Ipamorelin 10MG

Description

Ipamorelin is a short peptide sequence that binds selectively to the ghrelin/growth hormone secretagogue receptor. It is among the most selective growth hormone (GH) secretagogues identified, with laboratory studies demonstrating no impact on the release of ACTH, prolactin, follicle-stimulating hormone (FSH), luteinizing hormone (LH), thyroid-stimulating hormone (TSH), or cortisol [1]. Due to its high specificity, ipamorelin has attracted research interest both as a potential therapeutic agent and as a model peptide to explore the mechanisms underlying selective receptor binding.

Ipamorelin Structure

Source: PubChem

Peptide Sequence: Aib-His-D-2Nal-D-Phe-Lys
Molecular Formula: C₃₈H₄₉N₉O₅
Molecular Weight: 711.868 g/mol
PubChem CID: 9831659
CAS Number: 170851-70-4

Ipamorelin Research

1. Ipamorelin and Negative Corticosteroid Effects

Glucocorticoids, a widely used class of corticosteroids for treating inflammation in conditions such as cancer and autoimmune diseases, often cause serious side effects that limit their long-term use. Reducing these adverse effects could enable higher dosing and prolonged treatment, potentially improving patient outcomes. Multiple studies have shown that ipamorelin can reduce or even reverse the negative side effects associated with glucocorticoid therapy.

2. Ipamorelin and Bone Health

A significant complication of long-term glucocorticoid use is bone density loss, increasing fracture risk. While current treatments such as bisphosphonates, hormone therapies, and monoclonal antibodies are effective, they come with drawbacks including side effects, limited efficacy, or high costs. In contrast, ipamorelin is relatively inexpensive to produce and has minimal side effects. Animal studies demonstrate that ipamorelin can halt corticosteroid-induced bone loss and stimulate bone formation up to fourfold in rats exposed to glucocorticoids [2]. Additional research shows that ipamorelin increases systemic bone mineral density, strengthening both existing and newly formed bone [3]. Furthermore, it helps mitigate other steroid side effects such as muscle wasting and increased visceral fat deposition.

3. Ipamorelin and Muscle Growth

Growth hormone and secretagogues like ipamorelin may counteract glucocorticoid-induced muscle catabolism. In rat models treated with glucocorticoids, ipamorelin administration improved nitrogen balance and reduced nitrogen wasting in the liver [4]. Since muscle wasting is a major, treatment-limiting side effect of glucocorticoids, ipamorelin’s dual action on muscle and bone preservation could offer substantial benefits for patients requiring steroid therapy.

4. Ipamorelin and Diabetes

Studies in diabetic rats indicate that ipamorelin can enhance insulin secretion, likely through indirect stimulation of calcium channels on pancreatic islet cells where insulin is synthesized and stored [5]. These findings suggest that ipamorelin may provide new insights into the functional limitations of type 2 diabetes and pave the way for novel therapeutic or preventative approaches.

5. Studied for Treatment of Post-Operative Ileus

Post-operative ileus (POI), a common complication after surgeries—especially abdominal procedures—is characterized by gastrointestinal dysfunction that prevents oral nutrition and prolongs hospital stays. Ipamorelin has undergone several proof-of-concept clinical trials aimed at reducing POI duration. Results indicate that ipamorelin can shorten the time to first oral meal by about 12 hours [6], [7]. However, despite early promise, trials were discontinued due to insufficient efficacy to support commercial development. Ongoing research hopes to enhance ipamorelin’s effectiveness, possibly through combination therapies that could produce synergistic benefits.

Source: PubMed

Additional Findings on Ipamorelin and Post-Operative Ileus

Studies using radiolabeled food in rat models of POI have shown that ipamorelin administration significantly reduces the amount of food remaining in the stomach compared to untreated POI rats—even reaching levels lower than those seen in healthy controls. Furthermore, the spatial distribution of the radiolabeled food in ipamorelin-treated POI rats closely resembles that of rats without POI, indicating more normalized gastrointestinal transit. Specifically, the radiolabeled food moves more distally through the GI tract after ipamorelin treatment, further supporting its role in restoring gastrointestinal motility disrupted by POI.

