Ipamorelin

What Is Ipamorelin?

Ipamorelin represents a short peptide sequence with binding capability to the ghrelin/growth hormone secretagogue receptor. It is known as a selective growth hormone (GH) secretagogue that primarily stimulates GH release from the pituitary gland [1]. Laboratory studies have demonstrated its limited effects on the release of ACTH, prolactin, follicle-stimulating hormone, luteinizing hormone, thyroid-stimulating hormone, and cortisol. This high specificity makes ipamorelin valuable for research purposes, both as a therapeutic agent and as a model peptide for comprehending selectivity mechanisms in ghrelin receptor activation.

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Chemical Details

• Formula: C38H49N9O5
• Molecular Weight: 711.86 g/mol
• Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH2

Ipamorelin Research

1. Ipamorelin and Negative Corticosteroid Effects

Glucocorticoids, the class of corticosteroids used to address inflammation, carry a range of serious side effects that commonly restrict their therapeutic utility. Ipamorelin has demonstrated in animal studies its capacity to mitigate the adverse effects of glucocorticoid administration. Reducing these adverse effects could potentially enable higher medication dosages to remain active for extended durations, which might yield positive research outcomes.

2. Ipamorelin and Bone Health

One of the most significant problems linked to extended glucocorticoid administration is decreased bone density and heightened fracture risk. Current therapeutic approaches, while effective individually, often carry side effects, demonstrate limited efficacy, or incur high costs. Ipamorelin, conversely, offers the potential to completely reverse these effects through a highly restricted range of side effects [2]. Rat studies reveal that ipamorelin can fully prevent bone loss attributable to corticosteroid administration and may even stimulate bone formation. Additional research demonstrates that ipamorelin also enhances bone mineral density substantially, thereby improving strength and potentially lowering fracture risk [3]. In animal models, ipamorelin helps mitigate various other side effects of steroids extending beyond bone to internal organ disposition.

3. Ipamorelin and Muscle Growth

Evidence suggests that GH and growth hormone secretagogues such as ipamorelin may diminish the catabolic effects that glucocorticoids exert on muscle tissue. Rat research given glucocorticoids demonstrates a reduction in nitrogen wasting in the liver and a decrease in nitrogen balance after ipamorelin administration [4]. Muscle wasting constitutes one of the most prevalent side effects linked to glucocorticoid use. Studies indicate that combining ipamorelin with a single dose might prove highly advantageous for patients requiring glucocorticoid therapy.

4. Ipamorelin and Diabetes

Diabetic rat research has shown that ipamorelin can facilitate insulin release [5]. This effect is particularly beneficial during periods of reduced stimulation of pancreatic beta cells where insulin production and storage occur. Ipamorelin's effects on the pancreas involve better long-term functional capacity of pancreatic islets and contribute to developing novel therapeutic or preventative measures.

5. Studies for Treatment of Post-Operative Ileus (POI)

Post-operative ileus (POI) represents a condition that develops following certain surgical procedures, where the GI system remains in a dormant state. Ipamorelin has undergone investigation in multiple proof-of-concept clinical studies to assess whether peptide administration can reduce POI. Research indicates that ipamorelin does facilitate motility restoration within 12 hours following administration [6], [7]. Unfortunately, these studies revealed that ipamorelin's effectiveness proved insufficient to establish it as a commercially viable product. Hope exists that continuing research can improve efficacy.

The geometric positioning of food shows similarity to rats without POI when rats with POI receive ipamorelin.

6. Ipamorelin as Ghrelin Receptor Probe

Ipamorelin functions as a selective ghrelin receptor agonist and demonstrates strong binding affinity. Given that this receptor plays a significant role in increasing the abundance of cancer cells, researchers have recognized that ipamorelin could serve as a probe for tumors, such as for diagnosis using techniques like positron emission tomography (PET) scanning [8]. In vitro research has established the viability of this methodology and validated that ipamorelin effectively labels tumors.

Ipamorelin Is Neglected in Research

While ipamorelin lacks orphan drug designation at present, it remains a neglected focus in research environments. Despite limited early studies, interest in ipamorelin has grown significantly in recent years. Ipamorelin demonstrates interest in numerous disease conditions along with their physiologic effects. Ipamorelin shows moderate side effects, low oral and excellent subcutaneous bioavailability in mice. Ipamorelin is restricted to educational and scientific research purposes only, but licensed researchers may access it.

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 a key study on ipamorelin, 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 way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Peptide Sciences and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development work conducted by the scientists studying this peptide.

Referenced Citations

Citation #

Summary of Topic

Year

[1]

Ipamorelin, the first selective growth hormone secretagogue

1998

[2]

Ipamorelin counteracts glucocorticoid-induced decreases in bone formation

2001

[3]

Ipamorelin and GHRP-6 increase bone mineral content in adult female rats

2000

[4]

GH and GH secretagogue effects on nitrogen balance in steroid treated rats

2009

[5]

Mechanism of ipamorelin-evoked insulin release in normal and diabetic rats

2004

[6]

Study of Ipamorelin for the management of postoperative ileus

2014

[7]

Efficacy of ipamorelin on gastric dysmotility in rodent POI model

2012

[8]

Peptidominetic derivatives for PET imaging of the ghrelin receptor

2018