GABAergic modulation for the best possible PCT



Steroidology members,

12 months ago, Primordial Performance brought Sustain Alpha to the market as a testosterone boosting topical cream. Since then, this completely legal topical cream has swarmed the market, exceeding virtually all expectations.

Natural athletes use Sustain Alpha to boost testosterone and reap the benefits from enhanced testosterone levels. For Post Cycle Therapy (PCT), men shun Clomid & Nolvadex for Sustain Alpha to restore testosterone levels faster than ever before. Most importantly, blood tests from actual customers have proven Sustain Alpha to be just as effective as Clomid or Nolvadex for PCT, without the side effects.

It’s no surprise that Sustain Alpha is so effective. The active ingredients are delivered with an advanced topical delivery cream that pulls them through the skin and straight to the blood stream. Once in the blood, they are carried to the brain – right where they start triggering the testes to produce testosterone like a fountain of youth.

Speaking of the triggering testosterone production, How does Sustain Alpha work?

It’s well known, that the main ingredients in Sustain Alpha – resveratrol and 7,8-benzoflavone – are natural anti-estrogens. However, both of these compounds have proven to be very mild anti-estrogens as blood tests have revealed that Sustain Alpha only has a minor effect on total estrogen. (not even close to the aromatase inhibition of a pharmaceutical like Arimidex)

But that’s ok; Sustain Alpha was never intended to crush estrogen levels. Extremely low estrogen can reduce libido, inhibit recovery, and hurt cholesterol health.

So the question is…

If Sustain Alpha isn’t significantly inhibiting estrogen, then how exactly is it significantly increasing LH, FSH and natural testosterone levels?

It’s because Sustain Alpha is working by other mechanisms besides estrogen modulation.

Before jumping into the science, here is a brief background on hormone production -

Basic Hormone Production
The Hypothalamic Pituitary Testicular Axis (HPTA)

In a normal healthy male luteinizing hormone (LH) and follicle stimulating hormone (FSH) are sent from the brain (the pituitary) to stimulate the testes to make testosterone and sperm.

The release of LH & FSH from the pituitary is stimulated by Gonadotropin Releasing Hormone (GnRH) from the hypothalamus. The hypothalamus is stimulated to produce GnRH when it senses low levels of steroid hormones, such as testosterone and estrogen. (hypothalamus [GnRH] --- > pituitary [LH & FSH]--- > testes [testosterone])

On the other hand, when the brain detects high levels of steroid hormones it suppresses the release of GnRH, LH & FSH, and eventually testosterone production. This is called the negative feedback loop – the normal daily rhythm of hormone production.

Traditionally, boosting LH & FSH to stimulate testosterone involved the use of a Selective Estrogen Receptor Modulator (SERM) to directly block estrogen at the receptor (eg, Clomid & Nolvadex) or inhibition of estrogen formation by blocking the aromatase enzyme with aromatase inhibitors (eg, ATD, 6-bromo, formestane, Aromasin, Letrozol, ect).
Now on to the exciting part…

Recently, it has been found that the main ingredient in Sustain Alpha – the naturally occurring flavone 7,8-Benzoflavone -- increases testosterone production by preventing the negative feedback of testosterone and estrogen on the hypothalamus through GABAergic modulation. (1-10)

That’s right, GABAergic modulation, but please let me explain before jumping out of your seat.



As you may know, γ-amino-butyric acid (GABA) is an inhibitory neurotransmitter known to play an important role in sleep, learning, memory and pain sensation. In fact, GABA supplements are often used to promote relaxation and sleep. However, the GABAergic system is a tremendously complex family of receptors which interact not only with GABA, but hundreds of other neuro-active chemicals all throughout the body.

The important thing to understand here is that GABA and GABAergic transmission are two separate things.

With that in mind, researchers are just beginning to understand how the GABAergic system regulates the hypothalamus and GnRH secretion.

So far, it’s been established that there is no androgen receptor (AR) or estrogen receptor (ER) on GnRH releasing neurons. This is fascinating, because it means that steroid hormones such as testosterone and estrogen must communicate with GnRH neurons through intermediaries. Meaning, steroid hormones must signal the release of certain neurotransmitters to suppress GnRH secretion in the hypothalamus. One of the neurotransmitter systems involved in this communication process is the GABAergic system.

As you can imagine, if the neurotransmitters can be blocked or antagonized, then suppression from steroid hormones can be reduced. This would allow the hypothalamus to continue secreting GnRH, the pituitary secreting LH & FSH, and the testes secreting testosterone.

