Growth-Hormone Releasing Peptide

Hexarelin

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Overview

A potent secretagogue with additional cardiovascular receptor (CD36) interest in preclinical work; not approved.

How it works

Hexarelin is a potent growth-hormone-releasing peptide in the same ghrelin-receptor family, but with an extra twist.

Besides triggering strong GH release through the ghrelin receptor, it also binds CD36, a receptor found in cardiovascular tissue — which prompted preclinical interest in possible heart-protective effects. One quirk seen in studies is that its GH-releasing effect can fade with continuous dosing as the system desensitizes.

It's an injectable research compound and is not approved for human use.

Mechanism · Detailed Analysis

Molecular targetA potent GHS-R1a agonist that also binds CD36 in cardiovascular tissue.

Signaling & downstream effectsStrong GH release; the CD36 interaction prompted preclinical cardioprotection interest. GH response may desensitise with continuous dosing.

CaveatsNot approved.

Published EvidenceFree · cited live from PubMed

Human Data 191

Review

We are ageing

Kolovou GD et al. · BioMed research international · 2014 — PMID 25045704 ↗

Review

Growth hormone-releasing peptides

Ghigo E et al. · European journal of endocrinology · 1997 — PMID 9186261 ↗

Review

The Safety and Efficacy of Growth Hormone Secretagogues

Sigalos JT et al. · Sexual medicine reviews · 2018 — PMID 28400207 ↗

Review

Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases

Mosa RM et al. · Endocrine · 2015 — PMID 25645463 ↗

Review

Growth hormone and the heart

Colao A et al. · Clinical endocrinology · 2001 — PMID 11207626 ↗

Review

The CD36-PPARγ Pathway in Metabolic Disorders

Maréchal L et al. · International journal of molecular sciences · 2018 — PMID 29883404 ↗

Review

Growth hormone in obesity

Scacchi M et al. · International journal of obesity and related metabolic disorders : journal of the International Association for the Study of Obesity · 1999 — PMID 10193871 ↗

Review

Growth hormone-releasing peptides and their analogs

Camanni F et al. · Frontiers in neuroendocrinology · 1998 — PMID 9465289 ↗

Comparative Study

Natural (ghrelin) and synthetic (hexarelin) GH secretagogues stimulate H9c2 cardiomyocyte cell proliferation

Pettersson I et al. · The Journal of endocrinology · 2002 — PMID 12379504 ↗

Research Support, Non-U.S. Gov't

Hexarelin as a test of pituitary reserve in patients with pituitary disease

Korbonits M et al. · Clinical endocrinology · 1999 — PMID 10469018 ↗

Review

Alcohol-induced Cushing syndrome. Hypercortisolism caused by alcohol abuse

Besemer F et al. · The Netherlands journal of medicine · 2011 — PMID 21934176 ↗

Clinical Trial

Interaction of the growth hormone releasing peptide hexarelin with somatostatin

Massoud AF et al. · Clinical endocrinology · 1997 — PMID 9425393 ↗

See all 191 on PubMed →

Animal 106

Study

Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway

Guan C et al. · European journal of medical research · 2023 — PMID 37710348 ↗

Research Support, Non-U.S. Gov't

Hexarelin attenuates abdominal aortic aneurysm formation by inhibiting SMC phenotype switch and inflammasome activation

Jiang B et al. · Microvascular research · 2022 — PMID 34856183 ↗

Research Support, Non-U.S. Gov't

Hexarelin protects cardiac H9C2 cells from angiotensin II-induced hypertrophy via the regulation of autophagy

Agbo E et al. · Die Pharmazie · 2019 — PMID 31526442 ↗

Research Support, Non-U.S. Gov't

Hexarelin stimulation of growth hormone release and mRNA levels in an infant and adult rat model of impaired GHRH function

Torsello A et al. · Neuroendocrinology · 1997 — PMID 9067986 ↗

Research Support, Non-U.S. Gov't

Hexarelin protects H9c2 cardiomyocytes from doxorubicin-induced cell death

Filigheddu N et al. · Endocrine · 2001 — PMID 11322493 ↗

Study

Mechanism of action of hexarelin and GHRP-6: analysis of the involvement of GHRH and somatostatin in the rat

Conley LK et al. · Neuroendocrinology · 1995 — PMID 7731497 ↗

Study

Kinetics and disposition of hexarelin, a peptidic growth hormone secretagogue, in rats

