Ipamorelin overview:
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Introduction
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Ipamorelin is a synthetic pentapeptide that functions as a selective growth hormone secretagogue (GHS). It belongs to the class of GHRP (growth hormone-releasing peptides) and is one of the most selective and well-studied growth hormone secretagogues available for research purposes. Ipamorelin is notable for its high specificity for growth hormone release without significantly affecting levels of other hormones such as cortisol, prolactin, or aldosterone, which sets it apart from other GHRPs like GHRP-2 and GHRP-6.
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Molecular Formula: C38H49N9O5
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Molecular Weight: 711.868 g/mol
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Mechanism of Action:
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Ipamorelin acts as a selective agonist of the ghrelin/growth hormone secretagogue receptor (GHSR-1a). Ghrelin is a natural peptide hormone that stimulates growth hormone (GH) release from the anterior pituitary. Ipamorelin mimics the action of ghrelin by binding to the GHSR-1a receptor in the pituitary gland and hypothalamus, which triggers a cascade of intracellular events leading to the secretion of growth hormone.
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1. Receptor Binding:
Ipamorelin binds selectively to the GHSR-1a receptor on somatotroph cells in the pituitary.
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2. Calcium Release and GH Secretion:
Upon binding, Ipamorelin induces the release of intracellular calcium, which stimulates the exocytosis of growth hormone-containing vesicles.
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3. Growth Hormone Secretion Without Cortisol Elevation:
Unlike other GHRPs (e.g., GHRP-6), Ipamorelin does not significantly increase the levels of cortisol, ACTH, or prolactin, making it more targeted and reducing the risk of unwanted side effects.
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4. Negative Feedback Regulation:
Ipamorelin does not interfere with the body's natural negative feedback mechanisms regulating GH release, maintaining physiological balance.
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Pharmacokinetics
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Absorption: Ipamorelin is typically administered via subcutaneous or intravenous injection, with high bioavailability.
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Half-life: Approximately 2 hours.
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Metabolism: Ipamorelin is metabolized primarily in the liver and excreted via the kidneys.
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Duration of Action: The biological effects of Ipamorelin persist for a few hours post-administration, consistent with its half-life and receptor binding dynamics.
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Molecular Structure and Sequence
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Aib-His-D-2-Nal-D-Phe-Lys-NH2
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Aib – α-aminoisobutyric acid (non-standard amino acid)
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His – Histidine
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D-2-Nal – D-2-naphthylalanine (non-standard amino acid)
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D-Phe – D-phenylalanine
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Lys – Lysine
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The structure of Ipamorelin enhances its resistance to enzymatic degradation and increases receptor specificity, contributing to its potency and selectivity for GH secretion.
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Potential Research Applications
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1. Growth Hormone Secretion Studies – Ipamorelin is used to investigate the physiological mechanisms of GH secretion and its downstream effects.
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2. Muscle Growth and Regeneration – Research has explored Ipamorelin’s effects on muscle protein synthesis and repair mechanisms.
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3. Anti-Aging and Metabolic Studies – Its selective GH-stimulating properties make it a candidate for studying age-related GH decline and metabolic health.
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4. Bone Density and Fracture Healing – GH plays a key role in bone metabolism, making Ipamorelin useful for studying skeletal health and injury recovery.
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Safety Profile and Adverse Effects
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While Ipamorelin is considered highly selective and well-tolerated in research models, potential adverse effects include:
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Mild water retention
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Transient headache
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Injection site irritation
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No significant increases in cortisol, ACTH, or prolactin have been reported at research doses, distinguishing Ipamorelin from other GHRPs.
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For Research Use Only
Ipamorelin is strictly intended for laboratory research purposes and is not approved for human use, consumption, or medical treatment. It should only be handled by qualified professionals in a controlled research environment. Any misuse or administration to humans is strictly prohibited and may result in adverse health effects.