Ipamorelin 5mg

Ipamorelin — Selective Growth Hormone Secretagogue for Endocrine and Regenerative Research

Chemical and Biochemical Characteristics

• Amino Acid Sequence: Aib-His-D-2Nal-D-Phe-Lys

• Molecular Formula: C₃₈H₄₉N₉O₅

• Molecular Weight: 711.87 g/mol

• CAS Number: 170851-70-4

• PubChem CID: 9831659

• Peptide Class: Growth Hormone Releasing Peptide (GHRP) analogue

• Receptor Target: Ghrelin/Growth Hormone Secretagogue Receptor (GHS-R1a)

• Structure Type: Short linear pentapeptide, synthetic, D-amino acid–stabilized

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Overview

Ipamorelin is a synthetic GHRP-class peptide that selectively stimulates the release of growth hormone (GH) from the anterior pituitary.
Unlike earlier secretagogues such as GHRP-2 and GHRP-6, Ipamorelin does not elevate cortisol, prolactin, or ACTH levels, and does not stimulate appetite via ghrelin.

This makes Ipamorelin one of the most selective and physiologically clean GH secretagogues known to date.
Its pharmacological precision has made it a focus of scientific research in muscle preservation, bone density, endocrine modulation, and recovery physiology.

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Mechanism of Action

Ipamorelin acts as a selective agonist of the GHS-R1a (ghrelin receptor) located on somatotropic cells of the anterior pituitary.
Upon binding, it activates a calcium-dependent signaling cascade that triggers GH secretion while sparing other pituitary hormones.

Key biological features include:

• Selective GH release without affecting ACTH, prolactin, FSH, LH, TSH, or cortisol;

• No stimulation of appetite or ghrelin increase;

• Improved nitrogen balance and muscle anabolism;

• Modulation of glucocorticoid-induced catabolic effects.

These attributes distinguish Ipamorelin as a high-specificity model compound for GH pathway research.

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Ipamorelin and Glucocorticoid-Induced Side Effects

Chronic glucocorticoid therapy is known to cause bone demineralization, muscle wasting, and metabolic imbalance.
Research has shown that Ipamorelin can counteract or even reverse several adverse effects of prolonged steroid exposure.

• In rodent models, Ipamorelin completely prevented bone loss induced by corticosteroids and increased bone formation four-fold compared to controls【2】.

• It improved mineral density and structural strength of both new and existing bone tissue【3】.

• Ipamorelin also helped reduce visceral fat accumulation and muscle catabolism associated with steroid use.

These effects make it a valuable compound for studying bone metabolism and anabolic recovery under glucocorticoid stress.

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Ipamorelin and Muscle Growth

Studies have demonstrated that Ipamorelin can mitigate muscle catabolism and promote positive nitrogen retention in glucocorticoid-treated animals.
By reducing hepatic nitrogen loss and improving urea cycle efficiency【4】, the peptide helps maintain lean mass during metabolic stress.
This anabolic balance suggests potential research use in muscle atrophy, recovery, and cachexia models.

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Ipamorelin and Bone Health

Ipamorelin’s influence on the osteoblastic and mineralization processes has been well documented.
In controlled studies, it:

• Prevented steroid-induced bone demineralization;

• Stimulated osteoblast activity and bone remodeling;

• Improved overall bone mechanical strength.

This selective GH release without affecting cortisol levels provides an ideal model to study hormone-induced osteogenesis.

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Ipamorelin and Insulin Regulation

In diabetic rat models, Ipamorelin enhanced insulin secretion via calcium-channel modulation in pancreatic islet β-cells【5】.
This suggests potential metabolic regulatory roles relevant to insulin sensitivity, pancreatic function, and glucose homeostasis research.

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Postoperative Ileus (POI) Research

Ipamorelin has been investigated in clinical proof-of-concept trials for the management of postoperative ileus (intestinal motility suppression following surgery).
Data showed that treatment reduced the time to first oral intake by approximately 12 hours, improving gastrointestinal recovery【6】【7】.
Although development for this indication was later discontinued due to limited efficacy, these findings established Ipamorelin as a safe, well-tolerated ghrelin mimetic with measurable GI activity.

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Imaging and Diagnostic Applications

Because ghrelin receptors are overexpressed in certain cancers and cardiac pathologies, Ipamorelin has been proposed as a PET imaging probe for ghrelin receptor distribution.
In vitro studies confirmed that Ipamorelin derivatives can serve as radiolabeled tracers for diagnostic imaging, offering potential applications in oncology and cardiometabolic research【8】.

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Current Research Outlook

Despite early promise, Ipamorelin remains underexplored in modern peptide research.
Its clean receptor selectivity and favorable pharmacokinetics make it suitable for diverse research directions, including:

• Bone regeneration and osteoporosis;

• Glucocorticoid counteraction;

• Muscle preservation and anabolic recovery;

• Endocrine receptor mapping and imaging.

As scientific interest in selective GH secretagogues revives, Ipamorelin is expected to regain attention as a benchmark model for next-generation GHS compounds.

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Summary

Ipamorelin represents a next-generation growth hormone secretagogue with unmatched receptor selectivity and minimal endocrine interference.
It provides an advanced model for research in:

• Growth hormone signaling;

• Bone and muscle metabolism;

• Steroid-induced tissue degeneration;

• Ghrelin receptor pharmacology and imaging applications.

By isolating GH-specific pathways without triggering cortisol or prolactin release, Ipamorelin helps researchers explore precise hormonal regulation and tissue recovery mechanisms.

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Selected References

1. Raun K. et al. Ipamorelin, the first selective growth hormone secretagogue. Eur J Endocrinol, 1998; 139(5): 552–561. [PubMed]

2. Andersen N.B. et al. Ipamorelin counteracts glucocorticoid-induced bone formation decrease in adult rats. Growth Horm IGF Res, 2001; 11(5): 266–272. [PubMed]

3. Svensson J. et al. GH secretagogues ipamorelin and GHRP-6 increase bone mineral content in adult female rats. J Endocrinol, 2000; 165(3): 569–577. [PubMed]

4. Aagaard N.K. et al. Growth hormone secretagogue effects on nitrogen balance and urea synthesis in steroid-treated rats. Growth Horm IGF Res, 2009; 19(5): 426–431. [PubMed]

5. Adeghate E., Ponery A.S. Mechanism of ipamorelin-evoked insulin release from pancreas of diabetic rats. Neuro Endocrinol Lett, 2004; 25(6): 403–406. [PubMed]

6. Beck D.E. et al. Proof-of-concept study of ghrelin mimetic Ipamorelin in postoperative ileus. Int J Colorectal Dis, 2014; 29(12): 1527–1534. [PubMed]

7. Greenwood-Van Meerveld B. et al. Efficacy of Ipamorelin on gastric dysmotility in rodent POI model. J Exp Pharmacol, 2012; 4: 149–155. [PubMed]

8. Fowkes M.M. et al. Peptidomimetic GHS derivatives for PET imaging of ghrelin receptors. Eur J Med Chem, 2018; 157: 1500–1511. [ScienceDirect]

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