Hi-Tech Pharmaceuticals:

 Aromatase Inhibitor And Anabolic Agent.

Higher than normal levels of estrogen (estradiol) in men can lead to many undesirable problems, including gynecomastia (gyno). Gyno is the growth of hard nodular breast tissue under the nipple. This condition can greatly diminish the cosmetic appearance
of pectoral muscles. High estradiol can also cause excessive sodium and water retention. This will result in a bloated, puffy appearance in your muscles. Steroids and or prohormones that aromatize heavily are particularly notorious for causing water retention. All of this can be avoided by lowering estradiol levels.

Probably the worst side effect of higher than normal estradiol levels occurs when the excess estradiol sends a signal to the hypothalamus to shut down production of GnRH, a hormone that stimulates the pituitary to produce luteinizing hormone. When luteinizing hormone is shut down a signal is sent to the testicles to stop production of testosterone.

For decades bodybuilders have turned to non-nutraceutical means to “block” estradiol or prevent its development by inhibiting its conversion by the aromatase enzyme from testosterone. These latter compounds are called aromatase inhibitors and have been the most sought after approach to estradiol control.

Estradiol Control

Excessive estradiol isn’t just a concern for bodybuilders and athletes, but also for aging men – a much larger audience that is exposed to the problems associated with aging-related changes in sex hormones, such as estradiol and testosterone. As men age, these escalations in estradiol levels upset healthy testosterone to estradiol ratios, which contributes to numerous health problems, including issues for the prostate, cardiovascular system, and in maintaining desirable levels of body fat and muscle mass. Aromatase inhibitors are more desirable then estrogen receptor blockers because they function as true anti-estrogens.

Estrogenex® 2nd Generation - The All-Natural Aromatase Inhibitor

Is there an all natural, aromatase inhibitor? The answer is “YES” and its name is Estrogenex® 2nd Generation. Estrogenex® 2nd Generation binds to the aromatase enzyme and renders it inactive. This diminishes aromatase enzyme activity in the body and results in a substantial reduction in estradiol levels. The added bonus of an increase in testosterone production also occurs.

Why You Should Use Estrogenex® 2nd Generation

There are three cases when Estrogenex® 2nd Generation should be used.

The first case is while actually using prohormones or anabolic steroids. By taking Estrogenex® 2nd Generation during your prohormone/anabolic steroid cycles, you may help to avoid the problems of gynecomastia, excess water retention, and the shut down of GnRH production.

The second case is after a cycle of prohormones or anabolic steroids. By taking Estrogenex® 2nd Generation after your prohormone/anabolic steroid cycle you may help jump-start testicular testosterone production.

The third case is anytime you want a beneficial increase in natural testosterone production, even if you are not taking prohormones or anabolic steroids. Simply increasing your levels of free testosterone by only ½+ %, which can be the result of controlling excess estradiol, can give you a remarkable anabolic, muscle-building surge without the use of anabolic steroids or prohormones. (We do not advocate the use of anbolic steroids or any prohormone other than that specifically excluded in the laws that govern the DEA scheduling of anabolic steroids).

The Hypothalamic/Pituitary/Testicular Axis (HPTA)

To understand inhibition of testosterone production, you need to know first how it is produced and how production is controlled. The broad general picture is that the hypothalamus receives a variety of inputs, for example, levels of various hormones, and
decides whether or not more sex hormones should be produced. For example, both estradiol and dihydrotestosterone (DHT) are metabolites of testosterone.

The hypothalamus reacts to the presence of the metabolites in the blood. Thus, in the case of excessive levels of estradiol, the hypothalamus interprets this as being too much testosterone production and send signals to the pituitary to order the testicles to slow down testosterone production. That may sound strange that the hypothalamus responds to excessive estradiol by putting the brakes on testosterone, but it really isn’t. You have to remember that estradiol is a metabolite of testosterone, which means it originates from testosterone. Thus, (hypothalamus thinking) if there is too much estradiol, there must have been an increase in testosterone production. This reaction is part of what is called a “negative feedback” loop.

Carrying this to the next step, if less estradiol is being detected by the hypothalamus, it can react to this by telling the pituitary to signal the testicles to make more testosterone. This, then, can lead to further increases in free testosterone. Additionally, free testosterone levels can become enhanced simply because less testosterone aromatized into estradiol leaving more to possibly move about the body in the free state. Further, there are other compounds, such as those found in Estrogenex® 2nd Generation that bind to (inhibit) the action of sex hormone-binding globulin (SHB6), a transporter of sex hormones that normally binds about 97% of total testosterone rendering it incapable of providing its anabolic benefits. The more SHB6 that the compounds in Estrogenex® 2nd Generation bind up, the less available to bind to testosterone, thus leaving more testosterone in the free state. (A more detailed presentation of this activity is discussed hereafter.)

