Testosterone and testosterone receptors

[Dtlv74]

A nice article on testosterone:

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Increasing Testosterone and Testosterone Receptors

by naveen kumar

Optimizing testosterone secretion is especially important for natural bodybuilders. Proper training can increase the secretion, while over-training will reduce it to near zero.

An intense heavy squatting session can boost your testosterone secretion for several days. Even if you could somehow achieve a sky-high testosterone level, however, it wouldn’t guarantee fast muscle growth. The way the muscles “accept” the hormone is at least as important as how much your system has. The question is, Is it possible through proper training to maximize the impact of testosterone on your muscles?

Testosterone and Its Muscle Receptors

Various bodybuilding publications have recently featured articles stating that as a bodybuilder’s level of androgens increases, so does the level of testosterone receptors on his muscles. In other words, testosterone is said to be able to up-regulate its own receptors on the muscles. Needless to say, the more testosterone receptors you have, the more anabolic testosterone will be.

The result of the above reasoning is that it gives license to all sorts of excesses. Natural bodybuilders, who have a modest supply of testosterone, would, according to the theory, only have a limited number of testosterone receptors. Conclusion: They’ll be unable to accumulate a significant amount of muscle if they remain drug-free. They would, therefore, be limited in their muscle development by two factors:

1) Limited testosterone.
2) Limited impact of testosterone on the muscles due to a less-than optimum number of testosterone receptors.

So, based on the above reasoning, bodybuilders either have to use steroids or they are condemned to stay small forever. What’s more, the more anabolics they take and the longer they take them, the more significant the effect will be. Only massive amounts taken over a long period would give them the proper accumulation of testosterone receptors on the muscles. That’s supposedly the reason people grow more if they take more anabolics, because there are more receptors.

The good news is that the above theory is erroneous, not to mention dangerous and contrary to reality.

It’s dangerous because it promotes doping. It’s contrary to reality because one observes the opposite occurring among users of anabolics. Let’s look at this in terms of what you see in the gym.

First of all, if the theory were true, sedentary persons using androgens, for contraception, for example-would become huge. The extra testosterone would increase the number of testosterone receptors. The anabolic effect of testosterone would become increasingly stronger. In reality, untrained people who use steroids have very limited muscle growth. They rapidly become immune to testosterones anabolic effect. That doesn’t sound like an androgen receptor up-regulation, does it?

For the sake of argument, let’s say the above happens because the people
don’t use enough androgens. After all, the heaviest steroid users are found among bodybuilders. In those heaviest users there should be an up-regulation of androgen receptors. If that were true, here’s what would happen.

The androgens would cause their own receptors to multiply and get increasingly more potent as time went on. If androgen receptors were truly up-regulated that way, steroid users would get their best gains at the end of a cycle, not the beginning, and professional bodybuilders would get far more out of their cycles than first-timers. The trouble is, the best steroid gains are seen in the first cycles. The longer a course of treatment lasts, the more users are obliged to take drugs to compensate for the loss of potency. Besides, that’s the reason they do cycles in the first place. The time off is supposed to permit muscles to recover their natural responsiveness to testosterone.

Following the theory, there would be no need for training. As the doses were increased, the anabolic effects would be enhanced. In fact, drug users would be completely crazy to keep training while on a cycle when the steroids were going to do most of the work.

Androgen up-regulation would take place in every single muscle, not just in the exercised muscles. Consequently, a user of anabolics who only trained his arms should see his calves grow. That’s not the case, however, even for the professionals. I wish it were true, as they wouldn’t look so silly with their huge arms and puny calves.

I don’t have to keep demonstrating that the theory is just plain stupid. It is refuted daily by the experiences of bodybuilders who use anabolics, as well as by the research.

The fact is, excessive androgen levels induce the rapid loss of muscle testosterone receptors. There is absolutely no increase. The muscle fights the excess and immunizes itself against androgens, which is the reason steroids become less potent as time goes by.

The key point to remember is, only the trained muscles get bigger. The growth is determined by the numerous local alterations caused by muscular contractions, not a systemic circulating factor.

While this discussion may seem far removed from natural bodybuilding, it has important implications for everyone who trains. As suggested above, if the theory of testosterone-receptor up-regulation were true, there’d be no way a natural bodybuilder could ever get big.

cont...

[Dtlv74]

part 2

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Testosterone and Training

Obviously, testosterone is a hormone that makes the muscle grow, and the body will use all the anabolIc hormones at its disposal to respond to a bodybuilder’s training. Therefore, the training has a significant impact on testosterone, which can occur in one of two ways.

