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|Purity:||More Than 98%||PubChem:||CID 16133753|
|Synonyms:||Sermorelin Acetate Hydrate, GRF 1-29 NH2||CAS:||86168-78-7|
egf growth factor,
epithelial growth factor
GRF 1-29 Peptide 86168-78-7 Epithelial Growth Factor Growth Hormone Releasing Hormone
Sermorelin Acetate, also known as GRF 1-29, is a Growth Hormone Releasing Hormone (GHRP) produced by the brain that stimulates the production and release of Growth Hormone (GH). Sermorelin Acetate was first developed in the 70s, which is thought to be the shortest fully functional fragment of GHRH and has been used as a test for Growth Hormone secretion.
It is often used extensively in Anti-aging Therapy along with Testosterone in men. Sermorelin Acetate affects a more primary source of failure in the GH neuroendocrine axis, has more physiological activity, and its use for adult hormone deficiency is not restricted. Compared to human Growth Hormone (hGH), Sermorelin Acetate is a growth hormone secretagogue, which means that it stimulates the pituitary gland to produce and secrete growth hormone.
Also, Sermorelin Acetate and Modified GRF 1-29 contains 29 amino acids whereas hGH is a larger molecule containing 191 amino acids.
Sermorelin (GRF 1-29)
Molecular formula: C149H246N44O42S
Molar Mass: 3357.96
CAS number: 86168-78-7
PubChem: CID 16133753
Synonyms: Sermorelin acetate hydrate, GRF 1-29 NH2
What is Sermorelin?
Sermorelin is a GHRH (growth hormone–releasing hormone) peptide analogue. Its peptide sequence is comprised of 29 amino acids. This sequence is a portion of the endogenous human GHRH, and is currently considered to be the shortest synthetic peptide that possesses the full array of functional GHRH activity. Due to this fact, sermorelin is considered to be a growth hormone secretagogue.
Sermorelin has been used during research to stimulate the secretion of growth hormone from the adenohypophysis (also called the anterior pituitary). The anterior pituitary secretes trophic hormones. Sermorelin has also been used in research stimulation tests to assess for pituitary sufficiency in relation to the secretion of the growth hormone.
Growth hormone–releasing hormone
GHRH is 44 amino-acids polypeptide that stimulates the secretion of growth hormone from the adenohypophysis. It is also called somatocrinin or somatoliberin. It is produced in the cell bodies of periventricular arcuate neurons, and thereafter transported to the neurosecretory terminals of the neurons where they are released. The arcuate neurons do form part of the hypothalamo-hypophyseal portal system. Their release from the neurosecretory terminals occur in a pulsatile fashion and it thus follows that growth hormone (GH) release also occurs in a corresponding pulsatile fashion. GHRH binds to a secretin-type G-protein coupled serpentine receptor called the GHRH-receptor (GHRHR).
Binding causes the receptor to activate both the cAMP (cyclic Adenosine Monophosphate)-dependent pathway and the phospholipase C (PLC) pathway. The terminal downstream actions of the cAMP-dependent pathway do upregulate the transcription of both the GH and GHRHR genes thereby providing a positive feedback loop that amplifies the production of GH. The GH produced is thereafter packaged in secretory vesicles. The downstream actions of the PLC pathway results in both Na+-voltage-dependent and Ca2+-dependent fusion of the secretory vesicles with the plasma membrane thereby releasing GH into the bloodstream.
The actions of GH ensure an optimal well-regulated post-natal growth. GH also promotes efficient energy metabolism. Studies have also shown that GHRH directly promotes slow wave NREM (non-rapid eye movement) sleep, and thus GHRH insufficiency causes a reduction in the amount and intensity of slow wave NREM sleep which results in either insomnia or dysomnia (sleep disorders that causes sleep to lose its restorative capacity). Studies have also shown that GHRH inhibits the actions of somatostatin.
Somatostatin is a polypeptide hormone that inhibits GH secretion from the adenohypophysis. Both GHRH and somatostatin are produced in the same neuron but they are released in alternation to each other thereby resulting in the pulsatile release of GH from the neuron.
Recent research has also shown that GHRH is also produced outside the hypothalamus by pancreatic cells, gastrointestinal tract epithelial cells and in some neoplastic cells. Clinical studies have also shown that the actions of Sermorelin are similar to the GHRH actions. Thus, Sermorelin has been used to diagnose deficiencies in GH secretions. Also, Sermorelin has been investigated for its therapeutic properties as the studies discussed below show.