Fortunately, Sustain Alpha has the perfect ingredient for this -- 7,8-benzoflavone.

7,8-benzoflavone is a neuro-active flavone that can pass the blood brain barrier and bind to the GABAergic receptors that modulate GnRH release. (1-10) In fact, animal studies have already shown 7,8-benzoflavone can prevent the drug related decline in LH, FSH and testosterone production. (2-4) By interacting with the GABAergic receptors, 7,8-benzoflavone is able to offset hypothalamic suppression of GnRH from steroid hormones.

So what does this mean for a guy wanting to boost testosterone?

This means LH & FSH levels can be boosted quickly and effectively without overly suppressing estrogen and sacrificing sexual health. This means Sustain Alpha is perfect for any PCT, or any male wishing to optimize his “male performance” with higher testosterone levels. This also means that Sustain Alpha is unlike anything else on the market.

There is one factor that will keep you from getting maximum gains from Sustain Alpha, and that is testicular sensitivity.

Let me explain…

No matter how much LH & FSH is secreted, the testes won’t secrete testosterone if they are desensitized to LH & FSH. (which can happen from too much, or not enough stimulation)

Therefore, maintaining testicular sensitivity is critical, and this is precisely what Toco-8 was designed for.



Toco-8 is a powdered tocotrienol supplement proven to increase testicular sensitivity. When taken with Sustain Alpha, a powerful synergy occurs. By increasing testicular sensitivity, Toco-8 makes Sustain Alpha 3-4x more effective, thus allowing the body to produce more testosterone than it ever could before. Research has also proven that Toco-8 can increase the effectiveness of hCG by the same mechanism. Consider Toco-8 the beginning of a great testicular awakening – critical for a strong testosterone response to LH & FSH stimulation.

Make no mistake, this is one of the most powerful testosterone simulating stacks on the market, but don’t take my word for it. Jump on Google or any major bodybuilding forum and put in a search -- you will see Sustain Alpha and Toco-8 are the “real deal”, backed by thousands of positive reviews from actual users.

Yours in health & fitness,

Eric Potratz (Pp)
Primordial Founder & President


Questions?

Phone – 1-800-568-2924
Email - info@primordialperformance.com
Visit - Primordial Performance


References -

1. Neuroactive flavonoids interacting with GABAA receptor complex.
F Wang, M Shing, Y Huen, SY Tsang, and H Xue
Curr Drug Targets CNS Neurol Disord, Oct 2005; 4(5): 575-85.

2. Prevention of chronic alcohol and nicotine-induced azospermia, sterility and decreased libido, by a novel tri-substituted benzoflavone moiety from Passiflora incarnata Linneaus in healthy male rats.
K Dhawan and et al.
Life Sci, Nov 2002; 71(26): 3059-69.

3. Passiflora: a review update.
Dhawan K, Dhawan S, Sharma A.
J Ethnopharmacol. 2004 Sep;94(1):1-23. Review.

4. Drug/substance reversal effects of a novel tri-substituted benzoflavone moiety (BZF) isolated from Passiflora incarnata Linn. – a brief perspective.
Dhawan, et al.
Addiction Biology 379-386

5. A gamma-aminobutyric acidB agonist reverses the negative feedback effect of testosterone on gonadotropin-releasing hormone and luteinizing hormone secretion in the male sheep.
Endocrinology. 2000 Nov;141(11):3940-5.

6. Anticonvulsant effects of aerial parts of Passiflora incarnata extract in mice: involvement of benzodiazepine and opioid receptors.
Nassiri-Asl M, Shariati-Rad S, Zamansoltani F.
BMC Complement Altern Med. 2007 Aug 8;7:26.

7. Effects of Dialyzing γ-Aminobutyric Acid Receptor Antagonists into the Medial Preoptic and Arcuate Ventromedial Region on Lutienizing Hormone Release in Male Sheep.
Suzie A, et al.
Biology of Reproduction 58, 1038-1046 (1998)

8. Antiandrogen Microimplants into the Rostal Medial Preoptic Are Decrease γ-Aminobutyric Acidergic Neuronal Activity and Increase Luteinizing Hormone Secretion in the Intact Male Rat.
David R et al.
Endocrinology, Vol. 137 No. 10 (1996)

9. Non-classical estrogen modulation of presynaptic GABA terminals modulates calcium dynamics in gonadotropin-releasing hormone (GnRH) neurons.
Nicola Romano, et al.
Endocrinology, 10.1210/en.2008-0424 (2008)

10. Restoration of the Luteinizing Hormone Surge in Middle-Aged Female Rats by Altering the Balance of GABA and Glutamate Transmission in the Medial Preoptic Area
Genevieve S, et al.
Biol Reprod, Jul 2008; 10.1095/biolreprod.108.069831.
 
