Overview
Hexarelin is a synthetic hexapeptide member of the GHRP family with potent GH-releasing activity. It is unique among GHRPs for its demonstrated direct cardiovascular effects that are independent of GH secretion. Hexarelin binds to CD36, a multifunctional scavenger receptor expressed in cardiomyocytes and microvascular endothelial cells, triggering dose-dependent coronary vasoconstriction and conferring cardioprotective effects against ischemia-reperfusion injury in GH-deficient and senescent animals.
Mechanism of Action
Hexarelin acts via two distinct mechanisms: (1) GHS-R1a receptor binding in pituitary and hypothalamus to drive GH secretion via PKC signaling; (2) direct binding to cardiac CD36 receptors, modulating coronary vascular tone and providing cardioprotection through L-type calcium channel involvement. The cardiac receptor is distinct from pituitary GHS-R1a, explaining the GH-independent cardiac effects. It also blocks SMC phenotype switching and NF-κB inflammatory signaling.
Potential Benefits
- Potent GH secretagogue comparable to GHRP-6
- GH release at both pituitary and hypothalamic levels
- Unique direct cardioprotective effects via CD36 activation
- Protection against postischemic ventricular dysfunction
- Stimulates IGF-1 in short-stature children
- Anti-inflammatory via NF-κB inhibition
- Potential cardiac remodeling benefits in heart failure
Research Dosage Notes
The following reflects doses used in published research studies. This is not medical advice.
Research doses: 100-200 mcg subcutaneously 2-3x/day. Cardiac studies have used 80 mcg/kg in rodent models.
Amino Acid Sequence
His-D-2-MeTrp-Ala-Trp-D-Phe-Lys-NH2
Side Effects & Safety
- Cortisol and prolactin elevation
- Appetite stimulation
- Cardiac effects (coronary vasoconstriction) may limit therapeutic use
- Water retention
- Desensitization with chronic use
Synergistic Compounds
The following compounds have been studied alongside Hexarelin for potential complementary or synergistic effects:
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References & Further Reading
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