The two studies reviewed hereafter have provided adequate and conclusive findings that sermorelin can be used clinically to promote growth and manage GHRH deficiency.
1. Sermorelin and growth hormone (GH) deficiency.
In 1999, a study entitled “Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency” was authored by Aitabh Prakash and Karen Goa and published in the journal Biodrugs.
The aim of this study was to investigate whether sermorelin injection stimulates GH secretion from the adenohypophysis. The subjects of this study included adults and pre-pubertal children (both normal and those suffering from GH deficiency). The subjects were randomly divided into two groups with one group receiving intravenous sermorelin injection and the other group receiving subcutaneous sermorelin injection.
The results obtained from both groups showed that Sermorelin was able to rapidly diagnose GH insufficiency in children affected by GH deficiency (p < 0.05). The p<0.05 is a measure of statistical significance, and the value 0.05 shows that the results are statistically significant. However, the diagnosis could only isolate GH insufficiency caused by GHRH deficiency.
The results also revealed that subcutaneous sermorelin injection did cause a significant increase in height in children suffering from idiopathic GH deficiency, and that this acceleration in growth rate could be maintained consistently for 36 months. Likewise, the results also revealed that both Sermorelin administrations were well tolerated with the only observable adverse effects being injection-site pain and transient facial flushing.
In summary, the findings of this study show that sermorelin stimulates GH secretion from the adenohypophysis. Also, intravenous sermorelin can be used to diagnose some cases of GH deficiency, and subcutaneous sermorelin can be used to manage GH insufficiency.
2. Sermolelin and growth acceleration in a chronic disease state.
In 1996, Pasqualini et al conducted a study that was published under the title “Growth acceleration in children with chronic renal failure treated with growth-hormone-releasing hormone (GHRH)” in the journal Medicina. The subjects involved in this study were 9 children aged between 1 to 14 years old. They all suffered from chronic renal failure (CRF). The aim of this study was to investigate whether subcutaneous Sermorelin causes growth increase in children ailing from CRF.
The subjects were categorized into 3 groups, the first group comprised of 3 children on conservative management, the second group comprised of 3 children on dialysis and the last group comprised 3 children who had undergone renal transplantation. Each of the three groups was administered with subcutaneous Sermorelin acetate (Geref ®) for a period of 3-6 months.
The results showed that the mean serum creatinine and urea levels remained stable in all the subjects except for two children on conservative management who showed an increase in their serum creatinine levels. The results also revealed that the rate of height increase in 5 of the subjects (3 on conservative management, one on dialysis and the other had undergone transplantation) averaged about 4.2cm/year (p < 0.05).
Also, Geref® caused a higher peak in GH response among growth non-responders as compared to the growth responders (p < 0.05). The results obtained in this study do show that non-responders suffered from GH-resistance as demonstrated by the fact that they had high levels of GH but their growth was still stunted.
In summary, the findings of this study show that sermorelin does increase the rate of growth in GH-responsive CRF children, though it has no appreciable effect on the course of the CRF.
In conclusion, the above two studies show that Sermorelin can be used in research to diagnose cases of GH deficiency, stimulates GH secretion from the adenohypophysis, manage GH insufficiency and increase the rate of growth in GH-responsive CRF children.
3. The Sermorelin Acetate Peptide and HGH
Sermorelin Acetate, which shares similar structure to CJC-1295, is a bio-identical synthetic hormone that is extremely effective in increasing the amount of HGH. Human Growth Hormone is a hormone released by the body that controls the reproduction and growth of the cells and each of the organs in the body.
At a young age, the body's HGH production is most active while the growth rate is at its highest point. After the age of 30, for every decade of life, there is a 14% reduction in HGH production . By the age of 40, HGH production is about 40 percent of what it was at the age of 20. With the further development of Growth Hormone Releasing Factors (GHRF), such as Modified GRF 1-29, HGH production may possibly begin again by stimulating the pituitary gland.
4. Sermorelin Acetate and Related Research
Since 1980, scientists have been studying GHRH for many years. Dr. D. Rudman was testing Sermorelin as a tool for anti-aging processes and Dr. William Wehrenberg was looking at different peptides and particularly GHRH to identify which part of it is needed for pituitary gland stimulating response.