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For Post Cycle Therapy (PCT), men shun Clomid & Nolvadex for Sustain Alpha to restore testosterone levels faster than ever before. Most importantly, blood tests from actual customers have proven Sustain Alpha to be just as effective as Clomid or Nolvadex for PCT

give me a break.
info like this can be dangerous.

pct with sustain alpha and toco-8 is like trying to do post cycle therapy (pct) with red wine and vitamin-e

the studies provided on your own website use generic vitamin-e anyway and are done on vitamin-e deficient subjects

9. Effect of Vitamin E on Function of Pituitary-Gonadal Axis in Male Rats and Human Subject
Fumio et al
Endocrinology, Japan. 29(3) 287-292 (1982)

10. Functional and morphological studies on pituitary-gonadal, and adrenal axes in vitamin E deficient and supplemented male rats.
Umeda, et al.
Fukuoka acta Med. 69, 327-337

11. The effects of vitamin E deficiency on some enzymes of steroid hormone biosynthesis.
Barnes, et al.
Int J. Vit. Nutr. Res. 45, 369-403

in an earlier thread you concluded (with your own "lab results") that after sustain alpha and toco-8 post cycle therapy (pct) LH and FSH levels were reduced claiming its a good thing but now you claim them to be raised.

You will also notice a reduction in LH/FSH. This shows that his testes where sensitized to the effects of the LH/FSH and where able to make more testosterone with less stimulation.
 
give me a break.
info like this can be dangerous.

post cycle therapy (pct) with sustain alpha and toco-8 is like trying to do post cycle therapy (pct) with red wine and vitamin-e

the studies provided on your own website use generic vitamin-e anyway and are done on vitamin-e deficient subjects.

Plenty of customers no longer use Clomid or Nolva for post cycle therapy (pct) and feel that they recover better with Sustain and Toco-8. Remember, these guys are also using hCG during or after the cycle. We always advise the use of hCG during the cycle. If you do this recovery is much easier.

in an earlier thread you concluded (with your own "lab results") that after sustain alpha and toco-8 post cycle therapy (pct) LH and FSH levels were reduced claiming its a good thing but now you claim them to be raised.

That quote was noting the decline in LH & FSh levels from the baseline pre-cycle levels. [not really in the same context as the original post, but I will explain…]

That particular user had never used a pro-hormone or steroid prior to the first blood test, which showed low testosterone levels even with high LH & FSH levels. This shows he had reduced sensitivity to LH & FSH.

See the whole thread here -
http://www.steroidology.com/forum/a...s-sustain-alpha-post cycle therapy (pct).html

The Sustain Alpha and Toco-8 post cycle therapy (pct) improved his LH:Testosterone ratio. If you can increase Total Testosterone and reduce circulating LH & FSH levels then you are increasing testicular sensitivity. [assuming you aren’t using an exogenous source of test]

Plus, the final blood test was taken 4 weeks after he had discontinued the Sustain Alpha, so any boost in LH & FSH would be gone. [however he still was maintaining higher than normal testosterone levels with lower LH & FSH levels]

Now, for an individual going into post cycle therapy (pct) who has non-existent LH/FSH levels – Sustain Alpha will boost these levels and thus stimulate testosterone. At the same time Toco-8 will be promoting a stronger response to LH & FSH in the testes by promoting testicular sensitivity. Once natural Testosterone levels begin to return, you will be able to maintain this with an overall lower level of LH & FSH.

-Pp
 
Another thing too….

Older men with low testosterone levels generaly have high circulating LH levels, but disorderly and washed out spikes in LH. In other words, older men have consistently high LH & FSH, while younger men produce more defined “peaks and drops” in LH & FSH and maintain higher testosterone with less overall LH & FSH levels.

Therefore, for the highest testosterone response from the testes its desirable to have strong, precise bursts of LH & FSH.

One possible mechanism for Toco-8 increasing testicular sensitivity is by promoting a stronger more defined burst in LH & FSH from the pituitary gland by supporting higher concentrations and more buildup of LH & FSH in the pituitary. This is a good thing, since the testes respond best to sharp spikes in LH & FSH. [they can become desensitized to consistently heightened LH & FSH levels.]

-Pp
 
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