GHRP-6

GHRP-6 is a synthetic hexapeptide and met-enkephalin analog widely used in research to study ghrelin receptor (GHSR-1a) signaling, growth hormone (GH) physiology, and related intracellular pathways. It also interacts with the CD36 receptor, making it a valuable tool for exploring cellular metabolism and inflammatory pathways. Ghrelin Receptor Activation

GHRP-6 binds to the GHSR-1a receptor, initiating signaling cascades involving:

  • Phosphatidylinositol turnover
  • Protein kinase C
  • Intracellular calcium mobilization
  • cAMP-independent pathways

Pituitary / Endocrine Studies
Research models demonstrate that GHRP-6 can stimulate GH release from somatotrophs and may act synergistically with endogenous GHRH in controlled laboratory settings.
Cellular Pathway Exploration

Preclinical experiments have used GHRP-6 to investigate:

  • Oxidative-stress–related pathways
  • Inflammatory signaling
  • Fibrotic mechanisms and Bcl-2 gene expression
  • Receptor-mediated cellular protection models

These findings are limited to in vitro, ex vivo, and animal studies.

  1. Berlanga-Acosta J, et al. Synthetic growth hormone-releasing peptides (GHRPs): A historical appraisal of the evidences supporting their cytoprotective effects. Clin Med Insights Cardiol. 2017;11:1179546817694558.
  2. Popovic V, et al. Blocked GHRP-6-induced GH secretion and absence of synergy with GHRH in hypothalamopituitary disconnection. J Clin Endocrinol Metab. 1995;80(9):2723–2727.
  3. Adams EF, et al. GHRP-6 stimulates phosphatidylinositol turnover in human pituitary somatotroph cells. J Endocrinol. 1995;145(1):35–41.
  4. Berlanga-Acosta J, et al. GHRP-6 prevents doxorubicin-induced myocardial and extra-myocardial damage via prosurvival mechanisms. Front Pharmacol. 2024;15:1402138.
  5. Nass R, et al. Effects of an oral ghrelin mimetic on body composition and clinical outcomes in healthy older adults. Ann Intern Med. 2008;149(9):601–611.

*Summaries below describe preclinical research only. Not indicative of human therapeutic effects.

  • Endocrine Function Studies: GHRP-6 is frequently utilized to study pulsatile GH release, ghrelin biology, and hypothalamic-pituitary axis regulation.
  • Metabolic & Cellular Models: Experimental systems have examined lipid metabolism markers, mitochondrial activity, and intracellular antioxidant responses following GHRP-6 exposure.
  • Tissue & Fibrosis Research: In vitro and animal models have explored GHRP-6’s effect on:
  • Fibrosis-related gene expression
  • Cellular stress response pathways
  • Bcl-2 modulation
  • Oxidative stress markers
  • Neurological / Sleep Pathway Modeling: Preclinical studies have evaluated potential effects on REM-associated neural circuits and slow-wave sleep markers, exclusively in animal models.

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