1) It increases the level of testosterone. It’s true that training, if it’s intensive and brief, will raise the level of testosterone, but never as much as one might wish. What’s worse, if you train too much, the level of testosterone really falls. If training increased the level of testosterone enormously, all bodybuilders would be covered with pimples and would have prostate problems. In short, we’d all resemble users of anabolics and we’d suffer from all those side effects. That’s the reason proper training can boost testosterone secretion but not in excessive amounts.

One solution to the above dilemma would be to stimulate the secretion of testosterone in the trained muscle itself. That would allow the stimulated muscles to be flooded with testosterone while other organs would still be exposed to a normal testosterone level. Muscle growth would occur without any side effects of testosterone. Unfortunately, testosterone is not a paracrine or autocrine hormone. It is an endocrine hormone, and only the testicles (or the ovaries in women) and the adrenal glands can make it.

2) It increases the sensitivity of the muscle to testosterone. The body is ready for everything. Rather than increasing the level of testosterone significantly, training will increase the sensitivity of the trained muscle to testosterone. In other words, proper training can force your stimulated muscles to suck up all the blood testosterone. How do you make that happen? Simply by increasing the number of testosterone receptors in the muscle that you train. As a result, a normal level of testosterone will have a normal effect on your organs, since the number of testosterone receptors there doesn’t change. As the number of testosterone receptors in the trained muscle increases, however, the hormone’s effects will be multiplied.

That brings us to the million-dollar question: How do you increase the number of testerone receptors? There’s a lot to be said on that subject, but here are some highlights.

Testosterone Receptors and Negative Reps

It seems clear that negative-accentuated training lowers the sensitivity of the muscle to testosterone, at least in the short term. So while that type of training will trigger the anabolism of fibroblast growth factor, insulinlike growth factor 1 and the satellite cells, it will also reduce the impact of the anabolism of testosterone. A few days after the damage occurs, the number of testosterone receptors will be increased; however, for some days at least the testosterone will lose its effects on the muscle. There are three possible reasons for this:

1) Destruction of the testosterone receptors.
2) Inactivation of the receptors, they don’t respond to the signals that are sent to them anymore.
3) A little of both effects described above. This will slow the muscular recuperation, providing another reason to avoid doing pure negative repetitions too often on the same muscle.

Testosterone Receptors and Positive Reps

Positive repetitions will have the most beneficial effects on the proliferation of the testosterone receptors in the trained muscle. The big problem is that although training a muscle specifically to increase the receptors will in fact increase their number, it will also cause a decline in the level of testosterone in the natural bodybuilder. So we face an unavoidable trade-off: training enough to increase the number of testosterone receptors without training too much, causing the level of testosterone to collapse. That’s not an easy equilibrium to find.

Taking anabolics doesn’t solve the problem either. Users of anabolics certainly have elevated levels of androgens, but they have very few testosterone receptors in their muscles. If they could combine the two conditions, it would not take more than a year to acquire a physique of Olympia caliber.

The paradox for natural bodybuilders is that they have plenty of receptors but not enough testosterone. Therefore, their training should be oriented toward the restoration of the level of this hormone first and then to the up-regulation of the receptors. They should also consider using testosterone precursos, such as androstenedione.

Users of anabolics, on the other hand, have more androgens than they need, so their training should be oriented exclusively toward reopening the testosterone receptors. Anabolics users don’t fear a reduction of the level of testosterone, since they control it artificially. That has an important consequence: Naturals and non-naturals certainly have the same overall objective, to build muscle, but they have training objectives that are diametrically opposed. One group needs more testosterone, the other needs more receptors. Each group needs what the other has, which is the very reason that the first cycle of anabolics has the most effect. It’s the only time there are simultaneously plenty of receptors and hormone. Meanwhile, there’s only one obvious conclusion that everyone can agree on: Natural bodybuilders shouldn’t train like the champions or even like the biggest guys in the gym.

[Bison]

Good post.

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Natural bodybuilders shouldn’t train like the champions or even like the biggest guys in the gym.

This is why I don't pay any attention to people who use steroids, not through lack of respect or anything but they're playing a whole different ball game. Different rules completely.

[Dtlv74]

Another good article on testosterone in general with some practical recommendations for the natural:

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Natural Ways To Increase Testosterone Bioavailability In Athletes

by Ivan Nikolov

Being a natural athlete I’ve always sought to find more ways to increase testosterone levels naturally. The question I’ve always asked myself was what are the variables, which determine how much testosterone is boiavailable.

