Description
Hexarelin for sale
Hexarelin has shown potential to help with joint restoration, protection, and healing, neural protection, muscle fiber size increase, and enhanced strength when administered on lab subjects.
The peptide is also thought to decrease overall fatty tissue, which helps the subjects lose fat. Any form of growth, however, is solely a result of the rise in hormone levels; gastric draining isn’t accelerated, and appetite is not stimulated.
Hexarelin – Potent Synthetic GH Analog
Growth hormones, or GH, is a vital hormone released by the pituitary gland of both men and women. Growth hormones are important because they are critical to healthy metabolism, lean mass build up, cell regeneration, skin thickness, and overall well being of the humans.
A decline in the level of growth hormones can adversely impact human health. This reduction in hormone level is not uncommon, especially in adults and aged people, and also when people suffer from inherent growth hormone deficiency.
So, how do we beat this commonly occurring phenomenon of growth hormone reduction?
There are medications to beat this, but there are some serious adverse effects caused by them and are not readily bioavailable. The other alternative is peptides. The main advantage of peptides is they are similar to natural hormones and are highly stable, readily bioavailable, and cause minimal side effects.
What is Hexarelin?
Hexarelin is a growth hormone releasing peptide (GHRP) that is highly similar to the other efficient peptide GHRP-6 (1).
Hexarelin, also called Examorelin, is a six amino acid containing synthetic peptide (2).
Hexarelin Discovery
Ghrelin is a natural, 28 amino acid containing peptide that possesses growth hormone releasing activity. Several synthetic compounds similar to ghrelin activity, including Hexarelin, were invented more than 25 years ago (3).
Since then, synthetic studies and research have continued to date to fully examine peptide effects in the therapeutic field.
Working Mechanism of Hexarelin
GH Releasing Effects
A study (4) was conducted on infant and adult rats to understand the mechanism of Hexarelin.
In this study, pups aged 10 days old were passively immunized against the natural growth hormone releasing hormone (GHRH) from birth. These pups were then treated with 80 microg/kg Hexarelin twice a day for 3 to 10 days. This administration led to significant increase in growth hormone levels in the subject plasma.
Furthermore, adult male rats were surgically treated to remove the anterior pituitary tissue (i.e., mediobasal hypothalamus removal.)
These rats were treated with 150 microg/kg Hexarelin twice a day 5 days prior to the surgery. This administration showed no significant changes in the concentrations of growth hormone. Interestingly, when these operated rats were treated with GHRH, it induced high levels of growth hormones within 7 days after the treatment. After 30 days, both Hexarelin and GHRH induced similar rises in the hormone plasma levels.
Based on this study, it was understood that Hexarelin works via three different mechanisms:
(a) directly acts on the pituitary gland,
(b) indirectly works via stimulating GHRH release, and
(c) releases an ‘unknown’ hypothalamic factor that leads to GH release in the plasma.
ACTH Releasing Effects
Analogous to other GHRPs, it is known that Hexarelin stimulates the release of prolactin and adrenocorticotropin (ACTH) hormones.
To understand the mechanism of Hexarelin, a study (5) was conducted on 7 young, healthy subjects who were either administered with Hexarelin (2 microg/kg body weight, intravenously), human corticotropin releasing hormone hCRH (2 microg/kg body weight, intravenously) and arginine (0.17 microg/kg body weight, intramuscularly). All these compounds were either given solo or in combination.
Upon analysis, it was indicated that all three compounds individually led to increased levels of ACTH hormones, with all three showing similar effects. When given in combination, hCRH and arginine showed synergistic effects, however, co-administration with Hexarelin showed no changes in ACTH release.
These results suggest that Hexarelin elicits its actions by acting on the pituitary to adrenal axis in humans and do not depend on both hCRH and arginine mediated effects in humans.
Benefits and Positive Effects
Several health benefits of Hexarelin include:
- Elevated growth hormone release
- Increased lean muscle mass
- Increased metabolism and fat reduction
- Improved recovery rate of injuries
- Improved bone density and muscle strength
- Potential effects on insulin growth factor (IGF-1)
- Elevated levels of ACTH hormones
Research and Clinical studies
Growth Hormone Release
This study (6) was conducted on 12 children (6 of pubertal age, 6 of prepubertal age), 12 young adults (22 to 30 years), and 12 elderly volunteers (53 to 79 years) to evaluate the GH releasing effects of the peptide.
