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Hexarelin

Examorelin, HEX

A synthetic hexapeptide growth hormone secretagogue that stimulates GH release by acting on the ghrelin receptor in the pituitary and hypothalamus.

Quick Stats
Studies 233
Trials 61
Formula C47H58N12O6
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Utility 3
pubmed 2010

Effects of hexarelin (a ghrelin analogue) on fertilisation and the pre- and postnatal development of mice.

Luque. E M EM; Carlini. V P VP; Vincenti. L M LM; Puechagut. P P; Stutz. G G; Santillán. M E ME...

Hexarelin, a drug that mimics the hunger hormone ghrelin, can lower the number of eggs released in female mice and, when given during pregnancy, speeds up baby mouse development but also harms memory later in life, especially in females. The same memory problems show up in adult mice given the drug continuously.

Utility 3
pubmed May 1, 2018

Hexarelin treatment preserves myocardial function and reduces cardiac fibrosis in a mouse model of acute myocardial infarction.

McDonald. Hayley H; Peart. Jason J; Kurniawan. Nyoman N; Galloway. Graham G; Royce. Simon S; Samuel....

In mice that had a heart attack, giving the synthetic peptide hexarelin for three weeks helped the heart pump better, reduced scar tissue, lowered inflammation, and shifted the nervous system toward a more relaxed (parasympathetic) state. These effects suggest hexarelin could aid heart healing, but the work was done in animals, not people.

Utility 3
pubmed Nov 30, 2009

Hexarelin suppresses high lipid diet and vitamin D3-induced atherosclerosis in the rat.

Pang. Jinjiang J; Xu. Qihua Q; Xu. Xiangbin X; Yin. Hongchao H; Xu. Rongkun R; Guo. Shu S; Hao. Wei...

In rats fed a high‑fat diet and vitamin D3, the peptide hexarelin (a growth‑hormone‑releasing peptide) reduced the buildup of atherosclerotic plaques, improved the good‑to‑bad cholesterol ratio, boosted nitric‑oxide production in blood vessels, and slowed the growth of vascular smooth‑muscle cells and foam‑cell formation.

Utility 3
pubmed Nov 30, 2006

A growth hormone-releasing peptide promotes mitochondrial biogenesis and a fat burning-like phenotype through scavenger receptor CD36 in white adipocytes.

Rodrigue-Way. Amélie A; Demers. Annie A; Ong. Huy H; Tremblay. André A

A study in mouse fat cells and mice shows that hexarelin, a growth‑hormone‑releasing peptide, can make white fat act more like brown fat – it burns more fat, builds more mitochondria, and turns on ‘heat‑making’ genes. This effect needs the CD36 receptor and was not seen in mice that lack CD36.

Utility 3
pubmed Jun 18, 2019

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

Agbo. Elvis E; Liu. Donhai D; Li. Meixiu M; Saahene. Roland Osei RO; Chen. Liqiang L; Zhao. Lunpeng...

In a rat study, giving the peptide hexarelin twice daily for a month helped hearts recover after a heart attack. It worked by boosting a protein called PTEN and turning down the Akt/mTOR pathway, which together reduced heart damage, oxidative stress, and improved heart pumping ability.

Utility 3
pubmed Jan 5, 2021

Effect of paracellular permeation enhancers on intestinal permeability of two peptide drugs, enalaprilat and hexarelin, in rats.

Dahlgren. David D; Olander. Tobias T; Sjöblom. Markus M; Hedeland. Mikael M; Lennernäs. Ha...

In rats, adding the gut‑opening agents chitosan or EDTA to the intestinal lumen made it easier for the peptide hexarelin (and a smaller peptide, enalaprilat) to cross into the bloodstream. This shows that certain “paracellular” enhancers can boost oral absorption of hydrophilic peptides, though the study was done in animals and didn’t test a real oral dosing protocol.

Utility 3
pubmed May 1, 2005

Central control of penile erection: role of the paraventricular nucleus of the hypothalamus.

Argiolas. Antonio A; Melis. Maria Rosaria MR

In rats, a brain area called the paraventricular nucleus (PVN) controls erections by using oxytocin‑producing neurons. These neurons can be turned on by things like dopamine, certain amino acids, oxytocin itself, or electrical stimulation, leading to an erection, while they are shut down by GABA, opioids, or similar drugs. The study found that peptide versions of hexarelin, a growth‑hormone‑releasing peptide, can also activate these PVN neurons and help produce erections, suggesting a possible new way to boost sexual function.

Utility 3
pubmed Sep 1, 2001

Hexarelin--evaluation of factors influencing oral bioavailability and ways to improve absorption.

Westberg. C C; Benkestock. K K; Fatouros. A A; Svensson. M M; Sjöström. B B

Hexarelin taken by mouth is barely absorbed (about 0.3% gets into the bloodstream) because gut enzymes quickly break it down, especially at a lysine spot. Adding certain protease blockers or substances that open up the gut lining can slow this breakdown and let a bit more get through, but overall absorption stays low.

Utility 3
pubmed Oct 10, 2005

Cardiac and peripheral actions of growth hormone and its releasing peptides: relevance for the treatment of cardiomyopathies.

Marleau. Sylvie S; Mulumba. Mukandila M; Lamontagne. Daniel D; Ong. Huy H

The paper reviews studies where growth‑hormone‑releasing peptides like hexarelin have been tested in animals and some heart‑failure patients. It suggests these peptides can improve heart muscle function and reduce damage in both ischemic (blocked‑artery) and non‑ischemic cardiomyopathies, but most evidence is still pre‑clinical or from small clinical trials.

