestane fadrozole. Although not all users notice a decrease in estrogen levels, the one who is still bothered by this question, can solve this problem long-term testosterone therapy or estrogen in small quantities. It is also important to note that the use of strong non-aromatizing steroids sometimes leads to this effect, as well as, probably, due to the suppression of natural testosterone production (disconnecting the main substrate in the male body for the production of estrogen).
Anti-Estrogens in sport
So, what do you need to bodybuilders who want to achieve the best results? Basically – a selective approach to the use of estrogen drugs, if weight is a key objective set (all changes, of course, if it comes to drying). Obviously, antiestrogens needed to use them only if there is a clear need (due to possible side-effects of estrogen), or at least should replace these preparations neestrogennye compound. Gynecomastia is certainly a problem for users of steroids, as well as a significant collection of fat mass. But if these problems do not occur, then the testosterone or Dianabol cycles can be added to estrogen, which helps to build muscle mass and saves energy. Customers who believe that they will notice the appearance of estrogenic side effects, or that they do not tend to their manifestation, can use estrogen drugs in order to achieve the best possible results.
Aromatization – transformation process of testosterone to estradiol. In men, estrogens are synthesized by the body only in this way, and in the body of women, they are synthesized in the ovaries.
Aromatization of testosterone occurs in the target cells, and estrogen receptors. Testosterone, contacting them, the output becomes estradiol.
It is noteworthy that the more testosterone in a man, the stronger it is and the more perfumes will estradiol, of course, if not to use aromatase inhibitors or antiestrogens (for them below), however, the level of flavoring in all the different male.
Aromatization in the required quantities – is vitally important, because estradiol in the body of the man responsible for the water balance, the recovery of the nervous system, fluid and electrolyte balance, and much more, but excessive testosterone aromatization give us the following negative side effects:
- Severe fluid retention as a result of which the muscles become, as it were inflated, swollen, the skin under the water accumulates, the joint of the joints become thicker, increased strength endurance (in some cases).
- The increased pressure caused by fluid retention.
- “Women’s mood” – mood swings, change in the character towards more vulnerable and soft, excessive emotional sensitivity.
- According to some estimates, greatly increased estradiol is able to cause hypertrophy of the prostate.
- Acne (pimples) mainly on the back.
- Weak libido, the ability to lose potency during intercourse, a very long recovery time between acts.
In fairness, it should be noted that it is not critical estradiol increased greatly assists in the set weight, due to the fact that the joints and ligaments become stronger, which makes working with large working scales. Also, due to the same fluid retention, according to some theories, the water enters the cells, and more nutrients that accelerate muscle growth. By the way, somewhat elevated estradiol (10-15%) in some cases can lead to an increase in libido and sexual intercourse time.
In summary: testosterone aromatization need, but in the right quantities. Do not allow estradiol levels above the upper reference analysis values, in which case you will get all the advantages of estradiol and bypass the disadvantages.
How to suppress testosterone aromatization
First of all, we should understand that taking anti-estrogens on the course – not the best choice. Antiestrogens strongly limit the ability of your body to the flavoring, to the point that they can lock it at all, when properly selected doses. Admission antiestrogens on the course is justified only in the case when you have a gynecomastia, and aromatase inhibitors can not cope with it, in all other cases, the anti-estrogens taken strictly not recommended.
So what is to take in this case? Aromatase inhibitors. They do not inhibit the aromatization of testosterone to estrogen receptors, they are directly linked already available estradiol in the blood, so even if you reduce it to a critical value, the new estradiol in the required amount starts synthesized in a few days, but in the case with aromatase inhibitors, a process recovery aromatization of testosterone can last much longer.
How to critically low levels of estradiol in the blood?
As has been said, is critically low estradiol as bad as critically high, and determine both the cases is easy. When a critically low estradiol you will experience a state similar to the flu: be ache joints, increase the temperature, a fever can be a very strong thirst. In this case, you must immediately stop taking any flavoring blockers and, if possible, to put the 100-200 mg of testosterone propionate in addition to its main course. It is best to use a testosterone phenylpropionate, but find it difficult, the dosage will be 200-300 mg.