What Is Hexarelin?

Hexarelin (Examorelin) is a synthetic hexapeptide growth hormone secretagogue. It's one of the most potent GHRPs, producing strong GH release. Notably, hexarelin also has cardioprotective properties independent of GH, making it unique among GH secretagogues.

Sequence: His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2 Molecular Weight: 887.04 g/mol Type: Growth Hormone Releasing Peptide Receptor: Ghrelin receptor (GHS-R1a) + CD36

Key Characteristics

  • Potency: Among strongest GHRPs for GH release
  • Unique: Cardioprotective via CD36 receptor
  • Tolerance: Desensitization occurs with chronic use
  • Side Effects: Increases cortisol and prolactin

Mechanism of Action

GH Release

  • Activates ghrelin receptor (GHS-R1a) on pituitary
  • Produces dose-dependent GH release
  • Also acts on hypothalamus
  • Synergistic with GHRH

Cardioprotective Effects

Unique among GHRPs, hexarelin protects the heart:

  • Acts on CD36 (scavenger receptor) in cardiac tissue
  • Independent of GH or ghrelin receptors
  • Reduces infarct size in animal models
  • Anti-apoptotic effects on cardiomyocytes

Research Findings

GH Secretion

  • Produces very strong GH release
  • Higher peak GH than most other GHRPs
  • Develops tolerance (desensitization) with daily use
  • May require cycling or intermittent dosing

Cardiac Research

  • Protected against myocardial ischemia in multiple models
  • Improved cardiac function post-infarct
  • Effects persist even in GH-deficient animals
  • Entered clinical trials for heart failure

Comparison with Other GHRPs

FeatureHexarelinGHRP-6Ipamorelin
GH ReleaseVery HighHighModerate-High
DesensitizationSignificantMildMinimal
CortisolIncreasedIncreasedNone
ProlactinIncreasedIncreasedNone
CardioprotectionYes (CD36)SomeNo

Research Status

Hexarelin is not FDA-approved. It underwent clinical trials but development was halted. The desensitization issue limits its utility for chronic GH enhancement. It remains a research compound, with particular interest in its cardioprotective mechanisms.

Summary

Hexarelin stands out among GH secretagogues for its potent GH release and unique cardioprotective properties mediated through CD36. However, the development of tolerance with repeated use limits its practical application for sustained GH enhancement. Its cardiac effects independent of GH continue to be of scientific interest.

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