What is GHRP-6?
GHRP-6 (Growth Hormone Releasing Peptide-6) is a synthetic hexapeptide and one of the earliest discovered growth hormone secretagogues, first characterized by Bowers et al. in the 1980s. It acts as an agonist at the growth hormone secretagogue receptor (GHSR/ghrelin receptor), stimulating GH release from anterior pituitary somatotrophs. GHRP-6 contains two unnatural D-amino acids (D-tryptophan and D-phenylalanine) that confer metabolic stability and receptor selectivity. Historically, GHRP-6 played a critical role in the discovery and characterization of the ghrelin receptor — the search for the endogenous ligand of the GHRP-6 binding site ultimately led to the discovery of ghrelin by Kojima et al. in 1999. In addition to GH release, GHRP-6 is known for its appetite-stimulating properties, which are attributed to GHSR activation in hypothalamic feeding centers.
Mechanism of Action
GHRP-6 has been investigated for its agonist activity at the growth hormone secretagogue receptor 1a (GHS-R1a). Researchers observed that GHRP-6 binding activates Gq-coupled signaling, leading to phospholipase C activation, inositol trisphosphate (IP3) generation, and intracellular calcium mobilization in pituitary somatotrophs. This calcium influx triggers exocytosis of GH-containing secretory granules. Studies suggest that GHRP-6 also modulates hypothalamic signaling by stimulating GHRH neurons in the arcuate nucleus and suppressing somatostatin release from periventricular neurons, creating favorable conditions for GH pulse generation. GHRP-6 demonstrates notable appetite-stimulating effects attributed to GHSR activation in the hypothalamic feeding centers, including neuropeptide Y (NPY) and agouti-related peptide (AgRP) neurons. Researchers observed that this orexigenic effect distinguishes GHRP-6 from more selective secretagogues like ipamorelin, which releases GH with minimal appetite stimulation.
Published Research
Role in Ghrelin Discovery
Kojima et al. (1999) identified ghrelin as the endogenous ligand of the GHS-R, the receptor originally characterized through GHRP-6 binding studies. This landmark discovery established the physiological basis for growth hormone secretagogue pharmacology [1].
GH Secretagogue Characterization
Bowers CY (1998) reviewed the history and pharmacology of GHRPs, describing how GHRP-6 was one of the first synthetic peptides shown to release GH through a receptor distinct from the GHRH receptor [2].
Appetite and GH Effects
Arvat et al. (2001) investigated GHRP-6 in human subjects and characterized its dual effects on GH release and appetite stimulation. The study quantified the orexigenic response and compared it to other GH secretagogues [3].
Product Specifications
| Product | GHRP-6 Lyophilized Powder |
|---|---|
| Available Sizes | 5mg, 10mg |
| Purity | ≥99% (HPLC verified) |
| CAS Number | 87616-84-0 |
| Sequence | His-D-Trp-Ala-Trp-D-Phe-Lys-NH₂ |
| Molecular Formula | C₄₆H₅₆N₁₂O₆ |
| Molecular Weight | 873.01 g/mol |
| Appearance | White lyophilized powder in glass vial |
| Storage | Store lyophilized at -20°C. Reconstituted solution at 2-8°C, use within 21 days. |
| Testing | Third-party tested — Certificate of Analysis available |
Frequently Asked Questions
GHRP-6 is a synthetic hexapeptide that activates the growth hormone secretagogue receptor (GHSR). It was one of the earliest GH secretagogues discovered and played a key role in ghrelin receptor research.
The CAS registry number for GHRP-6 is 87616-84-0.
Yes, GHRP-6 is known for its appetite-stimulating properties due to GHSR activation in hypothalamic feeding centers. This distinguishes it from more selective GH secretagogues like ipamorelin.
Store lyophilized GHRP-6 at -20°C. Once reconstituted, store at 2-8°C and use within 21 days.
GHRP-6 and ghrelin both activate the same receptor (GHS-R1a). Research on GHRP-6 binding sites directly led to the discovery of ghrelin as the endogenous ligand in 1999.
GHRP-2 is generally considered more potent for GH release with less appetite stimulation. GHRP-6 produces robust GH release but has a more pronounced orexigenic (appetite-stimulating) effect.
References
- Kojima M, et al. Ghrelin is a growth-hormone-releasing acylated peptide from stomach. Nature. 1999;402(6762):656-660. PMID: 10604470
- Bowers CY. Growth hormone-releasing peptide (GHRP). Cell Mol Life Sci. 1998;54(12):1316-1329. PMID: 9893710
- Arvat E, et al. Endocrine activities of ghrelin, a natural growth hormone secretagogue, in humans. Eur J Endocrinol. 2001;145(5):R11-R14.
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