Ipamorelin is a synthetic pentapeptide that acts as a selective growth hormone secretagogue (GHS), mimicking ghrelin to stimulate growth hormone (GH) release. Its unique receptor selectivity and pharmacological profile have made it a focus of research for potential therapeutic uses, particularly in growth disorders, gastrointestinal motility, and pain management.
Mechanism of Action and Selectivity
Ipamorelin binds to the ghrelin receptor (GHSR) in the brain and peripheral tissues, selectively stimulating GH release from the pituitary gland without significantly affecting other pituitary hormones or increasing cortisol and ACTH levels, distinguishing it from other GHSs. This selectivity reduces the risk of side effects commonly seen with other GH-releasing peptides.
Clinical and Preclinical Applications
- Growth and Body Composition: Ipamorelin increases GH release, body weight, and longitudinal bone growth in animal models, with effects similar to GHRH but without desensitizing the GH response. It can also increase body fat through GH-independent mechanisms, possibly by stimulating appetite and leptin.
- Gastrointestinal Motility: In rodent models, ipamorelin accelerates gastric emptying and improves symptoms of postoperative ileus, likely via cholinergic pathways. However, a clinical trial in humans found no significant benefit over placebo for postoperative ileus, though it was well tolerated.
- Pain and Other Effects: Ipamorelin attenuates visceral and somatic pain in animal models, suggesting potential for novel pain therapies. It also mitigates chemotherapy-induced weight loss in animal studies.
Pharmacokinetics and Safety
Ipamorelin demonstrates dose-proportional pharmacokinetics, a short half-life (~2 hours), and is generally well tolerated in both animal and human studies. No significant adverse effects on other pituitary hormones or cortisol have been observed at therapeutic doses.
Ipamorelin
Ipamorelin stimulates selective growth hormone production and is a ghrelin receptor agonist. Ghrelin is a hormone produced by enteroendocrine cells (specialized cells found in the gastrointestinal tract, stomach, and pancreas) of the gastrointestinal tract that is often referred to as the “hunger hormone,” as it increases the urge to eat. Ghrelin helps prepare for food intake by increasing gastric motility (the movement of food through the stomach and into the intestines, which is controlled by muscles in the stomach and the enteric nervous system) and stimulating the secretion of gastric acid.
Ipamorelin binds to ghrelin receptors, stimulates the release of somatocrinin (a hormone released by the hypothalamus which induces the growth of human growth hormone), and inhibits somatostatin (growth hormone-inhibiting hormone that regulates the endocrine system and affects neurotransmission and cell proliferation) and suppresses its action.
It is best known for its lean muscle-growing benefits, as well as fat burning effects, accelerating injury recovery, and as an anti-aging peptide.
Muscle Growth and Maintenance
- Stimulates the pituitary gland and mimics the body’s natural release of growth hormone and ghrelin
- Promotes the growth of lean muscle by increasing collagen levels and promoting muscle regeneration
- Prevents muscle-wasting whether caused by aging or medication
- Safe for long-term use due to minimal impact on acetylcholine, prolactin, cortisol, or aldosterone
Promotes Healthy Bones
- Increases bone density and bone mineral content
- Supports bone formation, growth, and longitudinal development
Metabolic and Digestive Benefits
- Enhances metabolism and burns fat
- Improves gut health, protects against ulcers, and improves gastric tissue health
- Accelerates gastric emptying and GI tract function
Enhances Recovery and Regeneration
- Supports cartilage repair via chondrogenesis
- Improves collagen synthesis and healing of injured tissues
Strengthens the Immune System
- Increases white blood cells, T-cells, and B-cells
- Reduces inflammation and improves phagocyte activity
- Corrects metabolic states caused by disease
Prevents Cognitive Decline
- Improves cognitive function and protects brain cells
- Prevents age-related dopamine loss tied to Alzheimer’s and Parkinson’s
- Boosts memory and problem-solving skills
Additional Benefits
- Improves cardiovascular function
- Regulates blood sugar
- Increases libido and combats erectile dysfunction
- Boosts estrogen and sexual desire in women
- Enhances sleep by promoting deep (slow-wave) sleep
Possible Side Effects
Common:
- Injection site reactions
- Dry mouth
- Headache
- Nausea
- Vomiting
- Increased hunger
- Hyperactivity
- Drowsiness
- Skin flushing
Rare:
- Changes in taste
- Difficulty swallowing
- Chest tightness
- Hives
Dosing Considerations
Subcutaneous administration
Should be taken on an empty stomach, at least 30 minutes before meals
Inject slowly to avoid flushing or discomfort
IPAMORELIN: 10MG
Mix with 3mL (300 units) of BAC water
Use .3cc (30-unit) syringes for accurate measurement
8-week cycle followed by a 6-week washout period
Dose 5 consecutive days, then 2 days off per week
Initial Dose (all protocols)
100mcg (3 units), 1x/day
Remain at this dose until fully tolerated without side effects
Low Dose Protocol (general wellness, anti-aging, women)
100–300mcg, 1x/day
5 days per week with 2 days off
- 3 units = 100mcg
- 6 units = 200mcg
- 9 units = 300mcg
Standard Protocol (moderate muscle gain and fat loss)
100–300mcg, 2x/day
5 days per week with 2 days off
- 3 units = 100mcg
- 6 units = 200mcg
- 9 units = 300mcg
Maximum Protocol (aggressive muscle building and recovery)
100–300mcg, 3x/day
5 days per week with 2 days off
- 3 units = 100mcg
- 6 units = 200mcg
- 9 units = 300mcg
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