All volunteers were either administered with highest effective dose of Hexarelin, i.e., 2 microg/kg body weight, and with GHRH alone (1 microg/kg) and in combination with arginine (500 microg/kg), all via an intravenous route.
In prepubertal children, the GH levels were significantly elevated by GHRH + arginine combination, while GH levels were not highly raised by Hexarelin alone. On the other hand, Hexarelin induced GH levels were much higher than the increased GH levels induced by GHRH alone and GHRH + arginine combination in pubertal and adult volunteers. In elderly volunteers, Hexarelin induces higher GH levels in comparison to GHRH, however, the GH levels are lower than GHRH + arginine combination.
These results suggest that Hexarelin causes elevated GH levels in pubertal children and adults. While it does increase GH levels in elderly and prepubertal children, it is not up to a significant effect.
Effects on GH1 Cell Lines
The main aim of this in vitro study (7) was to determine the effects of Hexarelin on GH1 rat tumor cell line, which is insensitive towards GHRH. Furthermore, this study also monitored the involvement of GHRH in the effects of Hexarelin in the GH1 rat cells.
Hexarelin was administered in both normal, healthy rat cells and GH1 rat cells at a dose of 0.01 to 1 microM. The most effectual dose was 1 microM which significantly increased the GH levels in both rat cell cultures.
While GHRH increased GH levels in normal rat cells, it showed no effects on GH1 cells. What’s more, when administered with Hexarelin, GHRH caused no impact on the GH release.
These results suggest that GHRPs and GHRHs act on two distinct sites and GHRPs, such as Hexarelin, have the potential to act on cells that are not sensitive to GHRH effects.
Cardiovascular Effects of Hexarelin
Studies (8) have shown that the acute administration of Hexarelin causes positive inotropic effects in the cardiovascular system.
When administered intravenously in seven male volunteers, the peptide increased LVEF ejection rate without affecting blood pressure. This effect lasted up to 60 minutes after administration. When administered in 24 male patients with coronary artery disease undergoing surgery while under anesthesia, the intravenous administration of 2 microg/kg dose of Hexarelin led to increased cardiac output, increased arterial pressure with no change in heart rate.
Furthermore, when administered in ischemic rat hearts, Hexarelin restored the electrophysiological properties of the heart cells and inhibited cell apoptosis, thereby producing positive inotropic effects and promoting heart cell survival (9).
Another study (10) was conducted where 100 microg/kg Hexarelin was administered daily in male rat hearts that were experimentally induced to undergo myocardial infarction. The results demonstrated that the peptide treatment led to increased stroke volume and increased cardiac output, while decreasing peripheral resistance.
Effects on Body Composition
The main aim of this study (11) was to determine the effects of body composition and gender on the growth hormone releasing effects of Hexarelin.
This study was conducted on 28 healthy volunteers (both male and female) aged between 60 to 81 years. All volunteers were administered with 1.5 microg/kg body weight Hexarelin via subcutaneous route.
Upon analyzing the blood samples, it was determined that the peak growth hormone release is negatively correlated to fat mass. Increased fat mass leads to reduction in GH release. However, gender had no significant effect on GH release.
These results suggest that Hexarelin has the potential to be used as a diagnostic and therapeutic agent to monitor human disorders.
Hexarelin Peptide Dose Studies
Effects of Repeated Administration and Coadministration with GHRH
The main aim of this study (12) was to determine the effects of repeated Hexarelin administration in humans, and its effect when co-administered with GHRH.
This study was conducted on six healthy male adults who were administered with either saline (control group), Hexarelin (1 microg/kg), GHRH (1 microg/kg) or combination of both Hexarelin and GHRH. All doses were given in two repetitive intravenous boluses with 60- or 120-minute intervals between the two administrations.
The results of the study indicated that Hexarelin showed potent GH releasing effects on both administrations, where the concentration of GH increased after the second administration. Co-administration of GHRH and Hexarelin showed positive synergistic effects, which was lost in the repeated administration.
These results indicate that GHRPs (Hexarelin) are highly efficacious in releasing growth hormones and can be potentially used as therapeutic agents in humans.
Dose Response Study
The main aim of this study (13) was to determine the effects of increased doses of Hexarelin in humans.
12 adult male subjects were administered with intravenous doses of Hexarelin in a rising dose fashion of 0.5, 1 and 2 microg/kg, with the control being randomly added to the sequence.
