SleepMuscle GrowthWell-evidencedHuman trials

Ghrelin

Ghrelin

Overview

Ghrelin is a 28-amino-acid peptide hormone produced primarily in the stomach that functions as the body's primary hunger signal and a potent GH secretagogue. It is often called the hunger hormone and plays central roles in energy homeostasis appetite regulation GH secretion and metabolic function. Ghrelin declines after meals and rises before them creating the hunger drive. Beyond appetite ghrelin has important effects on sleep cardiovascular function immune modulation and stress response. It is the endogenous ligand for the ghrelin receptor that synthetic compounds like MK-677 and Hexarelin target.

Mechanism of Action

Ghrelin acts through the growth hormone secretagogue receptor (GHSR-1a) expressed in the hypothalamus pituitary stomach and other tissues. In the hypothalamus it activates neuropeptide Y and AgRP neurons in the arcuate nucleus stimulating appetite and reducing energy expenditure. In the pituitary it synergizes with GHRH to produce robust GH pulses. Ghrelin exists in two forms: acylated ghrelin (AG) which is the active form that crosses the blood-brain barrier and activates GHSR-1a and desacyl ghrelin (DAG) which has distinct effects including anti-inflammatory and cardioprotective actions through different receptors. Circulating ghrelin levels are highest during fasting and lowest after eating. In sleep ghrelin promotes slow-wave sleep and is thought to mediate some of the GH release that occurs during deep sleep stages.

Where does Ghrelin sit?

See how this peptide compares across all 85 peptides in our database.

Dosage Information

Typical Dose

N/A — reference compound. See MK-677 or Hexarelin for ghrelin receptor agonists

Frequency

N/A

Administration

Reference compound

Notes

Native ghrelin is not used therapeutically due to short half-life and complex acylation requirements. This entry provides mechanistic context for the ghrelin receptor agonist class including MK-677 and all GHRPs.

Compound Data

Ghrelin structure

Molecular Formula

C149H249N47O42

Molecular Weight

3370.90 g/mol

IUPAC Name

(4S)-4-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-hydroxypropanoyl]amino]-3-octanoyloxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-5-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[(2S)-2-[(2S)-2-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[(2S)-2-[[(1S)-4-carbamimidamido-1-carboxybutyl]carbamoyl]pyrrolidin-1-yl]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid

PubChem CID

16133832

Potential Side Effects

N/A for native ghrelin — see ghrelin receptor agonist entries

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Quick Facts

Administration
Reference compound
Typical Dose
N/A — reference compound. See MK-677 or Hexarelin for ghrelin receptor agonists
Frequency
N/A
References
0 curated + 47 from PubMed
Clinical Trials
48 registered
Evidence Score
80.0 / 100