I’ve read articles before, giving some advice on what in my every day life causes my test levels to go up and what causes them to go down. But after an extensive research I couldn’t find an article, explaining in detail how and actually what exactly I should manipulate directly in my system to achieve the effects I desired – namely not only higher levels of circulating testosterone but also how much of it will be available to the corresponding receptors in the cell walls. Moreover, I wanted to know all this in regards to natural bodybuilding…

So, I decided to do some good digging and reading and then if I manage to put things together, to lay that in writing form so that others can benefit as well.

Without wasting even a minute more I will start this off by describing what testosterone is and what it does in the human body. Testosterone is a steroid hormone with anabolic and androgenic properties. It is the main hormone, responsible for the increase in lean muscle tissue, increased libido, energy, bone formation, and immune function.

Testosterone is secreted in the testes in men and in the ovaries in women. Small amounts are also secreted in the adrenal glands. Testosterone is derived from cholesterol. The levels of testosterone in men range between 350 and 1,000 nanograms per deciliter (ng/dl). After the age of 40 these normal levels start dropping by roughly 1 per cent a year.

In the blood stream testosterone circulates in great percentage bound to so called binding proteins. Sex Hormone Binding Globulin or SHBG is the one that concerns us the greatest. Why? Because this is the main reason why testosterone might not be available to reach the cell receptor. When testosterone gets attached to SHBG, it is no longer able to perform its anabolic functions.

What elevates SHGB: Anorexia nervosa, Hyperthyroidism, Hypogonadism (males), Androgen insensitivity/deficiency, Alcoholic hepatic cirrhosis (males), Primary biliary cirrhosis (females).
What suppresses SHGB: Obesity, Hypothyroidism, Hirsutism (females), Acne vulgaris, Polycystic ovarian disease, Acromegaly, Androgen-secreting ovarian tumors

Less than 1% of the circulating testosterone is in a free form in males (less that 3% in females). Only when in a free form this hormone can exhibit its properties by connecting to the androgen receptors on the cell walls. Based on a study 14 to 50 per cent of the testosterone is bound to SHBG in males and 37 to 75 in females. It is worth mentioning that SHGB poses very high affinity for binding to testosterone. Therefore, changes in the SHGB levels noticeably influence the level of bioavailable testosterone.

Let’s discuss for a moment what exactly a testosterone bioavailability is. Other than SHGB there are two more testosterone-binding proteins, also called carriers. One of them is albumin. It is a low-affinity binding protein, thus testosterone bound to it is considered “bioavailable”. Albumin binds to testosterone in the range 45 to 85 per cent in men (25 – 65 in women). The third carrier is the cortisol binding globulin, which binds also with low-affinity to less that 1 % of the testosterone in circulation.
The free androgen index (FAI) indicates the amount of bioavailable testosterone. FAI is the sum of the free testosterone and the albumin and cortisol binding globulin. Or it’s the total serum testosterone minus the SHGB-bound testosterone.

It is now clear why we should focus our attention on the properties of SHGB. The levels of this binding protein increase when there is excess estrogen present. Conversely, SHGB levels drop if the testosterone levels are elevated. Here I should mention the fact that SHGB exhibits higher affinity to testosterone than to estrogen. Now, pay close attention…
It’s a well-known fact that testosterone is an estrogen precursor – it will convert to estrogen under the influence of the enzyme aromatase. Nothing that we don’t know so far. Here is where it gets interesting. Suppose that we have normal testosterone levels and we don’t suffer from any of the health ailments, which influence the SHGB levels. That means that SHGB levels are normal, too.

Bare with me now. If more of this testosterone is converted to estrogen due to abnormal aromatase levels, the SHGB I will increase as well. SHGB, being more readily bound to testosterone, will leave us with excess estrogen levels in the system, which in turn will stimulate increased production of the SHGB protein from the liver. This whole process ultimately amplifies estrogen levels. Estrogen readily binds to the androgen receptors in cells thus leaving less opportunity for the free testosterone. Even more important, estrogen is the messenger molecule that signals the brain to decrease testosterone production.

Another thing of great importance is the fact that over 40 per cent of the SHGB protein circulates unbound in the blood stream in man (over 80 per cent in women), and albumin circulates unbound almost all of the time. Thus increase in the total testosterone levels does not produce any noticeable changes in the free testosterone levels unless there is a significant increase like the one seen after synthetic steroid hormone administration.