Roumi M et al. · Drug metabolism and disposition: the biological fate of chemicals · 2000 — PMID 10611139 ↗

Research Support, Non-U.S. Gov't

Hexarelin suppresses cardiac fibroblast proliferation and collagen synthesis in rat

Xu X et al. · American journal of physiology. Heart and circulatory physiology · 2007 —

In Vitro 49

Study

Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway

Guan C et al. · European journal of medical research · 2023 — PMID 37710348 ↗

Study

Hexarelin Modulation of MAPK and PI3K/Akt Pathways in Neuro-2A Cells Inhibits Hydrogen Peroxide-Induced Apoptotic Toxicity

Meanti R et al. · Pharmaceuticals (Basel, Switzerland) · 2021 — PMID 34066741 ↗

Review

Looking to the future for erectile dysfunction therapies

Hatzimouratidis K et al. · Drugs · 2008 — PMID 18197727 ↗

Study

In vitro models for metabolic studies of small peptide hormones in sport drug testing

Esposito S et al. · Journal of peptide science : an official publication of the European Peptide Society · 2015 — PMID 25469748 ↗

Research Support, Non-U.S. Gov't

Rapid desensitisation of the GH secretagogue (ghrelin) receptor to hexarelin in vitro

Orkin RD et al. · Journal of endocrinological investigation · 2003 — PMID 14669829 ↗

Research Support, Non-U.S. Gov't

Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1

Demange L et al. · Journal of medicinal chemistry · 2007 — PMID 17375904 ↗

Research Support, Non-U.S. Gov't

Hexarelin Protects Rodent Pancreatic Β-Cells Function from Cytotoxic Effects of Streptozotocin Involving Mitochondrial Signalling Pathways In Vivo and In Vitro

Zhao Y et al. · PloS one · 2016 — PMID 26918825 ↗

Research Support, Non-U.S. Gov't

Metabolism of growth hormone releasing peptides

Thomas A et al. · Analytical chemistry · 2012 —

Studies are surfaced live from the U.S. National Library of Medicine (PubMed). biohackr indexes and links the published record; it does not host or alter source articles.

Published EvidenceLoading cited studies from PubMed…

Human Data ···

Searching the published record…

Animal ···

Searching the published record…

In Vitro ···

Searching the published record…

Educational aggregation of public literature. Not medical advice and not a recommendation to use any compound. Many compounds here are not approved for human use. Consult a licensed clinician.

Published EvidenceFree · cited live from PubMed

Human Data 191

Review

We are ageing

Kolovou GD et al. · BioMed research international · 2014 — PMID 25045704 ↗

Review

Growth hormone-releasing peptides

Ghigo E et al. · European journal of endocrinology · 1997 — PMID 9186261 ↗

Review

The Safety and Efficacy of Growth Hormone Secretagogues

Sigalos JT et al. · Sexual medicine reviews · 2018 — PMID 28400207 ↗

Review

Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases

Mosa RM et al. · Endocrine · 2015 — PMID 25645463 ↗

Review

Growth hormone and the heart

Colao A et al. · Clinical endocrinology · 2001 — PMID 11207626 ↗

Review

The CD36-PPARγ Pathway in Metabolic Disorders

Maréchal L et al. · International journal of molecular sciences · 2018 — PMID 29883404 ↗

Review

Growth hormone in obesity

Scacchi M et al. · International journal of obesity and related metabolic disorders : journal of the International Association for the Study of Obesity · 1999 — PMID 10193871 ↗

Review

Growth hormone-releasing peptides and their analogs

Camanni F et al. · Frontiers in neuroendocrinology · 1998 — PMID 9465289 ↗

Comparative Study

Natural (ghrelin) and synthetic (hexarelin) GH secretagogues stimulate H9c2 cardiomyocyte cell proliferation

Pettersson I et al. · The Journal of endocrinology · 2002 — PMID 12379504 ↗

Research Support, Non-U.S. Gov't

Hexarelin as a test of pituitary reserve in patients with pituitary disease

Korbonits M et al. · Clinical endocrinology · 1999 — PMID 10469018 ↗

Review

Alcohol-induced Cushing syndrome. Hypercortisolism caused by alcohol abuse

Besemer F et al. · The Netherlands journal of medicine · 2011 — PMID 21934176 ↗

Clinical Trial

Interaction of the growth hormone releasing peptide hexarelin with somatostatin

Massoud AF et al. · Clinical endocrinology · 1997 — PMID 9425393 ↗

See all 191 on PubMed →

Animal 106

Study

Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway

Guan C et al. · European journal of medical research · 2023 — PMID 37710348 ↗

Research Support, Non-U.S. Gov't

Hexarelin attenuates abdominal aortic aneurysm formation by inhibiting SMC phenotype switch and inflammasome activation

