Overview

Ghrelin is a 28-amino acid acylated peptide hormone produced primarily by X/A-like cells of the gastric fundus. It is the endogenous ligand for the growth hormone secretagogue receptor (GHS-R1a), stimulating GH release, appetite, and gastric motility. As the only known circulating orexigenic (appetite-stimulating) hormone and the endogenous counterpart to synthetic GHS-R1a agonists like GHRP-2, GHRP-6, Ipamorelin, and MK-677, ghrelin occupies a central position in metabolic and GH physiology research. Its unique octanoyl group modification at Ser3 is essential for GHS-R1a binding.

Mechanism of Action

Acylated ghrelin (the active form, octanoylated at Ser3 by ghrelin O-acyltransferase/GOAT enzyme) binds GHS-R1a (GHSR) on pituitary somatotrophs, triggering Gq-mediated phospholipase C activation, IP3-mediated calcium release, and GH secretion. In the hypothalamus, ghrelin activates NPY/AgRP neurons while suppressing POMC neurons, powerfully stimulating appetite. In the gastrointestinal tract, ghrelin via GHS-R1a promotes gastric motility and acid secretion. Ghrelin levels rise markedly before meals (promoting hunger) and fall post-meal. Des-acyl ghrelin (without octanoyl group) has distinct biological activities via non-GHS-R1a receptors.

Potential Benefits

  • Endogenous GH secretagogue (natural GH pulse driver)
  • Understanding ghrelin enabled development of all GHS-R1a agonist drugs
  • Research target for anti-obesity drugs (ghrelin antagonists)
  • Gastroparesis treatment target (promotes gastric motility)
  • GH deficiency and cachexia therapeutic target

Dosage Protocols

The following reflects doses used in published research studies. This is not medical advice. Consult a qualified healthcare professional.

BeginnerResearch/clinical only — not a consumer peptide
IntermediateN/A
AdvancedN/A
Cycle DurationResearch protocols: hours to days

Endogenous appetite hormone. Therapeutics target ghrelin pathway (GHRPs are synthetic mimetics).

Routes of Administration

Intravenous (research) 100%

Primary research route.

Subcutaneous Moderate — rapidly degraded

Acylated ghrelin requires stable formulation.

Stacking Protocols

Popular research stacks involving Ghrelin:

Research Context Only

Endogenous ghrelin is not used in stacking — GHRP-2/GHRP-6/Ipamorelin/MK-677 are synthetic mimetics used instead.

Reconstitution

StorageRefrigerate at 2-8°C after reconstitution. Do not freeze reconstituted solution.

Typical vial sizes: 0.5-1 mg (research). Add bac water slowly down the side of the vial, swirl gently — do not shake. Use insulin syringe for precise dosing.

Need exact syringe measurements?

Amino Acid Sequence

Gly-Ser-Ser(octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-Val-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg

Side Effects & Safety

  • Appetite stimulation (primary pharmacological effect)
  • Hyperinsulinemia at pharmacological doses
  • Gastric acid secretion increase

Safety & Contraindications

This information is for educational purposes only. Consult a qualified healthcare provider before using any peptide.

Relative

Pregnancy / Lactation

Relative

Bleeding Disorders

Absolute

Active Skin Infection at Injection Site

Pharmacokinetics

Half-Life~10-30 minutes (acylated ghrelin)
StorageStore lyophilized peptide at -20°C (long-term) or 2-8°C (short-term, under 30 days). Reconstituted: refrigerate at 2-8°C and use within 28-30 days. Protect from light. Do not freeze reconstituted solution.

Synergistic Compounds

The following compounds have been studied alongside Ghrelin for potential complementary or synergistic effects:

Learn More

References & Further Reading