GH Secretagogues Anti-aging Hormonal Modulators Peptide Hormones Under research

Hexarelin

Also known as: Examorelin, EP-23905, MF-6003

Hexarelin is a synthetic hexapeptide growth hormone secretagogue. It primarily acts through the GHS-R1a receptor, the same receptor activated by natural ghrelin. It is one of the most potent known GH secretagogues, although prolonged use generates desensitization and loss of response. Also investigated for its cardioprotective properties.

Mechanism of action

Potent GHS-R1a receptor agonist
Stimulates pulsatile GH release from the anterior pituitary
Elevates cortisol, ACTH, and prolactin (unlike ipamorelin)
Direct cardioprotective effects through GHS-R receptors in the myocardium
Anti-apoptotic effect in cardiomyocytes

Uses & indications

Endogenous GH stimulation (more potent than other GHRPs)
Cardiovascular research: Post-ischemia cardioprotection, cardiomyopathies
Body composition: Muscle hypertrophy, fat reduction

Effects

Positive effects: Higher GH peak than other GHRPs. Unique cardioprotective properties documented in animal models.

Adverse effects: Cortisol and prolactin elevation, greater water retention than ipamorelin, GHS-R1a receptor desensitization with frequent dosing (requires rest periods).

Considerations & contraindications

Not approved for human use (FDA/EMA)
Avoid continuous use without breaks (cycling recommended)
Not recommended in active diabetes (cortisol stimulation)
Contraindicated in active malignancies

Regulatory approval

Research peptide. Not approved. Investigated by Europeptides and Mediolanum Farmaceutici in Phase I–II trials for GHD and heart failure.

Dosage

100–200 μg/dose, 2–3×/day. 8-week cycles with 4-week rest to avoid desensitization.

Storage

Lyophilized: −20°C. Reconstituted: 4°C, use within 30 days.

Technical data

Regulatory status Under research

Molecular weight 887.04 Da

Half-life ~1–2 h

Administration routes Subcutánea, intravenosa