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Sermorelin: The most potent GHRH/GRF analogue known to man!

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  • Sermorelin: The most potent GHRH/GRF analogue known to man!

    Sermorelin (also known as "Mod GRF 1-29") is a man-made growth hormone releasing hormone (GHRH), an analogue of the endogenous GHRH found in the many species. Sermorelin is a 29- amino acid polypeptide analog that is very similar to endogenous GHRH. Sermorelin is one of the shortest fully functional fragments of GHRH that has been made to date. Sermorelin was first developed thanks to a one-step chromatographic method capable of separating all isomers of polyethylene glycol (PEG) from endogenous GHRH. Sermorelin is now used as part of a standard test for growth hormone secretion.

    The beginning:
    This all started in 1982 when a man named "Guillemin et al" reported the isolation the growth hormone releasing factor (GRF) from a pancreatic tumour. It was at that time that researchers started to work on the development of potent GRF analogues and their possible applications. Guillemin set the gears in motion for the discovery of Sermorelin soon after. After the introduction of Sermorelin to the research field studies started popping up quite frequently with amazing feedback from researchers. The biological actions of Sermorelin were first seen in vitro by utilizing stimulation of growth hormone release in cultured rat pituitary cells and in a study soon after the GH-releasing potencies of several pegylated GRF analogs were compared to a series of model analogs and Sermorelin was found to be the most potent analog identified in the study. It was even found to be 4-5X more potent than endogenous GHRH/GRF! Pegylated analogs such as Sermorelin have been shown in research to retain an increased level of biological activity independent of its PEG molecular weight compared to endogenous GRF.

    Sermorelin (Mod GRF) and endogenous GRF:
    In a study done to compare the effects of two GRF analogues with those of native GRF using a pig animal model; it was also shown that GRF analogues (Sermorelin) were more potent than endogenous GRF. It was shown time and time again in these early studies that a peptide like GRF can be pegylated (cut shorter) and still have its full potency in effects and even enhanced effects in some cases, such as seen with Sermorelin particularly. It is important to note that the biological activity is highly dependent on the area of pegylation in the peptide. You cannot simply "cut up the peptide" and expect results in your research. Due to these studies and many like it that followed Sermorelin soon became a standard test for growth hormone secretion in various fields. It is just that great of a compound! Many of these studies did not only find Sermorelin to be more potent than endogenous GHRH/GRF, but also found GRF analogs to be highly specific, stay active for longer periods of time and were able to cause changes in tissue similar to those reported with Growth Hormone (GH) research. Thanks to this kind of research the development of peptides with site-specific pegylation has become a reality and led to the widespread utilization of Sermorelin in many areas of research.

    How it was made:
    As already mentioned Sermorelin was first developed by a one-step chromatographic method capable of separating isomers of polyethylene glycol (PEG). This was done with unmodified GRF (1-29) (endogenous GRF) and the investigation of seven different isomers of PEG-GRF (1-29). The conjugates were separated by using a reversed-phase HPLC method depending on the differences in hydrophobicity. The possible difference of hydrophobicity is due to the number and site of PEG attachment on the peptide.

    The PEGylation site of isomers of GRF (1-29) conjugates were identified in research by finding "the molecular masses of the Lys-C digested fragments with matrix-assisted laser desorption/ionization time-of-flight mass spectrometry." It was this study that was the first to report the separation of all PEG-conjugate isomers in GRF (1-29) and it is from that research that has made super potent analogs like Sermorelin possible. It was also found that a strategically placed reactive group on an active peptide is a useful tool to extend the half-life of it (basically adding a compound on, as opposed to cutting part of the compound off, as is the case with Sermorelin). In vivo research; "Three maleimido derivatives of GH-releasing factor (GRF)(1-29) were synthesized and bioconjugated to serum albumin. All three serum albumin conjugates showed enhanced in vitro stability against dipeptidylpeptidase-IV and were bioactive in a GH secretion assay in cultured rat anterior pituitary cells." This is where similar analogs to Sermorelin came along, like the compound CJC-1295 for example. They may have a very long active life per administration, But I would like to make note that a longer active live does NOT always correlate to more potent effects for various reasons. Depending on the research setting other analogs with longer half-lives may still be a worthwhile venture to researchers as well. If research is geared strictly to maximum muscle tissue growth and regeneration without the researcher having any issues with multiple administrations per day, then Sermorelin is still the compound to research with over all the others in this class for optimum results.

    Sermorelin and aging:
    GH/IGF1 plays a big role in the living animal and as seen in research with aging research subjects, there is an age-related decrease in GH and IGF1 levels as they get older. This has been found to contribute to decreased muscle mass and strength in older subjects, along with other diseases that are inter-related. This makes research into Sermorelin's effects on ageing and its possible protection from illness in older subjects a very worthwhile venture in my opinion.
    In a study aimed to determine whether administration of Sermorelin would sustain an increase in GH and IGF-I along with improving skeletal muscle function and body composition it was found that: "GHRH treatment increased mean nocturnal GH release, the area under the GH peak and GH peak amplitude. Two of six measures of muscle strength and a test of muscle endurance improved." This study was conducted on research subjects with low baseline IGF-I levels that were administered nightly subcutaneous injections of Sermorelin for 6 weeks. Researchers measured GH/IGF1 levels in the blood of subjects every 20 minutes during both sustained and ramped exercise in part of this study. Even more importantly found in this study was "No significant adverse effects were observed"!

    This is very important because research should not just be about how active a Mod GRF like Sermorelin (or any compound) can be, it should also be about how safe and tolerable the compound is as well. That is what makes for the most effective and fruitful research on any compound. It is nice to know that Sermorelin is one of those compounds where side effects are not of much concern. Another thing that this study also pointed out is that a single nightly dose of Sermorelin is less effective than multiple daily doses. This means if you want to have the most effective spikes in GH secretion and the best possible results in Sermorelin research that the researcher should administer this compound to their research subjects multiple times per day.

