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Hexarelin (also known as Examorelin) is a synthetic hexapeptide analog of ghrelin with selective agonist activity at the ghrelin/growth hormone secretagogue receptor (GHS-R). In research settings, it is investigated for its effects on growth hormone release dynamics, receptor binding characteristics, and pituitary-hypothalamic signaling pathways, making it a subject of interest in studies on neuroendocrine regulation, cellular protection mechanisms, and secretagogue receptor pharmacology.
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Hexarelin functions as a multi-receptor peptide agonist influencing growth hormone release, metabolic signaling, and cardiovascular responses through GHS-R1a and CD36 receptor pathways. As a synthetic hexapeptide growth hormone secretagogue (GHS) that acts as a potent agonist of the growth hormone secretagogue receptor type 1a (GHS-R1a, or ghrelin receptor), hexarelin demonstrates enhanced stability and potency compared to natural ghrelin. Research models examine hexarelin’s effects on GH pulsatility, IGF-1 production, cardiac function, and metabolic regulation in laboratory and preclinical experimental settings, with particular interest in its cardioprotective and metabolic actions.
Hexarelin was developed in the 1990s as part of systematic research into growth hormone-releasing peptides (GHRPs), following the identification of GHRP-6 and other early GHS compounds. Synthesized to optimize GH-releasing potency and duration of action, hexarelin emerged as one of the most potent synthetic GHS compounds. Subsequent research revealed its unexpected cardioprotective effects independent of growth hormone, leading to expanded investigation of its cardiovascular applications.
CAS#: 140703-51-1
Molecular Formula: C₄₇H₅₈N₁₂O₆
Molecular Weight: 887.04 g/mol
PubChem ID: 6918245
Hexarelin has been investigated in growth hormone secretagogue research and cardiovascular pharmacology studies, with particular focus on GHS-R1a receptor activation, cardiac protection mechanisms, metabolic effects, and multi-tissue signaling responses in experimental animal models and cellular assays.
Key Areas of Research:
• Endocrine regulation: GH secretion, IGF-1 production, pituitary receptor expression
• Cardiovascular function: Cardioprotection, ischemia-reperfusion injury, cardiac remodeling
• Metabolic signaling: Lipid metabolism, insulin sensitivity, energy homeostasis
• Receptor pharmacology: GHS-R1a activation, CD36 binding, receptor tissue distribution
These findings demonstrate hexarelin’s versatility as a research compound across endocrine, cardiovascular, and metabolic systems. Through dual receptor engagement (GHS-R1a and CD36), hexarelin provides a unique experimental platform for studying growth hormone regulation, cardiac protection mechanisms, and integrated metabolic-cardiovascular signaling in diverse research models.
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