Tag Archive for Growth Hormone Releasing Hormone

Basic guide to using CJC-1295 & GHRP-6

What is growth hormone?

Synthetic Growth Hormone is an artificially created hormone “identical” to the major naturally produced (endogenous) isoform. It is often referred to by its molecular mass which is 22kDa (kilodaltons) and is made up of a sequence of 191 amino acids (primary structure) with a very specific folding pattern that comprise a three-dimensional structure (tertiary structure). This tertiary structure is subject to potential shape change through a process known as thermal denaturation. While many labs are capable of generating growth hormone (GH) with the proper primary structure not all will be capable of creating a tertiary structure identical to the major naturally occurring growth hormone. The tertiary structure can determine the strength with which the growth hormone molecule binds to a receptor which will in turn affect the “strength” of the intracellular signaling which mediates the events leading to protein transcription, metabolism, IGF-1 creation, etc. It is this inconsistency that accounts in part for the differences in effectiveness of various non-pharmaceutically produced synthetic growth hormone.

Naturally produced Growth Hormone is produced in the anterior pituitary and to a far lesser extent in peripheral tissue. It is made up of a blend of isoforms the majority of which is the 22kDa (191 amino acid) variety with which most are familiar. In addition an isoform that is missing the 15 amino acids that interact with the prolactin receptor is also produced. This form is known as 20kDa and although it binds differently to the growth hormone receptor it has been shown to be equally potent to 22kDa. It appears that 20kDa has lower diabetogenic activity then 22kDa. The pituitary releases a blend of these two isoforms with 20kDa averaging perhaps 10% of the total although this percentage increases post-exercise. Currently there is no synthetic produced for external administration for this isoform.

Growth hormone (GH) in the body is released in pulsatile fashion. It has been demonstrated that this pattern promotes growth. The pituitary is capable of rather quickly synthesizing very large amounts of growth hormone which it stores large amounts in both a finished and unfinished form. Adults rarely experience GH pulses (i.e. releases of pituitary stores) that completely deplete these stores. As we age we do not lose the ability to create and store large amounts of growth hormone. Rather we experience a diminished capacity to “instruct” their release. The volume of GH that is released can not be properly equated to the exogenous administration of synthetic GH for the reason that a set of behavioral characteristics accompany natural GH that differ from those of synthetic GH. Among those characteristics are concentrated pulsatile release which upon binding in mass to growth hormone receptors on the surface of cells initiate signaling cascades which mediate growth events by translocating signaling proteins to the nucleus of the cell where protein transcription and metabolic events occur.

These very important signaling pathways desensitize to Growth Hormone’s initiating effects and need to experience an absence of Growth Hormone in order to reset and be ready to act again. The presence of GH released in pulsatile fashion is graphed as a wave with the low or no growth hormone period graphed as a trough. Therefore attempting to find a natural GH to synthetic GH equivalency is not very productive because in the end what is probably import is:

- the quantity & quality of intracellular signaling events; and
– the degree to which GH stimulates autocrine/paracrine (locally produced/locally used) muscle IGF-1 & post-exercise its splice variant MGF.
Synthetic GH versus Natural GH in IUs

An attempt has been made on my part and can be found at:

#8 – Growth Hormone Administration vs. CJC-1295/GHRP-6 + GHRH (part I of II)

#9 – Growth Hormone Administration vs. CJC-1295/GHRP-6 + GHRH (part II of II)
Rather than demonstrate absolute values this comparison articles should serve to demonstrate that the body can produce pharmacological levels of growth hormone.

Brief overview of natural GH release

The initiation of growth hormone release in the pituitary is dependent on a trilogy of hormones:

Somatostatin which is the inhibitory hormone and responsible in large part for the creation of pulsation;

Growth Hormone Releasing Hormone (GHRH) which is the stimulatory hormone responsible for initiating GH release; and

Ghrelin which is a modulating hormone and in essence optimizes the balance between the “on” hormone & the “off” hormone. 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 Ghrelin-mimetics or the 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.