Well, this whole story brings us to the conclusion that the main approach should be - to keep the testosterone bioavailability high.
In this regard a natural athlete should strive to:

· Prevent testosterone levels from getting low
· Attempt to increase the total testosterone as a means of keeping the testosterone levels from plunging
· Block the testosterone-binding effects of SHBG
· Lower the levels of the enzyme aromatase - less testosterone conversion to estrogen

cont...

[Dtlv74]

part 2

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Natural Ways To Increase Testosterone Bioavailability In Athletes

1. How to prevent testosterone levels from getting low?

- Avoid obesity. Based on the way the testosterone-estrogen mechanism works, increased levels of estrogen will ultimately decrease the circulating testosterone. Excess fat causes more estrogen production due to the fact that fat cells are those, which manufacture estrogen. So, the more fat cells, the more estrogen in the blood and the less testosterone.

- Drug and alcohol abuse. Alcohol has the property to inhibit your ability to remove estrogen from the blood stream by acting as a central nervous system depressant and also by decreasing zinc levels.

- Stress elevates corticosteroid levels in the blood steam, which causes the testosterone levels to decrease.

- Medications. Some medications, including estrogen and progesterone, lower the lutenizing hormone (LH) levels. LH is the hormone, responsible for the steroid hormones production.

- Diabetes. Studies suggest that there is a link between type 2 diabetes and lower testosterone levels.

- Hypertension and high cholesterol levels. These both cause the arteries to harden, this way decreasing the blood flow to the sex hormone producing organs. That of course leads to low sex hormone levels.

- Aging. Fact is after the age of 40 test levels drops by roughly one per cent per year. We can’t do too much about that. The clock keeps ticking for all of us. However, we can try to manipulate testosterone levels in any other possible way.

- Low fat diet. Low fat consumption causes increase of the SHGB, which means one thing – less free testosterone. It is considered that monounsaturated fats play an important role in testosterone levels and bioavailability.

- Overtraining can contribute to as much as 40 per cent drop in testosterone levels. That is why it’s important to notice early the signs of overtraining and give the body a week or two well-deserved rest.

- Not enough sleep. If you are not getting enough sleep the body is not recuperating well, which causes less testosterone and more corticosteroids to be released. Just to mention corticosteroids like cortisol are in fact catabolic hormones meaning they use up muscle tissue to provide the brain and the heart with energy.

- Vitamin C. It suppresses the release of the stress hormone cortisol. Cortisol decreases testosterone levels. So, ultimately less cortisol, more testosterone.

2. How to boost testosterone levels

- Incorporate basic movements that involve several muscle groups in your training routine. Good ones are squats, dead lifts, and military presses. Basic (compound) exercises have been shown to play an important role in the testosterone levels.

- The greatest workout related testosterone production occurs with the use of heavier weights and lower rep range. A study shows that the best is 85 per cent of your one-rep max.

- Tribulus terestris is a natural supplement, which has been shown in some studies to have the ability to increase the leutenizing hormone (LH) levels. As we already mentioned above, one of the functions of LH is to stimulate testosterone production by the testes.

3. Block the testosterone-binding effects of SHBG

- Nettle root as a highly concentrated extract has shown to be effective at binding to SHBG and therefore it permits more free testosterone to circulate the system. It also acts as a 5-alpha reductase inhibitor. This is the enzyme, responsible for the conversion of testosterone to dihydrotestosterone (DHT), a more potent form of the male sex hormone, which causes prostate enlargement and ultimately cancer. Methanolic extract of nettle can also cut down the SHBG levels, which is another form of elevating the free testosterone in the blood stream.

- Pygeum (prunus africana) is another herb, known to block the testosterone-binding effects of SHBG. Nettle root and pygeum extracts also benefit the prostate gland as a preventive treatment for benign prostatic hyperplasia (BPH) both by blocking the 5-alpha reductase action.

- Avena Sativa is an extract from the straw of oats. It has somewhat different properties. It works by freeing bound testosterone, which increases the free testosterone in circulation.

4. Lowering aromatize levels

- Zinc. The mineral zinc inhibits the aromatase enzyme that converts testosterone into excess estrogen. The recommended dose for inhibiting aromatase is 80mg daily. However, be sure the combined zinc quantity of all the daily supplements you are taking does not go over this benchmark.