    Sermorelin and physical development:
    In a recent study with a GRF immunization against GRF (No GRF effects allowed to happen) it was found that; "administration initiated at 3 or 6 months of age showed a decreased weight gain, increased deposition of fat, and delayed puberty in heifers." This shows that GH and GRF does play a VERY large role in not just the maintenance of tissue and function in aging animals, but also in their early development as well. This paves the way for further research into the mechanisms and possible applications with Sermorelin to help conditions of both age related illness and developmental dysfunction as well.

    Sermorelin effect/use in livestock:
    The research findings into Sermorelin's positive effects on muscle mass have been so positive that research has already been done (and continues to be done) to check animal live stocks genetics and their GH response by a single acute dose of Sermorelin. Currently the use of Sermorelin and like compounds are being used as an evaluation tool to predict the future growth performance and carcass characteristics of bulls and other livestock with good success.
    Here are the basics of just a couple studies that have done this GH response evaluation research with the administration of Sermorelin:

    In Bulls: "In a Latin square design balanced for residual effects. Blood samples were collected via jugular catheter at -60, -45, -30, -15, 0, 5, 10, 15, 30, 45, 60, 90 and 120 min relative to GHRH injection. Serum concentrations of GH were plotted over time. Response to GHRH was calculated as the area under the GH response curve (AUC-GH)- carcass measurements from a 140-d growth performance test were evaluated using simple linear regression. A positive correlation between AUC-GH and ADG and an inverse relationship between AUC-GH and carcass fat were observed."

    In Pigs: "Pituitary cells, from seven 160- to 170-day-old pigs, were studied in primary culture to determine the affects NPY on LH and GH secretion at the level of the pituitary.- Relative to control at 4 h, 10(-10), 10(-8) and 10(-6) M GRF increased GH secretion by 111%, 125% (P < 0.01) and 150%"

    This type of GH response evaluation provides an early and fairly accurate evaluation of livestock?s genetic potential in the food industry and this may potentially help cut down on the amount of slaughtered animals, needed feed (cost) and farm space needed (cost). This should lead to more profit with less waste and less overall cost.


    Sermorelin and sleep:
    As I am sure most of us know there is an association between sleep and the nocturnal GH release of many species. In a recent study it was shown that Sermorelin administration to test subjects increased slow-wave sleep (SWS) and GH levels. This leads me to think that Sermorelin can induce SWS. There is still some debate on that and more research needs to be done in this area, but none the less a worthy finding to note for further researchers interested in this area of research.


    Sermorelin really is the most effective GRF analog known to increase skeletal muscle mass in young and aging research subjects alike and it has also specifically been noted for altering the baseline relationships between muscle strength and muscle bioenergetics with a reduced need for anaerobic metabolism during heavy exercise. This means Sermorelin is not only a great tool for researching its positive effects on muscle mass and the preservation of aging research subjects, but it is also a great tool for researching the enhancement of physical function as well.

    I hope that this article has helped to show you just what possible applications Sermorelin has to offer for your research.

    Thank you for reading.


    Get it here > Sermorelin 2mg


    Ref:
    1) The use of pigs as an animal model to evaluate the efficacy, potency and specificity of two growth hormone releasing factor analogues.Dubreuil P, Brazeau P, Moreau S, Farmer C, Coy D, Abribat T. The use of pigs as an animal model to ev... [Growth Horm IGF Res. 2001] - PubMed - NCBI
    2) Tryptic hydrolysis of hGH-RH(1-29)-NH2 analogues containing Lys or Orn in positions 12 and 21.Witkowska E, Orłowska A, Sagan B, Smoluch M, Izdebski J. Tryptic hydrolysis of hGH-RH(1-29)-NH2 analogues ... [J Pept Sci. 2001] - PubMed - NCBI
    3) Predicting bull growth performance and carcass composition from growth hormone response to growth hormone-releasing hormone.Connor EE, Barao SM, Douglass LW, Zinn SA, Dahl GE. Predicting bull growth performance and carcass co... [J Anim Sci. 1999] - PubMed - NCBI
    4) Effects of active immunization against growth-hormone releasing factor on puberty and reproductive development in gilts.Swanchara KW, Armstrong JD, Britt JH. Effects of active immunization against growth-hor... [J Anim Sci. 1999] - PubMed - NCBI
    5) Pegylated peptides. IV. Enhanced biological activity of site-directed pegylated GRF analogs Felix AM, Lu YA, Campbell RM. Pegylated peptides. IV. Enhan... [Int J Pept Protein Res. 1995 Sep-Oct] - PubMed - NCBI
    6) Neuropeptide Y modulates growth hormone but not luteinizing hormone secretion from prepuberal gilt anterior pituitary cells in culture.Barb CR, Barrett JB. Neuropeptide Y modulates growth hormo... [Domest Anim Endocrinol. 2005] - PubMed - NCBI
    7) growth hormone-releasing factor (hGRF)1-29-albumin bioconjugates activate the GRF receptor on the anterior pituitary in rats: identification of CJC-1295 as a long-lasting GRF analog.Jett? L, L?ger R, Thibaudeau K, Benquet C, Bridon DP. Human growth hormone-releasing factor (hGRF)1-... [Endocrinology. 2005] - PubMed - NCBI
    8) Chromatographic separation and mass spectrometric identification of positional isomers of polyethylene glycol-modified growth hormone-releasing factor (1-29).Youn YS, Na DH, Yoo SD, Song SC, Lee KC. Chromatographic separation and mass spectrome... [J Chromatogr A. 2004] - PubMed - NCBI


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