The exogenous administration of Growth Hormone Releasing Hormone (GHRH) creates a pulse of GH release which will be small if administered during a natural GH trough and higher if administered during a rising natural GH wave.

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.

Synergy of GHRH + GHRP

It is well documented and established that the concurrent administration of Growth Hormone Releasing Hormone (GHRH) and a Growth Hormone Releasing Peptide (GHRP-6, GHRP-2 or Hexarelin) results in synergistic release of GH from pituitary stores. In other words if GHRH contributes a GH amount quantified as the number 2 and GHRPs contributed a GH amount quantified as the number 4 the total GH release is not additive (i.e. 2 + 4 = 6). Rather the whole is greater than the sum of the parts such that 2 + 4 = 10.

While the GHRPs (GHRP-6, GHRP-2 and Hexarelin) come in only one half-life form and are capable of generating a GH pulse that lasts a couple of hours re-administration of a GHRP is required to effect additional pulses.

Growth Hormone Releasing Hormone (GHRH) however 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. This shortened peptide identical in behavior and half-life to that of GHRH is called Growth Hormone Releasing Factor and is abbreviated as GRF(1-29).

GRF(1-29) is produced and sold as a drug called Sermorelin. It has a short-half life measured in minutes. If you prefer analogies think of this as a Testosterone Suspension (i.e. unestered).

To increase the stability and half-life of GRF(1-29) four amino acid changes where made to its structure. These changes increase the half-life beyond 30 minutes which is more than sufficient to exert a sustained effect which will maximize a GH pulse. This form is often called tetrasubstituted GRF(1-29) (or modified) and unfortunately & confusingly mislabeled as CJC-1295. If you prefer analogies think of this as a Testosterone Propionate (i.e. short-estered).

Note that some may also refer to this as CJC-1295 without the DAC (Drug Affinity Complex).

Frequent dosing of either the aforementioned modified GRF(1-29) or regular GRF(1-29) is required and as previously indicated works synergistically with a GHRP.

In an attempt to create a more convenient long-lasting GHRH, a compound known as CJC-1295 was created. This compound is identical to the aforementioned modified GRF(1-29) with the addition of the amino acid Lysine which links to a non-peptide molecule known as a “Drug Affinity Complex (DAC)”. This complex allows GRF(1-29) to bind to albumin post-injection in plasma and extends its half-life to that of days. If you prefer analogies think of this as a Testosterone Cypionate (i.e. long-estered)

CJC-1295 is difficult to produce and expensive to make. As a result it could be cost-prohibitive to use extensively. Modified GRF(1-29) while less convenient is much less expensive to make and because it is a pure peptide the synthesis process is straightforward. It should sell at a fraction of the cost of CJC-1295.

written by DatBtrue

Share with your friendsEmail this to someoneTweet about this on TwitterShare on Google+Share on FacebookPin on PinterestDigg thisShare on StumbleUponShare on TumblrShare on Reddit

Complete step-by-step Guide for Peptide Beginners

Complete step-by-step Guide for Peptide Beginners

1 – You are on this site because you have heard of and want to become more familiar with Growth Hormone Releasing Peptide (GHRP) and/or Growth Hormone Releasing Hormone (GHRH). These 2 materials administered can give you an increased quality of life in ways of anti-aging, muscular hypertrophy, fat loss, injury repair, higher bone density, and better sleep.

2 – GHRP can be used on its own to increase our natural Growth Hormone (GH) pulse release from the Pituitary Gland in the brain. GHRP dosed in conjunction with GHRH will amplify our growth hormone release significantly to gain maximal benefit.

3 – There are various types of GHRH’s. The only GHRH to consider is tetra-substituted CJC-1295 / CJC-1295(without DAC) / modGRF(1-29). They are all the same thing but with a different name. They come in vials ranging in material weights measured in milligrams (mg) consisting of a solid freeze-dried (lyophilized) substance.

4 – There are various types of GHRP’s. GHRP-6, GHRP-2, Hexarelin, and Imaporelin. The differences between them are potency and side effects. GHRP-6 is very potent and makes you quite hungry. GHRP-2 is potent and can slightly affect your sleep somewhat. Hexarelin is very potent but you can desensitize from higher dosages. Imaporelin is potent with the minimalist side effects of all 4 GHRP’s.