Jiang B et al. · Microvascular research · 2022 — PMID 34856183 ↗

Research Support, Non-U.S. Gov't

Hexarelin protects cardiac H9C2 cells from angiotensin II-induced hypertrophy via the regulation of autophagy

Agbo E et al. · Die Pharmazie · 2019 — PMID 31526442 ↗

Research Support, Non-U.S. Gov't

Hexarelin stimulation of growth hormone release and mRNA levels in an infant and adult rat model of impaired GHRH function

Torsello A et al. · Neuroendocrinology · 1997 — PMID 9067986 ↗

Research Support, Non-U.S. Gov't

Hexarelin protects H9c2 cardiomyocytes from doxorubicin-induced cell death

Filigheddu N et al. · Endocrine · 2001 — PMID 11322493 ↗

Study

Mechanism of action of hexarelin and GHRP-6: analysis of the involvement of GHRH and somatostatin in the rat

Conley LK et al. · Neuroendocrinology · 1995 — PMID 7731497 ↗

Study

Kinetics and disposition of hexarelin, a peptidic growth hormone secretagogue, in rats

Roumi M et al. · Drug metabolism and disposition: the biological fate of chemicals · 2000 — PMID 10611139 ↗

Research Support, Non-U.S. Gov't

Hexarelin suppresses cardiac fibroblast proliferation and collagen synthesis in rat

Xu X et al. · American journal of physiology. Heart and circulatory physiology · 2007 —

In Vitro 49

Study

Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway

Guan C et al. · European journal of medical research · 2023 — PMID 37710348 ↗

Study

Hexarelin Modulation of MAPK and PI3K/Akt Pathways in Neuro-2A Cells Inhibits Hydrogen Peroxide-Induced Apoptotic Toxicity

Meanti R et al. · Pharmaceuticals (Basel, Switzerland) · 2021 — PMID 34066741 ↗

Review

Looking to the future for erectile dysfunction therapies

Hatzimouratidis K et al. · Drugs · 2008 — PMID 18197727 ↗

Study

In vitro models for metabolic studies of small peptide hormones in sport drug testing

Esposito S et al. · Journal of peptide science : an official publication of the European Peptide Society · 2015 — PMID 25469748 ↗

Research Support, Non-U.S. Gov't

Rapid desensitisation of the GH secretagogue (ghrelin) receptor to hexarelin in vitro

Orkin RD et al. · Journal of endocrinological investigation · 2003 — PMID 14669829 ↗

Research Support, Non-U.S. Gov't

Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1

Demange L et al. · Journal of medicinal chemistry · 2007 — PMID 17375904 ↗

Research Support, Non-U.S. Gov't

Hexarelin Protects Rodent Pancreatic Β-Cells Function from Cytotoxic Effects of Streptozotocin Involving Mitochondrial Signalling Pathways In Vivo and In Vitro

Zhao Y et al. · PloS one · 2016 — PMID 26918825 ↗

Research Support, Non-U.S. Gov't

Metabolism of growth hormone releasing peptides

Thomas A et al. · Analytical chemistry · 2012 —

Studies are surfaced live from the U.S. National Library of Medicine (PubMed). biohackr indexes and links the published record; it does not host or alter source articles.

Hexarelin

We are ageing

Growth hormone-releasing peptides

The Safety and Efficacy of Growth Hormone Secretagogues

Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases

Growth hormone and the heart

The CD36-PPARγ Pathway in Metabolic Disorders

Growth hormone in obesity

Growth hormone-releasing peptides and their analogs

Natural (ghrelin) and synthetic (hexarelin) GH secretagogues stimulate H9c2 cardiomyocyte cell proliferation

Hexarelin as a test of pituitary reserve in patients with pituitary disease

Alcohol-induced Cushing syndrome. Hypercortisolism caused by alcohol abuse

Interaction of the growth hormone releasing peptide hexarelin with somatostatin

Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway

Hexarelin attenuates abdominal aortic aneurysm formation by inhibiting SMC phenotype switch and inflammasome activation

