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Increasing Growth Hormone with Peptides

Increasing Growth Hormone with Peptides

Increasing Growth Hormone with Peptides

 

There are many benefits for maintaining youthful levels of Growth Hormone (hGH). For detailed information on these benefits click here on Human Growth Hormone. Youthful Growth Hormone levels may be maintained by either using hGH supplementation or by stimulating its release from the pituitary gland with various peptides.

Brief Overview of Natural Growth Hormone Release

Growth hormone (hGH) secretion is controlled by a number of hormones:

(1) Somatostatin is an inhibitory hormone and prevents hGH release and is responsible in large part for the creation of hGH pulsation.

(2) Growth Hormone Releasing Hormone (GHRH) stimulates hGH release.

(3) Ghrelin which is a modulating hormone and in essence optimizes the balance between the “on” hormone & the “off” hormone.

GHRH – Growth Hormone Releasing Hormone

 

Growth Hormone Releasing Hormone (GHRH) is currently available in several forms which vary only by their half-lives. Naturally occurring GHRH is either a 40 or 44 amino acid peptide with the bioactive portion residing in the first 29 amino acids.

A shortened peptide with the bioactive portion of the first 29 amino acids of GHRH was made which is identical in behavior and half-life to that of GHRH and is called Growth Hormone Releasing Factor (GRF(1-29)), also known as Sermorelin. These both have a very short-half life measured in minutes which both require large doses to be effective.

To increase the half-life of Semorelin four amino acids were substituted which increased the half-life beyond 30 minutes which is more than sufficient to exert a sustained effect in order to maximize a GH pulse. This form is known as CJC-1295 (without DAC).

In an attempt to create an even longer lasting GHRH compound CJC-1295 was linked to a non-peptide molecule known as a “Drug Affinity Complex (DAC)” which created CJC1295 with DAC. This DAC complex allows it to bind to albumin in plasma and extends its half-life to that of days. This however is not desirable as it resulted in a continual GH bleed as it raises base levels of GH and creates a more ongoing pattern of release and not the natural pulsated release. This not desirable.

Therefore we recommend using CJC-1295 (without DAC) as a GHRH analog.

Ghrelin Mimetics – Growth Hormone Releasing Peptides

 

Before Ghrelin was discovered the synthetic growth hormone releasing peptides (GHRPs) were created and are superior to Ghrelin in that they do not share Ghrelin’s lipogenic behavior. These GHRPs are GHRP-6, GHRP-2, Hexarelin and later Ipamorelin all of which behave in similar fashion.

In the aging adult these GHRPs restore a more youthful ability to release GH from the pituitary as they turn down somatostatin’s negative influence which becomes stronger as we age and turn up growth hormone releasing hormone’s influence which becomes weaker as we age.

Growth Hormone Releasing Peptides (GHRP-6, GHRP-2, Hexarelin) are capable of creating a larger pulse of GH on their own then GHRH and they do this with much more consistency and predictability without regard to whether a natural wave or trough of GH is currently taking place.

As mentioned there are a number of GHRP’s some of which include Hexarelin, GHRP-2 and GHRP-6 which are listed from most potent to the least. The main side effects from these peptides is that they can adversely increase cortisol and prolactin levels. This side effect is most pronounced with the first two peptides listed which is why we favor GHRP-6 as it has the least side effects. In addition senitisation reactions are less prevalent with GHRP-6 when compared to the other peptides.

Synergy of GHRH + GHRP

 

It is well documented and established that the concurrent administration of Growth Hormone Releasing Hormone (CJC-1295) and a Growth Hormone Releasing Peptide (GHRP-6) results in synergistic release of hGH from pituitary stores.

Dosing GHRPs

Chronic use of GHRP-6 dosed several times a day every day will not cause pituitary problems, nor significant prolactin or cortisol problems, nor desensitize so is the analog of choice. For restoring youthful hGH levels once a day dose taken at night before bed is adequate.

Dosing GHRH analogs (CJC-1295)

The problem with using a GHRH analog alone is that they are only highly effective when somatostatin is low (the GH inhibiting hormone) and thus during a GH pulse or raising wave whereby the GHRH analog can add to this wave of release. If however you administer it in a trough (when a hGH pulse is not naturally occurring) you will add very little GH release.

The solution to this is to use it in combination with a GHRP-6 which is highly effective. The GHRP-6 creates a pulse or wave of hGH which the CJC-1295 can add to this causing even more hGH release thus the two working synergistically.

GHRP-6 creates a hGH pulse through several mechanisms. One mechanism is the reduction of somatostatin release from the hypothalamus, another is a reduction of somatostatin influence at the pituitary, still another is increased release of GHRH from the brain and finally it can act on the same pituitary cells (somatotrophs) as do GHRHs but use a different mechanism to increase cAMP formation which will further cause hGH release from somatotroph stores.

Protocol

To restore optimal hGH levels for its anti-aging benefits a once a day dose of GHRP-6 combined with CJC-1295 taken at night before bed is all you’ll need to restore youthful hGH levels. These are both best administered by subcutaneous injection.

Administration should ideally be done on either an empty stomach as fats and carbohydrates can blunt hGH release.

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MK-0677 shown to possess potent selective GH-secretory activity

Bodybuilding use of MK-0677 has shown a potent increase of GH within their system

 

The potential application of small molecules in GH therapy has recently become a topic of increasing interest. The spiroindoline  MK-0677,  the benzolactam L-692,429, and the peptides, GHRP-6 and
Hexarelin, have been shown to possess potent and selective GH-secretory activity in several species including human.

Moreover, MK-0677 being a synthetic GH secretagogues act on a signal transduction pathway distinct from that of GHRH. A specific high affinity binding site in porcine and rat anterior pituitary membranes that mediates the activity of these secretagogues has now been identified.

The binding affinity of these structurally diverse growth hormone secretagogues is tightly correlated with GH-secretory activity. The binding is Mg(2+)-dependent, is inhibited by GTP-gamma-S, and is not displaced by GHRH and Somatostatin.

The receptor is distinct from that for GHRH and has the properties of a new G-protein-coupled receptor. It is speculated that these GH secretagogues mimic an unidentified natural hormone that regulates GH secretion in concert with GHRH and Somatostatin.

What’s this all mean to the bodybuilder? MK-0677, L-692,429, and the peptides, GHRP-6 and Hexarelin, have been shown to possess potent GH activity in our bodies. By using them, we increase the growth hormone activity in our system.

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