The hypothalamus itself cannot produce any sex hormones – instead it produces LHRH, or luteinizing hormone (LH) releasing hormone, also called GnRH (gonadotropin releasing hormone.) This then stimulates the pituitary gland.

The pituitary uses the amount of LHRH as one of its signals in deciding how much LH it should produce. Proper response depends on having sufficient receptors for LHRH. These receptors must be activated for LH to be produced. The pituitary also uses
sex hormone levels, both current and the past history, in deciding how much LH to produce. Some aspects of the pituitary’s behavior are peculiar.

For example, too much LHRH results in the pituitary down regulating LHRH receptors, with the result that very high LHRH production, which one would think should result in high testosterone production, actually lowers testosterone production. Another oddity is that while high estradiol levels inhibit the pituitary, still some estradiol is required to maintain a high number of LHRH receptors. So both very low and high levels of estradiol can inhibit LH production. LH produced by the pituitary then stimulates the testicles to produce testosterone. Here, the amount of LH is the main factor, and high levels of sex hormones do not seem to cause inhibition at this level.

Estrogenex® 2nd Generation is a nutraceutical that belongs in the class known as aromatase inhibitors. Estrogenex® 2nd Generation is manufactured and marketed by Hi-Tech Pharmaceuticals,Inc., which is a leader in the Muscle & Strength category of nutritional supplements. Estrogenex® 2nd Generation binds irreversibly to the aromatase enzyme through competitive inhibition. Competitive inhibition is a form of enzyme inhibition where binding of the inhibitor to the enzyme prevents binding of the substrate and vice versa.

Estrogenex® 2nd Generation -The Most Potent Aromatase Inhibitor Available!

Estrogenex® 2nd Generation is a multi-pathway formulation that helps to minimize, or eliminate, the undesirable effects associated with an estrogen dominant environment. Estrogenex® 2nd Generation helps to support the correct testosterone to estradiol ratios that yield the benefits associated with normal estradiol levels. Estrogenex® 2nd Generation acts as an anti-aromatase agent and is thus a powerful elevator of total testosterone and maximum liberator of free testosterone. Estrogenex® 2nd Generation
may also play a role in long-term selective estradiol blocking and/or inhibition of selective
estradiol signaling. Estrogenex® 2nd Generation may contribute to notable improvements
in muscular growth and fat loss, in addition to its wide array of health and anti-aging benefits.

Estrogenex® 2nd Generation is designed for:

• Normalization of all hormone levels, with specific tendencies toward testosterone dominance, in all aging males.
• Bodybuilders and athletes during and immediately after periods of anabolic steroid use for the purpose of stimulating endogenous testosterone production, and also as a standalone anabolic formulation to enhance endogenous free testosterone levels.

Testosterone: Free-Testosterone and Plasma Protein-Bound Testosterone

As previously mentioned, testosterone exists in the blood in either an active (free) or unbound state (+-2%) or inactive state bound to one of two proteins: sex hormone-binding-globulin (SHBG) (+-45%) or albumin (+-53%). Only when testosterone is in its free state can it directly interact with cellular receptors and exert its activity.

SHBG preferentially binds to testosterone over estrogen. Higher levels of SHBG in women help to maintain higher estrogen to testosterone ratios. Increased estrogen leads to an increase in SHBG. Thus, lowering the level of SHBG allows for an increased level of free testosterone. Obviously, if testosterone finds it more difficult to locate available plasma proteins in the presence of the additional compound, more will be left in an unbound state. The amount of free testosterone can be altered (increased) by the use of aromatase inhibitors (the less testosterone that is synthesized [aromatized] into estradiol, the more total testosterone) or inhibitors of the plasma proteins that bind into testosterone.

Manipulating the tendency of a testosterone to exist in an unbound state is an effective way to alter the overall activity and potency of one’s overall testosterone levels. Higher levels of testosterone produce an enhanced anti-glucocorticoid effect, which yields an anti-catabolic, or more precisely, anti-proteoolytic, effect on muscle cells. This indirect anabolic effect is the result of testosterone’s high affinity for binding with glucocorticoid receptors, thus blocking the normal messenger pathway that triggers protein release from muscle tissue.

More free testosterone also likely results in higher concentrations of IGF-1 and IGF-1 receptor sites in skeletal muscle tissue. Correspondingly, lower testosterone also likely yields less IGF-1 production and a corresponding decrease in IGF-1 receptor sites. Lower free testosterone also likely means a weaker immune system.