Hexarelin protects cardiac H9C2 cells from angiotensin II-induced hypertrophy via the regulation of autophagy

Hexarelin stimulation of growth hormone release and mRNA levels in an infant and adult rat model of impaired GHRH function

Hexarelin protects H9c2 cardiomyocytes from doxorubicin-induced cell death

Mechanism of action of hexarelin and GHRP-6: analysis of the involvement of GHRH and somatostatin in the rat

Kinetics and disposition of hexarelin, a peptidic growth hormone secretagogue, in rats

Hexarelin suppresses cardiac fibroblast proliferation and collagen synthesis in rat

Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway

Hexarelin Modulation of MAPK and PI3K/Akt Pathways in Neuro-2A Cells Inhibits Hydrogen Peroxide-Induced Apoptotic Toxicity

Looking to the future for erectile dysfunction therapies

In vitro models for metabolic studies of small peptide hormones in sport drug testing

Rapid desensitisation of the GH secretagogue (ghrelin) receptor to hexarelin in vitro

Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1

Hexarelin Protects Rodent Pancreatic Β-Cells Function from Cytotoxic Effects of Streptozotocin Involving Mitochondrial Signalling Pathways In Vivo and In Vitro

Metabolism of growth hormone releasing peptides

We are ageing

Growth hormone-releasing peptides

The Safety and Efficacy of Growth Hormone Secretagogues

Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases

Growth hormone and the heart

The CD36-PPARγ Pathway in Metabolic Disorders

Growth hormone in obesity

Growth hormone-releasing peptides and their analogs

Natural (ghrelin) and synthetic (hexarelin) GH secretagogues stimulate H9c2 cardiomyocyte cell proliferation

Hexarelin as a test of pituitary reserve in patients with pituitary disease

Alcohol-induced Cushing syndrome. Hypercortisolism caused by alcohol abuse

Interaction of the growth hormone releasing peptide hexarelin with somatostatin

Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway

Hexarelin attenuates abdominal aortic aneurysm formation by inhibiting SMC phenotype switch and inflammasome activation

Hexarelin protects cardiac H9C2 cells from angiotensin II-induced hypertrophy via the regulation of autophagy

Hexarelin stimulation of growth hormone release and mRNA levels in an infant and adult rat model of impaired GHRH function

Hexarelin protects H9c2 cardiomyocytes from doxorubicin-induced cell death

Mechanism of action of hexarelin and GHRP-6: analysis of the involvement of GHRH and somatostatin in the rat

Kinetics and disposition of hexarelin, a peptidic growth hormone secretagogue, in rats

Hexarelin suppresses cardiac fibroblast proliferation and collagen synthesis in rat

Hexarelin alleviates apoptosis on ischemic acute kidney injury via MDM2/p53 pathway

Hexarelin Modulation of MAPK and PI3K/Akt Pathways in Neuro-2A Cells Inhibits Hydrogen Peroxide-Induced Apoptotic Toxicity

Looking to the future for erectile dysfunction therapies

In vitro models for metabolic studies of small peptide hormones in sport drug testing

Rapid desensitisation of the GH secretagogue (ghrelin) receptor to hexarelin in vitro

Synthesis and pharmacological in vitro and in vivo evaluations of novel triazole derivatives as ligands of the ghrelin receptor. 1

Hexarelin Protects Rodent Pancreatic Β-Cells Function from Cytotoxic Effects of Streptozotocin Involving Mitochondrial Signalling Pathways In Vivo and In Vitro

Metabolism of growth hormone releasing peptides

Six-week treatment with hexarelin in young dogs: evaluation of the GH responsiveness to acute hexarelin or GHRH administration, and of the orexigenic effect of hexarelin

Hexarelin treatment in male ghrelin knockout mice after myocardial infarction

Beneficial effects of desacyl-ghrelin, hexarelin and EP-80317 in models of status epilepticus

Modulation of PTEN by hexarelin attenuates coronary artery ligation-induced heart failure in rats

Effect of ghrelin and synthetic growth hormone secretagogues in normal and ischemic rat heart

Growth hormone-independent cardioprotective effects of hexarelin in the rat

Growth hormone-releasing activity of hexarelin in humans. A dose-response study

Novel domain-selective ACE-inhibiting activity of synthetic growth hormone secretagogues