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Hexarelin

Examorelin, HEX

Quick Stats
Studies 233
Trials 61
Score 2
2003 pubmed

Targeting the ghrelin receptor: orally active GHS and cortistatin analogs.

Deghenghi. Romano R; Broglio. Fabio F; Papotti. Mauro M; Muccioli. Giampiero G; Ghigo. Ezio E

Key Findings

  • Ghrelin and synthetic growth‑hormone secretagogues (GHS) have multiple effects beyond just raising GH levels, including appetite stimulation and cardiovascular actions.
  • Both agonists (activators) and antagonists (blockers) of the ghrelin receptor are being explored for treating eating disorders, obesity, and GH deficiency.
  • An oral, selective peptidomimetic GHS called EP1572 and the natural peptide cortistatin are under investigation as potential therapeutic agents.

Practical Outcomes

  • While the research points to future oral ghrelin‑receptor activators that might help with growth‑hormone support or appetite control, there are no ready‑to‑use protocols or dosage guidelines for biohackers yet. The main takeaway is that oral GHS analogs are being explored, but they remain experimental and not yet practical for self‑directed use.

Summary

The paper talks about ghrelin and man‑made compounds that stick to the same receptor, which can boost growth hormone, affect hunger, gut function, heart health, and even slow cell growth. Researchers are looking for natural and synthetic molecules that can turn the receptor on or off, which could help with things like appetite control, obesity, or growth‑hormone deficiency. One oral compound called EP1572 and a natural peptide called cortistatin are being studied, but no concrete dosing or usage advice is given yet.

Abstract

Ghrelin has been discovered as a natural ligand of the receptor specific for synthetic GH secretagogues (GHS). Ghrelin as well as synthetic GHS not only possess a remarkable GH-releasing activity but are also endowed with other endocrine and nonendocrine activities including orexigenic action, influence on gastro-enteropancreatic functions, and cardiovascular and anti-proliferative effects. Based on these data, particular effort has been focused on the isolation of new putative natural ligands of the GHS-receptors (GHS-R) and on the identification of synthetic compounds endowed with agonistic or antagonistic activity. For instance, ghrelin analogs acting as agonists or antagonists would be able to enhance or reduce appetite and food intake; these molecules would receive obvious interest for treatment of eating disorders and obesity, respectively. Ghrelin and its orally active, agonistic analogs could have prespectives for diagnosis and treatment of GH insufficiency. In this context, EP1572, a selective, orally active, peptidomimetic GHS as well as cortistatin, another putative, natural ligand of the GHS-R, and its analogs, are currently under investigation.

Study Information

Provider

pubmed

Year

2003

DOI

10.1385/endo:22:1:13