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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 2
pubmed Sep 7, 2006

A growth hormone-releasing peptide that binds scavenger receptor CD36 and ghrelin receptor up-regulates sterol transporters and cholesterol efflux in macrophages through a peroxisome proliferator-activated receptor gamma-dependent pathway.

Avallone. Roberta R; Demers. Annie A; Rodrigue-Way. Amélie A; Bujold. Kim K; Harb. Diala D; Ang...

Hexarelin, a peptide that makes the body release growth hormone, was shown in lab cells and mice to boost the removal of cholesterol from immune cells and shrink artery plaque, working through a protein called PPAR‑gamma. However, the work is still early‑stage and only in animals, so there’s no clear dosing or safety guide for people yet.

Utility 2
pubmed Nov 27, 2021

Hexarelin modulates lung mechanics, inflammation, and fibrosis in acute lung injury.

Zambelli. Vanessa V; Rizzi. Laura L; Delvecchio. Paolo P; Bresciani. Elena E; Rezoagli. Emanuele E;...

In a mouse study, giving the peptide hexarelin around the time of a chemically‑induced lung injury helped the lungs stay more flexible, cut down the early flood of immune cells (especially neutrophils), and later reduced scar tissue formation. The effect was seen whether the peptide was given before or after the injury.

Utility 2
pubmed Apr 19, 2016

Enhanced responsiveness of Ghsr Q343X rats to ghrelin results in enhanced adiposity without increased appetite.

Chebani. Yacine Y; Marion. Candice C; Zizzari. Philippe P; Chettab. Khadidja K; Pastor. Marie M; Kor...

A rat model with a specific GHSR mutation reacts more strongly to ghrelin, leading to extra weight and fat even though they don’t eat more, and they handle glucose worse. This shows that boosting ghrelin signaling can increase fat storage independent of appetite.

Utility 2
pubmed Jan 9, 2013

FAT/CD36 regulates PEPCK expression in adipose tissue.

Wan. Zhongxiao Z; Matravadia. Sarthak S; Holloway. Graham P GP; Wright. David C DC

The study shows that a protein called CD36 helps control a fat‑processing enzyme (PEPCK) in mouse fat cells. When CD36 is missing, both fat breakdown and the enzyme’s levels drop. Adding hexarelin, a synthetic peptide that activates CD36, boosts the enzyme’s gene activity even without changing fat breakdown.

Utility 2
pubmed Sep 1, 2009

Desacyl-ghrelin and synthetic GH-secretagogues modulate the production of inflammatory cytokines in mouse microglia cells stimulated by beta-amyloid fibrils.

Bulgarelli. Ilaria I; Tamiazzo. Laura L; Bresciani. Elena E; Rapetti. Daniela D; Caporali. Simona S;...

In a mouse brain cell model, the amyloid protein that builds up in Alzheimer's triggers inflammation. The synthetic peptide hexarelin (along with related compounds) was able to block this inflammatory response, likely by interfering with a receptor called CD36. Regular ghrelin didn't work, and the usual ghrelin receptor wasn't involved.

Utility 2
pubmed Dec 1, 2003

Activation of GABAA and opioid receptors reduce penile erection induced by hexarelin peptides.

Succu. Salvatora S; Mascia. Maria Stefania MS; Melis. Tiziana T; Melis. Maria Rosaria MR; Deghenghi....

In rats, a hexarelin‑like peptide called EP 80661 makes male rats get erections by raising nitric‑oxide levels in a brain area that controls sexual function. Turning on GABA‑A receptors with muscimol or opioid receptors with morphine blocks both the erection and the nitric‑oxide rise, and these blocks can be undone with specific antagonists. The findings show that GABA and opioid pathways can counteract hexarelin‑induced sexual effects, at least in rats.

Utility 2
pubmed Jul 19, 2002

Effects of acute hexarelin administration on cardiac performance in patients with coronary artery disease during by-pass surgery.

Broglio. Fabio F; Guarracino. Fabio F; Benso. Andrea A; Gottero. Cristina C; Prodam. Flavia F; Grana...

Giving a single IV dose of the peptide hexarelin (2 µg per kg) to men undergoing heart bypass surgery quickly boosted how well their hearts pumped blood, without changing the size of the heart chambers or overall blood vessel resistance. This effect was not seen with other growth‑hormone drugs and seemed to happen independently of any rise in growth‑hormone levels.

Utility 2
pubmed 2002

GH-independent cardiotropic activities of hexarelin in patients with severe left ventricular dysfunction due to dilated and ischemic cardiomyopathy.

