Sermorelin, also known as GRF 1-29 or Modified GRF1-29, is the first 29 peptides, biologically-active portion, of the 44-amino acid Growth Hormone Releasing Hormone (GHRH) with some slight modifications to certain amino acids in the peptide chain to extend the half-life of the molecule and produce higher yields. GHRH is a hormone that triggers the pituitary gland to release Growth Hormone (GH).
Human Growth Hormone (hGH), or commonly referred to simply as Growth Hormone (GH), is an endocrine peptide hormone, chemical structure shown in Figure 1.1, containing 191 amino acid residues, that stimulates cell growth, replication, and repair in human cells; especially in muscle, bone, and cartilage cells. GH is produced, stored and released by the anterior lobe of the pituitary gland but is regulated by the hypothalamus.
In mid-late adulthood a trend of physical decline in people. The lean muscle and lean body mass is reduced, and the body fat is increased. The reduction in lean body mass reflects the age-related atrophic effect on the skeletal muscle, bones, and skin. (Rudman 1990) As science developed a better understanding of human biochemical mechanisms and how these mechanisms were affected by the natural aging process; relationships were uncovered between the symptoms commonly associated with the natural of aging process and the levels of certain biological chemicals such as Human Growth Hormone (hGH), commonly referred to as (GH), Insulin-like Growth Factor-1 (IGF-1), Growth Hormone Releasing Hormone (GHRH), known as Somatocinin, and Growth Hormone Inhibiting Hormone (GHIH), known as Somatostatin.
Many studies have been conducted showing the relationships between these chemicals and the symptoms of the aging process. These relationships have a role in the way the body develops and preserves muscle mass, reduces adipose fat storage, preserves bone mineral density (BWD), increases epidermal (skin) thickness, regulates metabolism rate, sustains immune health, and preserves memory and cognitive function; all of which have been proven to be effected by age.
The findings of these studies have led to the development of treatments some of which have been proven to delay, prevent, and even reverse some of these symptoms commonly associated with the aging process. Currently the focus of research is on the best treatment method for adjusting the levels of these biological chemicals to safely treat some of the symptoms of age.
In the early 50s, scientists began performing studies with Growth Hormone (GH) obtained through animals. Human Growth hormone (hGH) first was isolated from a the pituitary gland in of a human cadaver in 1956, by both researchers from Berkeley, Li and Papkoff, and a researcher from Yale University, Raben. The biochemical structure of hGH was not elucidated until 1972. The primary use of hGH at the time was to treat children suffering from Growth Hormone Deficiency (GHD). (Frasier 1997)
In 1970s a Swedish pharmaceutical company, Kabi, began approaching hospitals to purchase pituitary glands with the goal of developing the first commercial hGH product, Crescormon. In 1981, an American pharmaceutical company, Genentech, working in collaboration with Kabi developed the first Recombinant Human Growth Hormone (rhGH) using a newly developed technology, recombinant DNA, in which human genes are inserted in bacteria producing an unlimited amount of the desired protein. This innovative technology allowed scientists to now produce a nearly unlimited supply of hGH. In 1985, following a report of four young adults contracting a fatal virus linked to contaminated cadaver extracted hGH, the FDA suspended cadaver hGH use. Also in 1985 an endocrinologist, Dr. Daniel Rudman MD of the Medical College of Wisconsin, began trails using the new rhGH treatment but these trials were not on children with GHD but rather elderly males that had seen a rapid decline in strength and metabolism due to the aging process. The results of Dr. Rudman’s studies were remarkable and were published in an article in the New England Journal of Medicine titled “Effect of human growth hormone in men over 60 years old.” The 26 men between ages 61-81 showed amazing changes in body composition with an average of 8% gain of lean muscle, an average of 14% decrease in body fat, and increased skin thickness. (Rudman 1990)
Rudman’s findings created a surge of interest to further explore the rejuvenating potential of hGH. However certain unresolved medical and legal issues surrounding rhGH have prevented physicians and scientists to thoroughly explore the use of rhGH. One concern is dosage related side effects that could be serious. Another is the injection of rhGH results in an unnatural exposure of the hormone that could have a negative impact on the subject’s physiology. Also, the Code of Federal Regulations legally limited the use of rhGH only for the treatment of AIDS or GHD. (Walker 2006)
In 2001 a study conducted at the University of Michigan identified the root cause of the age-related decline in hGH is due to the hypothalamus selectively reducing the secretion of Growth Hormone Releasing Hormone (GHRH). (Russell-Aulet 2001) This led to the development of a modified bioidentical hormone called Growth Releasing Factor (GRF1-29 NH-acetate), known as Sermorelin. (Merriam 2003) Sermorelin may prove to be a safe and effective method to delay, prevent, and possibly reverse some of the commonly associated symptoms of aging.
The Somatotropic Axis primarily consists of Growth Hormone Releasing Hormone GHRH, Growth Hormone (GH) and Insulin-like Growth Factor-1 (IGF-1). Somatotropes are cells found in the anterior pituitary gland which produce and secrete Growth Hormone (GH).
