SERMORELIN is among the growth hormone-releasing hormone (GHRH) analogs developed in recent years. It aims to maintain the positive effects of natural GHRH and overcome the adverse outcome of GHRH. Sermorelin (clinically known as Geref) has been researched to assess growth hormone secretion, but the peptide is of additional interest for its potential to:
– Decrease tissue scarring after the cardiac attack
– Improve bone density
– Enhance nutrition in chronic illness
– Improve renal function
– Combat the effects of dementia
– Reduce seizure activity
MOLECULAR FORMULA: C149H246N44O42S
MOLECULAR WEIGHT: 3357.9 g/mol
SEQUENCE: Tyr-Ala-Asp-Ala-lle-Phe-DL-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-NH2
PUBCHEM: CID 16129620
CAS NUMBER: 86168-78-7
RECONSTITUTION: Required
SERMORELIN AND CARDIAC HEALTH
Cardiac attacks, apart from being potentially fatal, can also cause long-term disability secondary to cardiac failure, cardiac conduction abnormalities (arrhythmias), decreased exercise capacity, pain, and more. A number of these issues arise from cardiac remodeling due to damaged myocytes (heart muscle cells). Often, it leads not only to scarring of tissue in the area of damage following a cardiac attack but extends to surrounding healthy tissues as well. Cardiac remodeling leads to long-term problems, and prevention helps to improve outcomes both immediately after a heart attack and years down the line. In 2016, a study in pigs observed that Sermorelin use appeared to help reduce the remodeling after a cardiac attack. The research suggested that Sermorelin:
– Decreases cell death in cardiomyocytes
– Improves the production of extracellular matrix components needed for adequate healing
– Promotes angiogenesis to damaged tissue
– Reduces the production of pro-inflammatory substances
It has been also studied for its potential to assist in diastolic function, decrease scar size, and increase capillary growth.[1] [2] The researchers note that “Treatment with GHRH agonists appears to reduce the inflammatory responses post-MI and may consequently improve mechanisms of healing and cardiac remodeling by regulating pathways involved in fibrosis, apoptosis and cardiac repair.” It is being explored for different cardiac diseases like a cardiac failure and valve disorders.
SERMORELIN AND EPILEPSY
Gamma-aminobutyric acid (GABA) is a central nervous system signaling molecule that decreases electrical activity in the spinal cord and reduces overall electrical excitability in the central nervous system. Many anti-seizure medications work either to: enhance levels of GABA in the central nervous system; or mimic GABA by binding to GABA. In a recent murine model with epilepsy, scientists administered Sermorelin to study the effect on seizure activity. GHRH analogs were observed to activate GABA receptors and inhibit seizures.[3] This may open avenues for new medicines as the existing ones have adverse effects.
SERMORELIN AND SLEEP
Orexin is a powerful neurochemical secreted by certain neurons in the brain. It has been observed to regulate sleep cycles. Growth and healing of the body by the growth hormone secretion happens maximally during sleep. Studies have found that a functional GHRH axis is required for orexin production and function. In addition, exogenous administration of Sermorelin and other GHRH agonists appears to enhance orexin secretion.[4] Sermorelin is being studied to improve sleep disorders.
SERMORELIN COMPARED TO GROWTH HORMONE
Sermorelin is a growth hormone-releasing hormone derivative that was developed to mediate the beneficial effects of GH but not its side effects. Sermorelin has been studied for its potential to increase GH levels in humans over direct use of the hormone itself, as the peptide appears to be regulated through physiological feedback mechanisms that prevent the adverse effects of GH. Adverse effects include overdose, improper dosing, and unintended side effects like edema, joint pain, and dysregulation of normal physiology.[5] Sermorelin researchers have posited that the peptide is not subject to tachyphylaxis, the process by which the body becomes acclimatized to a medication dose and requires higher doses to achieve desired effects. In certain cases, tachyphylaxis is so aggravated that complete stoppage of medication use is essential to regain the effects of medication. Studies have observed that the body appears to have a unique response to the long-term administration of Sermorelin.[6] Scientists conclude that “that the short time course of resensitisation following acute octreotide withdrawal is suggestive of an effect(s) on receptor function or on the receptor signal transduction cascade at sites further downstream, rather than an immune-mediated phenomenon.” The body appears to enhance the production of GHRH receptors instead of down-regulating them. This action would prevent the onset of tachyphylaxis and thus the effect of Sermorelin would be maintained without increasing its dose. Experimental studies report that the peptide exhibits moderate side effects, low oral bioavailability, and excellent subcutaneous bioavailability in mice. Per kg dosage in mice does not match up to human requirements.
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