Imazio. M M; Bobbio. M M; Broglio. F F; Benso. A A; Podio. V V; Valetto. M R MR; Bisi. G G; Ghigo. E...

A short IV dose of the peptide hexarelin raises growth hormone levels in people with severe heart failure, and it can temporarily improve heart pumping ability in those whose heart disease is caused by blocked arteries, but it doesn’t help those with a dilated heart. The heart boost seems to come from a direct effect on the heart muscle, not just the hormone rise.

Utility 2
pubmed 2000

Hexarelin, a growth hormone secretagogue, protects the isolated rat heart from ventricular dysfunction produced by exposure to calcium-free medium.

Rossoni. G G; Locatelli. V V; Müller. E E EE; Berti. F F

In rats, giving the peptide hexarelin under the skin for a week helped protect heart tissue from damage caused by a sudden return of calcium, but a single dose directly into the heart did not work. This protection didn't come from higher growth hormone or IGF‑1 levels, and the exact way it works is still unclear.

Utility 2
pubmed Jun 22, 2014

We are ageing.

Kolovou. Genovefa D GD; Kolovou. Vana V; Mavrogeni. Sophie S

The paper is a broad review of why we age, covering things like oxidative stress, metabolism, inflammation, DNA repair, and growth hormone pathways. It says the most promising ways to extend life right now are things like eating less, targeting the TOR pathway, activating sirtuins, using the peptide hexarelin, and applying hormetic stress. It doesn’t give any specific dosing or protocols for hexarelin, just lists it as a potential anti‑ageing tool.

Utility 2
pubmed 2000

Endocrine, metabolic and cardioprotective effects of hexarelin in obese Zucker rats.

De Gennaro-Colonna. V V; Rossoni. G G; Cocchi. D D; Rigamonti. A E AE; Berti. F F; Muller. E E EE

In a study on obese Zucker rats, giving the peptide hexarelin for a month did not improve growth‑hormone levels, actually raised blood sugar and insulin, but it did lower cholesterol and protected the heart from damage caused by lack of blood flow. The heart‑protective effect seemed unrelated to growth‑hormone activity.

Utility 2
pubmed Dec 8, 2000

The influence of sex and gonadectomy on the growth hormone and corticosterone response to hexarelin in the rat.

Sibilia. V V; Cocchi. D D; Pagani. F F; Pecile. A A; Netti. C C

In rats, the GH‑boosting peptide hexarelin triggers a much bigger growth‑hormone surge in males than in females, and this gender gap stays even when the animals’ sex hormones are removed. It also raises stress‑hormone (corticosterone) levels, but the timing and size of that rise differ between sexes – men‑like rats get a quick boost, while women‑like rats see a delayed, smaller increase.

Utility 2
pubmed Sep 21, 2001

Role of endothelial cells in modulation of contractility induced by hexarelin in rat ventricle.

Bedendi. I I; Gallo. M P MP; Malan. D D; Levi. R C RC; Alloatti. G G

In a lab study on rat heart muscle, the GH‑secretagogue hexarelin helped the tissue bounce back faster after a short loss of oxygen and briefly boosted its squeezing force. The boost was linked to the heart’s inner lining (endothelium) releasing a molecule called prostacyclin, not to direct changes in calcium inside heart cells.

Utility 2
pubmed 2000

Differences of hexarelin-induced prolactin and cortisol responses between prepubertal and early pubertal short children and lack of correlation with gonadotropin-releasing hormone-induced gonadotropin response.

Guzzaloni. G G; Grugni. G G; Morabito. F F

Hexarelin, a synthetic peptide that strongly boosts growth hormone (GH), was tested in 19 short children—12 pre‑pubertal and 7 early‑pubertal. It raised GH similarly in both groups, caused only a small increase in prolactin, and did not change cortisol levels. These hormone responses were unrelated to the kids' sex‑steroid levels or to how their gonadotropins reacted to GnRH.

Utility 2
pubmed 2000

The effects of a continuous infusion of hexarelin on pulsatile growth hormone release, growth axis and galanin gene expression and on the response of the growth axis to growth hormone-releasing hormone.

Conley. L K LK; Brogan. R S RS; Giustina. A A; Wehrenberg. W B WB

In rats, a 6‑hour steady drip of the peptide hexarelin (about 100 µg per hour) caused a quick spike in growth hormone that fell back to normal within an hour, and it didn’t change the normal pattern of GH pulses. However, after the infusion the animals responded much more strongly to a separate growth‑hormone‑releasing hormone (GHRH) challenge, and the brain’s levels of certain hormones that control GH (galanin went up, GHRH went down) were altered. This suggests hexarelin can make the GH system more sensitive to GHRH without directly raising baseline GH levels.