It is well documented and accepted that there is a natural age-related decline of GH levels and subsequently IGF-1 levels in the body. (Sonntag 1980) GH levels normally peak during adulthood and begin to decline once the body reaches full adult size and following complete maturation of reproductive organs, as shown in Figure 2.1. IGF-1 levels, following a similar trend to GH, peak during adolescence with lowest levels occurring during infancy and old age. This trend is consistent with the direct relationship between IGF-1 levels and GH levels
The overall age-related hormonal decline of the somatotropic axis has been termed “somatopause” analogous to menopause or adrenopause. (Bartke 2008) Somatopause occurs gradually over time and is viewed as adult onset GHD (AO-GHD), which has some different symptoms than adults with untreated childhood onset GHD (CO-GHD). AO-GHD can be treated in the same way as CO-GHD, however there were some side effects in patients with AO-GHD in response to the rhGH treatment which were attributed to GH dosage being too high for the elderly patients. (Van der Lely 1998)
Symptoms commonly associated with aging in humans are also the same symptoms of the Somatopause that have been found to be reduced, prevented, or reversed by increasing hGH levels in the body. These symptoms consist of decline in metabolism (Ayuk 2006), increasing stored adipose tissue (body fat) (Rudman 1990), decrease in development and preservation of muscle mass (Moller 2009), decease in bone mineral density (BMD) (Milman 2016), decease in skin thickness (Rudman 1990), decreased immune health, a decline in memory (Nieves-Martinez 2010), and a decrease of the overall sense of wellbeing (Nyberg 2005). Many studies have clearly discovered that supplementing the naturally declining levels of hGH have helped to slow down and in some ways, prevent these symptoms altogether. The question that remains is what is the safest and most effective method for the supplementation of naturally declining hGH levels in the body?
Research shows that currently there are only two clear treatment options to supplement this decline of hGH; either rhGH or Sermorelin (GRF 1-29). With the root cause of this decline now known to be initiated by the reduction of GHRH secretion over time, the challenges of regulating GH levels using rhGH, the legal constraints severely limiting the use of rhGH, and the risks associated with the dosage concerns surrounding rhGH treatments; Sermorelin (GRF 1-29) appears to be a promising solution to the dilemma that may delay, prevent, or even reverse some of the symptoms of aging. It appears that the stimulation of the natural production of hGH in the body is a way to supplement the decline of hGH without the risks associated with rhGH treatment. There are currently no legal constraints on the use of Sermorelin in any way. Because Sermorelin stimulates the natural production of hGH in the body, the negative feedback loop created by hGH and IGF-1 prevents the GH levels from rising above natural peak levels; giving Sermorelin yet another advantage over rhGH treatments.
GH and IGF-1 in combination create an anabolic effect in human tissue by hypertrophy, increasing the size of cells, and hyperplasia, increasing the number of cells. GH/IGF-1 axis plays a critical role in metabolism and homeostasis. (Moller 2009) The decline of GH and IGF-1 levels resulting from age have been matched to a number of symptoms commonly associated with the aging process.
GH promotes lipolysis, the enzymatic breakdown of fats and lipids by hydrolysis increasing the release of free fatty acids (FFA) by lipase and H2O.
The increasing in FFA results in an increase in the beta-oxidation of free fatty acids which produces more acetyl-CoA, and in turn supplies the citric acid cycle. (Moller 2009) GH increases lipid metabolism, reducing stored body fat and preventing obesity. As a result, GH plays a key role in the increasing overall metabolism in the body.
As shown in Figure 2.2, GH causes an increase in muscle mass by promoting the synthesis of Insulin-like Growth Factor (IGF-1) in the muscles. An increase in GH both directly and indirectly leads to an increase in muscle mass. (Rudman 1990) Increased IGF-1 synthesis occurs in response to exercise or the presence of GH by autocrine/paracrine signaling stimulating sarcomere hypertrophy increasing lean muscle mass. (Vellaso 2008)
During catabolic activity, the body in a fasting-state, GH promotes the hydrolysis, release, and beta oxidation of FFA. This can result in the preservation of lean body mass by preventing the oxidation of glucose and proteins. This helps the body preserve muscle mass and protein loss. (Moller 2009) People suffering from GHD tend to have increased body fat, as shown in Figure 2.3, and decreased fat-free mass in comparison to control subjects. They also have decreased muscle strength and exercise tolerance (Ayuk 2006).
Another area proven to be helped by supplementing GH decline has been bone strength. Bone mass and density have been proven to decline with age as shown in Figure 2.5. (Milman 2016)
GH and IGF-1 have been shown to improve Bone Mineral Density (BMD). GH plays an indirect role by stimulating IGF-1 secretion by osteoblasts. IGF-1 assists with cell differentiation and bone mineralization. Studies performed on the cross-sectional area of bones in elderly subjects have evinced the relationship between high IGF-1 levels with high BMD. (Milman 2016)
Epidermal tissue, skin, has been evidenced to decrease in thickness over time because of age. One of the interesting discoveries in the Rudman experiment was the increased in epidermal, skin, thickness resulting from the rhGH treatment. (Rudman 1990)
GHRH is a sleep stimulating peptide hormone that increases quality of sleep by increasing non-REM sleep and decreasing wakefulness. (Steiger 2013) Sleeping disorders have not been linked to age, although the improved quality of sleep contributes to the decrease in stress and increased natural energy levels which can be affected by age.
Historically used to improve body composition, GH also exhibits the ability to improved cognitive functions such as memory. A study was performed by the Neuroscience Program in Wake Forest University testing the effects of supplemental GH on the mid-life memory of patients with GH deficiency. The results of this study showed a link between the treatment of patients suffering from GHD with supplemental rhGH and improved mid-life memory. (Nieves-Martinez 2010)
The GH/IFG-1 axis also plays a pivotal role in the development and differentiation of cells throughout the Central Nervous System (CNS). It can protect against dementia and ischemia, which can hinder cellular metabolism and cause a heart attack or stroke. GH has also been shown to improve mood and wellbeing. There has been a link shown between depression and low levels of GH. (Nyberg 2005)
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