The Synthesis (Aromatization) of Testosterone to Estradiol in Males and the Significance of Maintaining Correct Testosterone to Estradiol Ratios

Although testosterone is considered to be a male hormone and estrogen a female hormone, both hormones exist in both males and females and serve important functions for both. Estrogen is a term that really represents a collection of female hormones, with estradiol predominating in men. Since estradiol is the estrogen that is normally in the highest concentration, it is an excellent marker for basic estrogen levels for that reason. At least three estrogens have multiple and overlapping functions.

Men obtain their estrogen through the action of the aromatase, which synthesizes (aromatizes) testosterone into estradiol. However, when concentrations of estradiol become too high and/or the normal ratio of testosterone to estradiol decreases, the potential for the development of undesirable conditions arises. As previously mentioned, this includes the development of the female breast tissue (gynecomastia), increased body fat and water retention. Also, research suggests that DHT and prostate tissue growth have a direct connection to above normal estradiol elevations and reduced testosterone levels.

The Estrogenex® 2nd Generation Mechanism of Action

The Estrogenex® 2nd Generation proprietary formula was developed by combining naturally occurring aromatase inhibitors and inhibitors of the action of SHBG. The primary active ingredients in Estrogenex® 2nd Generation are 6-bromoandrostenedione, indole-3-carbinol, coumesterol, quercitin and chrysin. Estrogenex® 2nd Generation does not exert its action through any direct hormonal or prohormonal activity (androgenic or estrogenic). Estrogenex® 2nd Generation also incorporates our proprietary delivery system called Extend-Rx®.

6-Bromoandrostenedione - 6-bromoandrostenedione binds to the aromatase enzyme making it unable to convert androgens to estrogen. Estrogenex® 2nd Generation contains two separate forms (isomers) that work to control and normalize estrogen and aromatase levels.

1. 6-alpha-bromoandrostenedione is a fast-acting competitive inhibitor of the aromatase enzyme. It works by binding to the aromatase enzyme to prevent it from aromatizing androgens. This is not a permanent binding and later acts to normalize aromatase (and thus estrogen levels) as hormone production returns to normal. It specifically targets aromatase and does not act as a central anti-androgen like some other post cycle products can. This means that your libido and mood will not be negatively affected.
2. 6-beta-bromoandrostenedione works in a similar way but has an irreversible and permanent effect. This works well to mediate excess aromatase, while the alpha isomer works to normalize the natural levels. The goal is again to transition into normal production levels for all hormones.

Chrysin - The flavonoid chrysin works to boost and preserve testosterone in two ways. First, through its anti-aromatase function and, second, by eliminating estrogen’s negative feedback loop. Aromatization or estrogen synthetase, is what is known as the conversion of testosterone into estrogen through the aromatase enzyme. Chrysin blocks the aromatase enzyme from converting testosterone into estrogen, thus allowing testosterone levels to remain high.

By stopping the aromatization of testosterone into estrogen, chrysin also encourages your body to produce more testosterone by eliminating the so-called “negative feedback” loop that would otherwise signal your body to stop or slow natural testosterone production. As has been discovered, your body uses estrogen levels as a sort of test to decide how much testosterone to produce. High estrogen levels means the testes will slow down or stop the production of testosterone. Low estrogen levels means it is time to turn up testosterone production. So, by reducing estrogen levels, chrysin fools the testes into producing more testosterone.

Coumesterol - In a study published in the Journal of Steroid Biochemical Molecular Biology, coumesterol and 10 other flavonoids were evaluated. The study tested the aromatase-inhibiting effects of these natural flavonoids (coumesterol, genistein, rutin, tea catechins, etc.) in human fat cell cultures. Coumesterol and chrysin were the most potent aromatase-inhibitors. Two recent studies have identified specific mechanisms by which coumesterol inhibits aromatase in human cells. These studies demonstrate that coumesterol is the most potent inhibitor of the aromatase enzyme of any phytoestrogen and other flavonoids that are known to have aromatase-inhibiting properties.

Indole-3-Carbinol (I3C) - Indole-3-carbinol (I3C) is a phytonutrient derived from the cruciferous vegetables of the Brassica genus (cabbage, broccoli, cauliflower and Brussels sprouts). I3C initiates a series of reactions in the body that culminates in the elimination of estrogen.

Directions

Take three tablets daily. Best taken near mealtime.

*These statements have not been evaluated by the Food and Drug Administration. This product is not intended to treat, cure, diagnose or prevent any disease.