Utility 2
pubmed 1998

Hexarelin, a synthetic GH-releasing peptide, is a powerful stimulus of GH secretion in pubertal children and in adults but not in prepubertal children and in elderly subjects.

Bellone. J J; Bartolotta. E E; Sgattoni. C C; Aimaretti. G G; Arvat. E E; Bellone. S S; Deghenghi. R...

Hexarelin is a synthetic peptide that can trigger a strong release of growth hormone (GH) when given by IV injection, especially in teenagers and young adults. It works less well in kids before puberty and in older adults, where the GH boost is modest.

Utility 2
pubmed 2004

Basal and stimulated levels of growth hormone, insulin-like growth factor-I (IGF-I), IGF-I binding and IGF-binding proteins in beta-thalassemia major.

Karydis. Ioannis I; Karagiorga-Lagana. Markisia M; Nounopoulos. Charalambos C; Tolis. George G

In kids with beta‑thalassemia, giving the peptide hexarelin caused a big jump in growth‑hormone (GH) levels, especially in those who were short. However, their IGF‑I (the hormone that actually drives growth) was only low‑normal and the way IGF‑I attached to cells was weaker, suggesting the growth problem is more about IGF‑I action than GH production.

Utility 2
pubmed Aug 22, 2003

Cardiac effects of ghrelin and its endogenous derivatives des-octanoyl ghrelin and des-Gln14-ghrelin.

Bedendi. Ivano I; Alloatti. Giuseppe G; Marcantoni. Andrea A; Malan. Daniela D; Catapano. Filomena F...

The study shows that hexarelin and natural ghrelin variants all make heart muscle contract a bit weaker at low heart rates, and this effect isn’t because they boost growth hormone but because they trigger a signal from the blood‑vessel lining that releases prostacyclin‑like molecules. Des‑octanoyl ghrelin was the strongest, while hexarelin was the weakest, and the effect disappears if the vessel lining is removed or its cyclo‑oxygenase enzyme is blocked.

Utility 2
pubmed Feb 1, 1997

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

Torsello. A A; Luoni. M M; Grilli. R R; Guidi. M M; Wehrenberg. W B WB; Deghenghi. R R; Müller....

Hexarelin, a GH-releasing peptide, is an effective GH secretagogue in man and a variety of experimental animals. In the present study, we sought to characterize the effects of short-term Hexarelin treatment on GH release and GH mRNA levels in infant and young-adult rats and in rats of either age passively immunized with an antiserum against GHRH (GHRH-Ab). Hexarelin (80 micrograms/kg, b.i.d. s.c.), administered for 3, 5 or 10 days to 8-, 6- and 1-day-old rats, respectively, induced a progressive enhancement of the plasma GH rise elicited by a subsequent acute Hexarelin (80 micrograms/kg s.c) challenge when pups were 10 days old. As expected, GHRH-Ab treatment decreased GH concentrations in 10-day-old pups. In GHRH-Ab-treated pups, Hexarelin administration for 3-10 days significantly enhanced the GH response to the acute Hexarelin injection, though the mean plasma GH values remained significantly lower than in the respective control group. Hexarelin treatment did not alter GH mRNA levels in control pups. In GHRH-Ab-treated pups Hexarelin treatment for 3 and 5 days, but not 10 days, restored GH mRNA levels to control values. In young-adult male rats, regardless of antiserum treatment, Hexarelin administration for 5 or 10 days significantly suppressed the GH response to a subsequent acute challenge with the peptide. Yet, 5-10 days of Hexarelin treatment did not alter GH mRNA in control young-adult rats. In adult rats GHRH-Ab also decreased GH mRNA levels, but 10 days of Hexarelin treatment were necessary to return GH mRNA back to normal levels. These results indicate that: (1) the effects of Hexarelin on GH release and GH mRNA levels may be unrelated events; (2) deprivation of GHRH function discloses the ability of Hexarelin to stimulate GH mRNA levels; (3) age plays a crucial role in setting the pituitary responsiveness to short-term Hexarelin treatment, and (4) the different ability of Hexarelin to stimulate GH release and GH synthesis in neonatal and young-adult rats may have clinical relevance in the chronic administration of the peptide.