5 – Peptides are dosed via a regular 1mL needle syringe typical to what a diabetic would use. It is administered Subcutaneously (SubQ) (just under the skin into the fat tissue), most usually around the abdomen region.

6 – The required amount (saturation dose) is 1mcg (microgram) per Kg (Kilogram) of bodyweight. The typical usage and for ease of measuring is 100mcg of modGRF(1-29) and/or 100mcg of your choice of GHRP. Lower dosages will simply result in less GH release due to a slightly weaker GH pulse and reduce any side effects you may have. A higher dose will have minimal benefit and is more a waste of money than anything else. But, in saying that, the more frequently dosed in any given day would result in more frequent pulses.

7 – Mixing (reconstitution) the lyophilized product in their vials with Bacteriostatic Water (BW) can take some getting used to. The idea is not to add too much dilution. Typical rule of thumb is to add 0.5mL of BW to 1mg of Peptide. So a 2mg vial should reconstitute with 1mL BW. 5mg with 2.5mL, 10mg with 5mL, etc. Squirt the BW along the inside wall of the vial in a smooth controlled manner being cautious not to agitate the mixture too much. It will dissolve itself and become clear. You can roll the vial gently between your fingers or hands but don’t shake it to dissolve. The reconstitute is ok to be drawn once fully dissolved.

8 – On a 1mL needle, there are either 50 tick marks from 0-100, skipping every odd number OR 100 international units (IU). A 100mcg dose is half way between the 2nd and 3rd tick mark, OR 5 IU’s (if you followed the above reconstitution). There are no half tick marks. It is OK to draw modGRF and GHRP into the one needle for a single shot. It is NOT OK to mix peptides in the same vial or syringe for storage.

9 – Reconstituted peptide should be stored in the refrigerator to prevent degradation. Left at room temperature, peptide will degrade within days but kept in the fridge will last months. You can pre-load syringes and store in freezer if you want but it is more of a hassle than being worth the effort.

10 – Doses can be taken throughout the day but at no less than 3 hour intervals between doses. 1 dose a day is typical for light injury repair, anti-aging effects, deeper sleep, and better quality of life. The most beneficial would be to dose immediately prior to going to bed for your daily sleep period. Sleep is the time when our pituitary is most active. 2 or 3 doses per day will give the added benefit of lean tissue build, and fat loss, considering your diet consists of good quality foods.

11 – Doses should be taken on empty stomach to benefit the most. This is usually 3 hours or more.

12 – Do not consume food for between 15-30 minutes after your dosage. Best time is around 20-25 minute mark. GH pulses should peak within about 10 minutes after dosage. Fats and Carbohydrates affect the pulse dramatically. protein has no effect on pulse and you can have a pure protein source in your stomach at anytime if you so choose to.

13 – Dosage timing can be beneficial to your goals. For muscle growth, the 2nd most beneficial time to dose is post workout (PWO). Best time is pre-bed because sleep is when we recover and our cells repair and grow. Within 30 minutes should be fine but sooner the better. Remember to have your meal 20-25 minutes after dose.

14 – For fat loss, your supplemental dose is 1 hour pre-cardio exercise after a long fasting without food. Best time is after waking up and before breakfast. During cardio exercise, maintain a moderate intensity for between 30-60 minutes. 45 minutes is a good session. You do not want to go too hard or too long. A moderate pace will utilize Free Fatty Acids (FFA) at the highest rate for energy. Refrain from eating for approximately 2 hours after your exercise because this is the time the body is still burning fat as fuel. You must eat throughout the day to reduce the chance of muscle catabolism (breakdown).

15 – These Peptides can be used on a daily basis for the rest of your life without any harm. Enjoy!!!
BY Aussie

Share with your friendsEmail this to someoneTweet about this on TwitterShare on Google+Share on FacebookPin on PinterestDigg thisShare on StumbleUponShare on TumblrShare on Reddit
eXTReMe Tracker