His results after eliminating single amino acids showed that 29-acid-chains were held responsible for pituitary stimulation. Many research studies have concluded that Sermorelin is a well tolerated analogue of GHRH. As a result, this is suitable for use as a provocative test of growth hormone deficiency (Prakash and Goa 1999). In 1999, both researchers, Goa and Prakash checked Sermorelin Growth Hormone as provocative tasting method for deficiency of endogenous G-hormone.
Sermorelin therapy increased the volume of hormone secreted by the stimulated pituitary gland, which is later converted by the liver into IGF-1. The increased amount of IGF-1 in the blood stream leads to many benefits from the use of Sermorelin: increasing metabolism and growth of new cells within the body’s organs and bones.
Sermorelin acetate is a recently synthesized (man-made) peptide analogue of growth hormone releasing hormone (GHRH) a naturally occurring hormone that is produced in the hypothalamus and stimulates and controls the production of growth hormone (GH) within the pituitary gland. GHRH, which is necessary for growth and development, was first described by Nobel Laureates R. Guilleman and A Shalley. In the 1970s one of their students, William Wehrenberg, began studying which part of the GHRH molecule was essential in stimulating the pituitary gland.
SERMORELIN FUNCTION AND TRAITS
By removing individual amino acids from the GHRH molecule, Wehrenberg found that only the first 29 amino acids were essential for the stimulation of GH production in the pituitary gland. Semorelin is therefore only comprised of these 29 essential amino acids, forming a short polypeptide chain that is considered one of the shortest functional fragments of the GHRH molecule. It was first developed with a one-step chromatographic method capable of separating all isomers of polyethylene glycol (PEG) from naturally occurring GHRH.
The biological effects of sermorelin were first observed in vitro cultures of rat pituitary cells. When compared to other GHRH analogues, sermorelin was found to be the most potent, potentially 4-5 times as potent as naturally produced GHRH. Recent studies of other GHRH analogues in pigs have also found synthetic GHRH analogues to be more effective than the naturally occurring hormone.
Sermorelin is now used as a standard test for growth hormone secretion and is primarily prescribed for children who do not produce GH properly and fail to grow healthily as a result. It has a secondary, off-label use in “repairing” declining GH levels (a natural side effect of aging that leads to weight gain, decreased strength and muscle mass, and insomnia in elder subjects). GH levels typically peak at around 20 years of age in humans and fall by about 14% for every decade that passes, but use of Sermorelin can potentially rejuvenate GH back to youthful levels.
EFFECTS OF SEMORELIN
Sermorelin has a wide range of positive effects. Due to its nature as a GHRH, sermorelin only increases the body’s ability to produce more growth hormone; it is not an injection of growth hormone itself. In both a performance enhancing and general well-being sense, sermorelin has a wide array of benefits that make it a powerful and valuable substance.
1. Mental: Focus and mental clarity improve, leading to an easing of general day-to-day tasks. Libido can be heightened and users have reported an improvement in their sex lives. General fatigue as well depression can also be reduced. All of these qualities can lead to a generally healthier, happier lifestyle.
2. Physical: Sermorelin increases the development of lean body mass through the development of new muscle cells and reduces body fat through lipolysis. This leads to increased strength and endurance and improved muscle tone as well as improved skin elasticity (smoother, less wrinkly skin) and loss of cellulite. Calcium retention improves, leading to the increased mineralization of bone (bone density), strengthening the skeletal system.
3. General enhancement: Protein synthesis increases, leading to the stimulation of all internal organs (including the heart) except for the brain. Cholesterol levels fall. Regardless of the purpose of use, joint and muscle pain is lessened, one’s recovery time from wounds increases, and the immune system improves. The individual will not tire as quickly and will be able to go longer in their daily activities, be those exercise related or other. Deeper, more restful and satisfying sleep can be expected (some have reported more vivid dreams) and hair can becomes thicker, fuller, and more lustrous.
There are a significant number of potential side effects that come with the use of sermorelin, although in the vast majority of cases the side effects, if present at all, are relatively mild. While side effects are certainly possible and semorelin is not risk-free, for a healthy adult these risk can be minimized and many will find no negative side effects at all.
1. Common side effects: The most common side effects (about 17% of total cases) include pain, swelling, and/or redness at the injection site. These side effects usually do not require medical attention. Less common are itching and trouble swallowing. As with any peptide, allergic reactions can occur. Many patients develop antibodies to growth hormone–releasing hormone at least once during treatment with sermorelin. However, the significance of these antibodies is not known.
