Ipamorelin

Ipamorelin Overview

Ipamorelin Overview: Ipamorelin is a synthetic pentapeptide recognized as a highly potent and selective agonist of the growth hormone secretagogue receptor (GHS-R1a), also known as the ghrelin receptor. In the landscape of biochemical research, Ipamorelin is distinguished by its ability to elicit a strong growth hormone pulse without the concomitant release of other pituitary hormones such as prolactin, ACTH, or cortisol. This precision makes it an invaluable model for studying the isolated pathways of growth hormone secretion and its downstream effects on systemic metabolism, tissue repair, and skeletal maintenance.

Ipamorelin Structure

The molecular architecture of Ipamorelin is designed for high affinity and stability within biological environments.

• Structure Solution Formula: 2-methylalanyl-L-histidyl-3-(2-naphthyl)-D-alanyl-D-phenylalanyl-L-lysinamide
• Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH2

Ipamorelin Research

Target System

Observed Biological Effect

Research Implication

Endocrine

Selective GH pulse without cortisol elevation

Hormonal specificity studies

Musculoskeletal

Prevention of nitrogen loss and bone degradation

Catabolic state reversal

Gastrointestinal

Restoration of contractile function

Motility disorder modeling

Diagnostic

Ghrelin receptor binding for PET imaging

Oncological detection methods

1. Ipamorelin and Negative Corticosteroid Effects

Glucocorticoids are essential for managing severe inflammatory responses, yet their long-term application is often derailed by deleterious side effects. Ipamorelin has become a subject of interest for its potential to serve as a protective adjunct. Animal models suggest that by maintaining growth hormone levels, Ipamorelin may offset the catabolic damage caused by high-dose steroids, allowing for potentially longer or more intensive therapeutic windows.

2. Ipamorelin and Bone Health

The skeletal system is highly susceptible to the thinning effects of prolonged corticosteroid use. Ipamorelin research indicates a significant capacity to preserve bone mineral density. In laboratory rats, administration of the peptide not only halted bone resorption but facilitated the formation of new bone tissue. This dual-action mechanism is currently a focal point for studies regarding age-related osteoporosis and recovery from stress fractures.

3. Ipamorelin and Muscle Growth

Research focusing on nitrogen balance—a primary marker for muscle health—shows that Ipamorelin can inhibit the muscle-wasting effects of glucocorticoids. By reducing hepatic nitrogen wasting, the peptide helps maintain protein synthesis in muscle tissue. This suggests a potential role for Ipamorelin in studying treatments for muscle atrophy and chronic wasting diseases.

4. Ipamorelin and Diabetes

In studies utilizing diabetic rat models, Ipamorelin was shown to stimulate insulin release. This suggests the peptide may play a role in supporting the functional lifespan of pancreatic islets. By enhancing insulin production during periods of low beta-cell activity, Ipamorelin provides a pathway for investigating preventative measures against the onset of metabolic failure.

5. Studies for Treatment of Post-Operative Ileus

Post-operative ileus (POI) remains a significant barrier to surgical recovery. Research indicates that Ipamorelin can restore gastrointestinal motility within 12 hours of administration. While these findings were not sufficient for standalone pharmaceutical commercialization, the data regarding food redistribution in the GI tract remains highly significant for researchers looking into synergistic gastroprokinetic therapies.

6. Ipamorelin as Ghrelin Receptor Probe

Beyond hormone regulation, Ipamorelin serves as a diagnostic tool. Its high binding affinity for ghrelin receptors—which are often over-expressed in certain carcinomas—allows it to act as a molecular probe. This facilitates the development of high-resolution PET scans for detecting malignancies and assessing the severity of heart failure conditions.

Ipamorelin Is Neglected in Research

Despite its lack of orphan drug designation, Ipamorelin is gaining renewed interest in academic circles. Researchers are particularly drawn to its low side-effect profile and high subcutaneous bioavailability. In rodent studies, the peptide has shown a remarkable ability to normalize the geometric positioning of food in the GI tract following surgical trauma.

Storage

Ipamorelin should be stored in a cool, dry environment. For long-term stability, lyophilized powder should be kept at -20 degrees Celsius. Once reconstituted, the solution should be refrigerated at 2 to 8 degrees Celsius and used within a short timeframe to prevent degradation.

Article Author

The above content was researched, edited, and organized by Dr. Logan, M.D. Dr. Logan possesses 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. David E. Beck, MD is being referenced as one of the leading scientists involved in the research and development of ipamorelin. In no way1 is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any r2eason. There is no affiliation or relationship, implied or otherwise, between Peptide Sciences and this doctor.

Referenced Citations

1. K. Raun et al., "Ipamorelin, the first selective growth hormone secretagogue," Eur. J. Endocrinol., vol. 139, no. 5, pp. 552-561, Nov. 1998.
2. N. B. Andersen et al., "The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decreases in bone formation of adult rats," Growth Horm. IGF Res., vol. 11, no. 5, pp. 266-272, Oct. 2001.
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.
4. N. K. Aasgaard et al., "Growth hormone and growth hormone secretagogue effects on nitrogen balance and urea synthesis in steroid treated rats," Growth Horm. IGF Res., vol. 19, no. 5, pp. 426-431, Oct. 2009.
5. E. Adegoke and A. S. Ponrny, "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.
6. D. E. Beck et al., "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.
7. B. Greenwood-Van Meerveld et al., "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.
8. M. M. Fowkes et al., "Peptidominetic growth hormone secretagogue derivatives for positron emission tomography imaging of the ghrelin receptor," Eur. J. Med. Chem., vol. 157, pp. 1506-1511, Sep. 2018.