Ipamorelin is a pentapeptide, meaning that its structure is comprised of five amino acids. It is a GH secretagogue, and is considered to be an agonist, meaning that it possesses the ability to bind certain receptors of a cell and provokes a cellular response. Ipamorelin’s operational mechanics enables the peptide to stimulate the production of pituitary gland-based expression of secretions related to growth amongst animal test subjects. At the same time, the presence of the peptide has been shown to inhibit the production of a secretion known as somatostatin. Additionally, it has been determined that Ipamorelin has the ability to boost the production of IGF-1, or Insulin-like Growth Factor 1. Its presence plays a key role in the overall growth and repair of muscular and skeletal tissue.
- Chemical Formula: C38H49N9O5 · xC2H4O2
- Molecular Mass: 711.9
- Synonyms: 2-Methylalanyl-L-histidyl-3-(2-naphthyl)-D-alanyl-D-phenylalanyl-L-lysinamide, 170851-70-4, C38H49N9O5, CHEMBL58547, SCHEMBL183305, SCHEMBL8169698, MolPort-039-139-953, 5020AF, ZINC29562299, AKOS030573449, DB12370, NCGC00167295-01, FT-0696037
- Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH2
- CAS Number: 170851-70-4
- PubChem: CID 20754357
- Total Amount of the Active Ingredient: 5 mg (1 vial)
- Shelf Life: 36 months
- BONE HEALTH
Prolonged use of glucocorticoids reduces bone density and can lead to fracture. Bisphosphonates, hormone therapies, and new monoclonal antibodies are used as alternative treatments though they come with their side effects and are often expensive. Reasearch in Ipamorelin therapies suggest a potential for the peptide to become an economic and physiologically safe alternative. Studies in rats have observed that the peptide may prevent bone loss from glucocorticoid treatment, and also may induce up to a four-fold increase in bone formation. The researchers also reported that “the decrease in muscle strength and bone formation found in GC-injected rats was counteracted by simultaneous administration of the growth hormone secretagogue.” The peptide may improve the bone mineral density of both existing and new bones. Additionally, it may reverse side effects like muscle wasting and fat deposition in the body’s visceral organs.
Studies in murine models of diabetes have suggested a strong efficacy of Ipamorelin in promoting insulin release from islet cells of the pancreas. Studies observe that the peptide may mediate the release of insulin through the indirect excitation of calcium channels found on the islet cells. The mechanism of Ipamorelin action highlights the limitations of type 2 diabetes, and further research in this area may help develop novel therapeutic medicines, and lead to more strategic and effective preventive measures.
- NEGATIVE CORTICOSTEROID EFFECTS
Glucocorticoids are the kind of corticosteroids that are commonly administered to treat inflammation in diverse conditions ranging from cancer to autoimmune disease. Unfortunately, their adverse side effects restrict their use. Over long durations, a higher dose of these hormones is required to overcome their physiological ill effects. This treatment regimen hence can be near-fatal. Researchers studying the effects of Ipamorelin have observed the peptide’s potential to decrease the side effects of glucocorticoid use.
- MUSCLE GROWTH
GH and GH secretagogues such as Ipamorelin may decrease the catabolic effects of glucocorticoids on muscles. Studies on Ipamorelin posit that it helps to reestablish the nitrogen balance and reduce nitrogen wasting in the liver of rats that were treated with glucocorticoids. Thus the molecule has the potential to help to overcome both muscle wasting and loss of bone density in patients who require glucocorticoids.
- GHRELIN RECEPTOR PROBE
The peptide binds strongly to the ghrelin receptor and acts as a selective agonist. Interestingly, the ghrelin receptor has been observed to increase cardiac failure and certain types of cancer, such as human carcinomas. Researchers have proposed using Ipamorelin as a probe in positron emission tomography (PET) scans to help diagnose patients. In vitro reports have confirmed the possibility of using it. The next approach would be to perform in vivo study and optimize parameters for interpretation of the results.
- POST-OPERATIVE ILEUS
Post-operative Ileus (POI) is a common condition that often follows abdominal surgery. It is characterized by an inability of the patients to accept oral nutrition as the GI system stops functioning. It can involve pain leading to prolonged stay in hospitals and extended tenure required for recovery. Ipamorelin has been studied in multiple proof-of-concept clinical trials to determine its efficacy to reduce POI. It was found to shorten the time of uptake of the first meal by about 12 hours in POI patients. The researchers concluded that “ipamorelin accelerates gastric emptying in a rodent model of postoperative ileus through the stimulation of gastric contractility by activating a ghrelin receptor-mediated mechanism involving cholinergic excitatory neurons.” However, the trials were discarded as the company conducting them decided the efficacy of the peptide to be insufficient for a viable product. However, the use of Ipamorelin in combination with other therapies might be more useful in treating POI. Some of the research observations are as follows:
– Residual radiolabeled food remaining in the stomach of rats with POI was less after the use of Ipamorelin, even when compared to rats without POI.
– When administered Ipamorelin, the geometric location of the food was observed to be similar for both rats without POI and those with POI.
– The radiolabeled food was located more distally in the GI tract and is similar to rats without POI, after Ipamorelin is used on rats with POI.
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