Their presence does not appear to affect growth, nor do they cause specific side effects. In less than 1% of cases, dizziness, flushing, headache, hyperactivity, or sleepiness have been reported. The use of semorelin could also potentially lead to reduced risk of hypertension, stroke/aneurysm/heart attack, heart and kidney failure, and vision changes or loss, however none of these conditions have been conclusively linked to its use.
2. Medical risk: Studies in rats, rabbits, and pigs have shown there to be an adverse effect upon the fetuses of pregnant females. There have been no studies at all regarding this product and its risks in human females who are pregnant or trying to become pregnant and it is currently unknown whether sermorelin is released in mammalian breast milk.
Using alcohol, tobacco or other medications (especially corticosteroids and glucocorticoid) with certain products may cause certain unwanted interactions to occur. Speak to your healthcare professional about other medicines you take and your lifestyle choices before starting to use this substance.
The presence of other medical problems may affect the use of this product, so always check with your doctor beforehand, especially if you suffer from an under/hyperactive thyroid. Long-term studies to determine if sermorelin has any carcinogenic properties in either humans or animals have not been conducted, but neither have any reports of cancer caused by semorelin been reported.
Sermorelin is prescribed as a fine white powder of a variable dose (in milligrams) in a vial that must be mixed with bacteriostatic water or medical grade saline solution as a diluent. The powder should be stored out of light at or below room temperature. The solution is used by injection into subcutaneous (below the skin) body fat using a very small needle, comparable to what a diabetic would use to take their insulin shots.
Once combined into solution form, sermorelin must be kept in the refrigerator (do not freeze—store between 2 and 8°C/36 and 46°F) ) and out of light or else the chain of amino acids will break down and it will be rendered ineffective. Before use, check the liquid for particles or discoloration and, if found, discard the solution. As with most peptides, there is a saturation dose at which point taking any more of the peptide will not increase the production of growth hormone, a consequence of the body’s natural mechanism to keep hormonal levels at a safe homeostasis. This saturation dose is typically around 100mcg.
It is best to use a different place on the body for each injection (for example, abdomen, hip, thigh, or upper arm). The dose of this medicine will be different for different patients based off of their body-mass index (BMI); use it exactly as directed by your doctor and do not use it more often than your doctor prescribed. Sermorelin has an ongoing effect in which optimal HGH levels can be sustained long after the last injection. Just like synthetic GH, sermorelin initially must be injected every day. Unlike synthetic HGH, once optimal levels reached, injection frequency can be decreased or stopped altogether
AVAILABILITY AND PURCHASE OF SERMORELIN
Products containing sermorelin acetate was pulled from the US market (under the brand name ‘Geref’) in November, 2002. Sermorelin is also not commercially available in Canada. Thus, one cannot buy sermorelin over-the-counter in North America. However, sermorelin can legally be prescribed by a doctor for “off label” use at home in the United States.
As with all products related to steroids and growth hormone, sermorelin can be found for purchase on the black market and the internet, even in geographic locations where its sale is prohibited by local, state, and federal law. While some of these sellers may be selling products of repute, the trustworthiness of products sold over the internet or black market cannot ever be verified in advance. Always remember that there are plenty of mislabeled or outright fake products sold on the internet/black market that are marketed as certain other products and substances.
Potential users should always consult with their medical professional and check the relevant laws of their home country/state before buying semorelin. Buying semorelin should not be a quick decision, but one made after some careful cost-benefit analysis of the effects and the consultation of professionals. Remember that purchasing semorelin online in the United States is still a crime, and that it can only be taken in the USA with a prescription written by your doctor.
There are currently no clinical trials being undertaken with sermorelin in the United States and consequently the jury is still out on its overall effectiveness when compared to its potential downsides, but very clearly it is a very powerful substance that has great potential for human general health and wellbeing, both mentally and physically. The key to getting the best results from the use of semorelin is understanding how GHRH affects the production of growth hormone in the body, which we have outlined above.
Many assume that the use of such products is solely for the purpose of bodybuilding or gaining an unfair advantage in sports and competition, but sermorelin can be used as a general product to promote one’s mental and physical health and wellbeing and to counter the inevitable effects of aging. If any of these are your goals, then sermorelin is an outstanding substance for you.