- Chrysin is a bioflavonoid that has shown a potential as a natural aromatase inhibitor. Chrysin is poorly absorbed in the system. It is found that when taken along with piperine, chrysin exhibits a lot better absorption. Supplementation with chrysin and piperine together might bring good results in reducing aromatase levels.

How does this all apply to the sport of natural bodybuilding?

Let’s assume you are an individual, who exercises regularly and who doesn’t consider taking exogenous steroid hormones. With other words you are a natural athlete or enthusiast, who desires to keep his natural testosterone levels in the range, favoring good health and lean muscle mass build up.
Here is what you do:

1. If you are even slightly overweight consider staring immediately a diet and training routine, tailored toward fat loss and lean muscle retention.

2. Consider also dropping the alcohol intake to absolute minimum if you want your efforts in keeping test levels high to give results.

3. Begin mastering some types of self-control or even meditation. These will take care of the excess stress levels.

4. Take medications only if they are absolutely essential for your health and are prescribed by your doctor. Talk to your personal physician to find out if there are any natural remedies to replace your current medications and if he recommends such approach for your health issue.

5. Keep your blood pressure and the serum cholesterol in check.

6. Eat enough good fats in your diet. Good means monounsaturated and omega-3 and 6 polyunsaturated fats.

7. Don’t ever overtrain. Sleep enough to promote good recovery. Signs of overtraining are loss of appetite, tiredness and irritability, lack of motivation, impaired mental focus, prolonged recovery periods.

8. Start relying more heavily on basic exercise movements. Train in the low rep range most of the time. 5 – 8 reps will ensure that you’re using weights that will eventually stimulate elevated testosterone levels.

9. It will only do you good if you decide to try some or all of these natural supplements: chrysin - piperine blend, nettle root extract, pygeum, avena sativa extract, and tribulus terestris. Try to find them in your local health store. Follow the directions for best results.

10. And you shouldn’t even consider training without supplementing your diet with enough vitamin C (at least 1g a day) and zinc (15mg min.). Take vitamin C with your multivitamin formula after breakfast, and post-workout with your protein shake. Zinc should be present in your multivitamin blend but this is not enough. Take zinc with magnesium in the form of ZMA right before you go to bed on an empty stomach.

[Dtlv74]

References for study above:

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References:
Ron Geraci, Men's Health, December 25, 2000; 13 Ways to Naturally Boost Your Testosterone Levels
LE Magazine January 2000; Replenish Testosterone Naturally Plant extracts favorably alter hormone metabolism and improve sexual desire in men
Jennifer A. Kelly, Ph.D. and Leo Vankrieken, Eur. Eng. Diagnostic Products Corporation; Sex Hormone Binding Globulin and the Assessment of Androgen Status
****atoo.com; Avena Sativa - are oats an aphrodisiac?
Gabe Mirkin, M.D.; High Cholesterol Causes Low Testosterone
Bodybuilding.com, Chrysin Info And Products - Block Estrogen, Increase Testosterone

[Dtlv74]

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Good post.

This is why I don't pay any attention to people who use steroids, not through lack of respect or anything but they're playing a whole different ball game. Different rules completely.

Spot on Bison. I have nothing against roid users but it's not my game personally, and there are definite differences in the way someone responds to things when on them. A mate of mine has started with them fairly recently and, of the people I know who are around my age and train, myself and one other guy are the only ones not taking them... and so I've seen first hand how different the game gets.

[kp1512]

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Less than 1% of the circulating testosterone is in a free form in males (less that 3% in females). Only when in a free form this hormone can exhibit its properties by connecting to the androgen receptors on the cell walls. Based on a study 14 to 50 per cent of the testosterone is bound to SHBG in males and 37 to 75 in females. It is worth mentioning that SHGB poses very high affinity for binding to testosterone. Therefore, changes in the SHGB levels noticeably influence the level of bioavailable testosterone.

I think that may be wrong.....

Doesnt 98% bind to SHBG and 2 percent for other uses?..Hence why you want to reduce SHBG ......

KP

[Dtlv74]

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I think that may be wrong.....

Doesnt 98% bind to SHBG and 2 percent for other uses?..Hence why you want to reduce SHBG ......

KP

You could well be right kp - I don't know myself. The author says that was "Based on a study", so I'm guessing different studies may have shown some different results...

[Tartulho]

97-99% of testosterone is binded to sex hormone
binding globulin (a.k.a. SHBG), albumin and cortisol binding globulin (a.k.a. CBG). The amount that is binded to the last is negligible, the amount binded to the others fluctuates depending on the study