Utility 3
pubmed Oct 1, 2017

Hexarelin, a Growth Hormone Secretagogue, Improves Lipid Metabolic Aberrations in Nonobese Insulin-Resistant Male MKR Mice.

Mosa. Rasha R; Huang. Lili L; Wu. Yeda Y; Fung. Chungyan C; Mallawakankanamalage. Oshini O; LeRoith....

In a mouse study, giving the peptide hexarelin twice a day for 12 days lowered blood sugar problems, cut down fat in the blood and liver, and changed body composition by reducing fat and increasing lean muscle, even though the mice ate more. These results hint that hexarelin could help with insulin resistance and unwanted fat, but the work was done in a specific mouse model, not people.

Utility 3
pubmed 2001

Recombinant human IGF-I does not modify the ACTH and cortisol responses to hCRH and hexarelin, a peptidyl GH secretagogue, in humans.

Gianotti. L L; Ramunni. J J; Lanfranco. F F; Maccagno. B B; Giordano. R R; Broglio. F F; Maccario. M...

Giving a dose of recombinant IGF‑I raises blood IGF‑I levels but doesn’t change the body's baseline stress hormones (ACTH and cortisol). Both CRH and the GH‑releasing peptide hexarelin normally spike ACTH and cortisol, and IGF‑I pretreatment doesn’t affect those spikes. However, IGF‑I does blunt the GH surge that hexarelin normally causes.

Utility 3
pubmed 2001

Permeability of the peptidic GH secretagogues hexarelin and EP 51389, across rat jejunum.

Roumi. M M; Kwong. E E; Deghenghi. R R; Locatelli. V V; Marleau. S S; Du Souich. P P; Béliveau....

The study shows that hexarelin and a similar peptide, EP 51389, barely get through the gut lining, so taking them by mouth won’t deliver much into the bloodstream. Hexarelin mostly slips through cells passively, while EP 51389 is pumped out and even blocks a gut protein (P‑gp) that normally pushes drugs out.

Utility 3
pubmed Sep 1, 2004

Identification of the growth hormone-releasing peptide binding site in CD36: a photoaffinity cross-linking study.

Demers. Annie A; McNicoll. Normand N; Febbraio. Maria M; Servant. Marc M; Marleau. Sylvie S; Silvers...

Researchers discovered that hexarelin, a peptide many biohackers use to boost growth hormone, also sticks to a protein called CD36 that helps cells take up bad cholesterol. By binding to the same spot that oxidized LDL uses, hexarelin might block this harmful uptake and could help protect against artery plaque, at least in mouse studies.

Utility 3
pubmed Jan 5, 1998

Peptide hormones: Review of current and emerging uses by nasal delivery.

Pontiroli. AE AE

This review says most peptide hormones can’t be taken as pills, but spraying them into the nose works well and is easy to use. Some hormones like desmopressin and oxytocin are already sold for nasal use, and hexarelin – a growth‑hormone‑releasing peptide – looks especially promising for this route, though it isn’t on the market yet.

Utility 3
pubmed 2001

Pharmacological profile of a new orally active growth hormone secretagogue, SM-130686.

Nagamine. J J; Nagata. R R; Seki. H H; Nomura-Akimaru. N N; Ueki. Y Y; Kumagai. K K; Taiji. M M; Nog...

SM-130686 is a new pill‑type compound that tricks the body’s ghrelin receptor into releasing growth hormone. In rats, a single dose raised GH levels for up to an hour, and giving the drug twice daily for nine days boosted lean body mass and IGF‑1, similar to giving growth hormone itself.

Utility 3
pubmed 1999

Hexarelin, a growth hormone - releasing peptide, counteracts bone loss in gonadectomized male rats.

Sibilia. V V; Cocchi. D D; Pagani. F F; Lattuada. N N; Moro. G L GL; Pecile. A A; Rubinacci. A A; Mu...

In a rat study, the peptide hexarelin (a strong growth‑hormone releaser) was given twice daily for a month. In normal rats it lowered markers of bone breakdown but didn’t change bone density. In rats that had their testes removed (a model of low testosterone and bone loss), hexarelin stopped the rise in bone‑resorption markers, kept bone‑formation activity up, and prevented the loss of bone density in the spine and thigh bone.

Utility 3
pubmed 2001

Growth hormone and the heart.

Colao. A A; Marzullo. P P; Di Somma. C C; Lombardi. G G

Growth hormone (GH) can both help and hurt the heart. Too much GH, as seen in acromegaly, can cause thickened heart walls and scar tissue, while not enough GH can make the heart walls thin and stiff, leading to poor pumping. Replacing GH in deficient people or carefully lowering it in excess can improve heart structure and function, and early studies even suggest GH might help people with chronic heart failure, though more research is needed.

Utility 3
pubmed 2001

Ghrelin, a natural GH secretagogue produced by the stomach, induces hyperglycemia and reduces insulin secretion in humans.

Broglio. F F; Arvat. E E; Benso. A A; Gottero. C C; Muccioli. G G; Papotti. M M; van der Lely. A J A...

In a small study of healthy young adults, giving the natural hormone ghrelin caused a big jump in growth hormone, raised blood sugar, and lowered insulin. The synthetic GH secretagogue hexarelin also boosted growth hormone but did NOT change blood sugar or insulin levels. This suggests hexarelin can raise GH without the immediate metabolic side‑effects seen with ghrelin.