Ipamorelin as Ghrelin Receptor Probe

Ipamorelin is a selective agonist of the ghrelin receptor, which is known to be upregulated in certain cancers such as human carcinomas, as well as in heart failure. This receptor specificity has prompted researchers to investigate ipamorelin as a potential probe for positron emission tomography (PET) imaging to aid in disease diagnosis. Initial in vitro studies have demonstrated the feasibility of labeling ipamorelin for PET applications, confirming that it can be synthesized relatively easily in the laboratory [8]. The next steps involve in vivo testing to evaluate its performance and establishing protocols for clinical interpretation of PET scans using ipamorelin-based probes.

Research Status and Potential

Despite its promising profile, ipamorelin remains somewhat neglected in current research. Interest diminished after early clinical trials assessing its efficacy for post-operative ileus (POI) did not lead to further product development. However, ipamorelin’s unique properties—ranging from selective GH secretion to its potential use as a diagnostic imaging agent—underscore its value as both a therapeutic candidate and a research tool. Renewed scientific focus on this peptide, backed by new data and innovative approaches, could reinvigorate its development.

Ipamorelin exhibits moderate side effects, low oral bioavailability, but excellent subcutaneous bioavailability in animal models. Dosage scaling from mice to humans is not direct. Ipamorelin available from suppliers like Peptide Sciences is intended solely for educational and scientific research purposes and is not approved for human consumption. Purchase is restricted to licensed researchers.

Article Author

The above literature was researched, edited, and organized by Dr. Logan, M.D., who holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.

Scientific Journal Author

David E. Beck, MD, co-author of “Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients,” specializes in colon and rectal surgery. Dr. Beck is referenced as a leading scientist in ipamorelin research.

There is no endorsement or advocacy by Dr. Beck regarding the purchase, sale, or use of ipamorelin products. No affiliation or relationship exists between Peptide Sciences and Dr. Beck. This citation acknowledges the rigorous research efforts of scientists studying this peptide. Dr. Beck is listed in [6] under referenced citations.

References

1. K. Raun et al., “Ipamorelin, the first selective growth hormone secretagogue,” Eur. J. Endocrinol., vol. 139, no. 5, pp. 552–561, Nov. 1998. [PubMed]
2. N. B. Andersen, K. Malmlöf, P. B. Johansen, T. T. Andreassen, G. Ørtoft, and H. Oxlund, “The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats,” Growth Horm. IGF Res. Off. J. Growth Horm. Res. Soc. Int. IGF Res. Soc., vol. 11, no. 5, pp. 266–272, Oct. 2001. [PubMed]
3. J. Svensson et al., “The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats,” J. Endocrinol., vol. 165, no. 3, pp. 569–577, Jun. 2000. [PubMed]
4. N. K. Aagaard et al., “Growth hormone and growth hormone secretagogue effects on nitrogen balance and urea synthesis in steroid treated rats,” Growth Horm. IGF Res. Off. J. Growth Horm. Res. Soc. Int. IGF Res. Soc., vol. 19, no. 5, pp. 426–431, Oct. 2009. [PubMed]
5. E. Adeghate and A. S. Ponery, “Mechanism of ipamorelin-evoked insulin release from the pancreas of normal and diabetic rats,” Neuro Endocrinol. Lett., vol. 25, no. 6, pp. 403–406, Dec. 2004. [PubMed]
6. D. E. Beck, W. B. Sweeney, M. D. McCarter, and Ipamorelin 201 Study Group, “Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients,” Int. J. Colorectal Dis., vol. 29, no. 12, pp. 1527–1534, Dec. 2014. [PubMed]
7. B. Greenwood-Van Meerveld, K. Tyler, E. Mohammadi, and C. Pietra, “Efficacy of ipamorelin, a ghrelin mimetic, on gastric dysmotility in a rodent model of postoperative ileus,” J. Exp. Pharmacol., vol. 4, pp. 149–155, Oct. 2012. [PubMed]
8. M. M. Fowkes, T. Lalonde, L. Yu, S. Dhanvantari, M. S. Kovacs, and L. G. Luyt, “Peptidomimetic growth hormone secretagogue derivatives for positron emission tomography imaging of the ghrelin receptor,” Eur. J. Med. Chem., vol. 157, pp. 1500–1511, Sep. 2018. [Science Direct]

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