Based on the study results, it was noted that Hexarelin effects were dose dependent as the efficacy increased with every rise in the dose. The effects of the peptide were maximal at about 30 minutes, and then decreased to baseline values within 4 hours, with a half-life of about 55 to 60 minutes.
These results show that the peptide produces significant and dose-dependent effects of growth hormone plasma levels.
Side Effects or Negative Effects
The common side effects of Hexarelin are common to those of other GHRPs, which include:
- Pain, inflammation and redness at the site of administration
- Lethargy, fatigue
- Elevated sleep levels
- Edema
- Flushes, headache
- Nausea
It should be noted that Hexarelin causes increased levels of ACTH and cortisol hormones, which is a positive effect, however, it may intervene with certain medications and may cause adverse effects.
Summary
Hexarelin is a potent, synthetic growth hormone releasing peptide composed of six amino acids and is similar to the other well known peptide, namely GHRP-6.
While the working mechanism of Hexarelin is still unclear, there are various theories to support that the peptide acts directly on the pituitary gland and binds with the growth hormone releasing receptors, which thereby leads to growth hormone release. Beyond this, studies have also suggested that there is also an ‘unknown’ hypothalamic factor which stimulates Hexarelin induced GH release in the plasma.
Hexarelin has various health benefits besides treating growth hormone deficiency. These include increased cortisol hormone release, increased metabolism and lean body mass, and efficient cardiovascular effects.
Similar to other growth hormone analogs and GH releasing peptides, Hexarelin is banned from sports by the World Anti-Doping Agency (WADA)(14). This is because athletes often misuse this peptide for its added advantage of increased energy levels.
References:
1. Giustina A, Bonfanti C, Licini M, Ragni G, Stefana B. Hexarelin, a novel GHRP-6 analog, stimulates growth hormone (GH) release in a GH-secreting rat cell line (GH1) insensitive to GH-releasing hormone. Regul Pept. 1997 May 14;70(1):49-54. https://pubmed.ncbi.nlm.nih.gov/9250581/
2. National Center for Biotechnology Information (2021). PubChem Compound Summary for CID 6918297, Examorelin. Retrieved August 19, 2021 from https://pubchem.ncbi.nlm.nih.gov/compound/Examorelin
3. Fabio Broglio et al, Ghrelin: Much more than a natural growth hormone secretagogue. Division of Endocrinology and Metabolism, Department of Internal Medicine; Division of Pathological Anatomy, Department of Biomedical Sciences and Oncology https://www.ima.org.il/FilesUploadPublic/IMAJ/0/56/28152.pdf
4. Torsello A, Grilli R, Luoni M, Guidi M, Ghigo MC, Wehrenberg WB, Deghenghi R, Müller EE, Locatelli V. Mechanism of action of Hexarelin. I. Growth hormone-releasing activity in the rat. Eur J Endocrinol. 1996 Oct;135(4):481-8. https://pubmed.ncbi.nlm.nih.gov/8921832/
5. Arvat E, Maccagno B, Ramunni J, Di Vito L, Broglio F, Deghenghi R, Camanni F, Ghigo E. Hexarelin, a synthetic growth-hormone releasing peptide, shows no interaction with corticotropin-releasing hormone and vasopressin on adrenocorticotropin and cortisol secretion in humans. Neuroendocrinology. 1997 Dec;66(6):432-8. https://pubmed.ncbi.nlm.nih.gov/9430449/
6. Bellone J, Bartolotta E, Sgattoni C, Aimaretti G, Arvat E, Bellone S, Deghenghi R, Ghigo E. 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. J Endocrinol Invest. 1998 Sep;21(8):494-500. https://pubmed.ncbi.nlm.nih.gov/9801989/
7. Giustina A, Bonfanti C, Licini M, Ragni G, Stefana B. Hexarelin, a novel GHRP-6 analog, stimulates growth hormone (GH) release in a GH-secreting rat cell line (GH1) insensitive to GH-releasing hormone. Regul Pept. 1997 May 14;70(1):49-54. https://pubmed.ncbi.nlm.nih.gov/9250581/
8. Mao, Yuanjie et al. “The cardiovascular action of hexarelin.” Journal of geriatric cardiology : JGC vol. 11,3 (2014): 253-8. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4178518/
9. Ma Y, Zhang L, Edwards JN, Launikonis BS, Chen C. Growth hormone secretagogues protect mouse cardiomyocytes from in vitro ischemia/reperfusion injury through regulation of intracellular calcium. PLoS One. 2012;7(4):e35265. https://pubmed.ncbi.nlm.nih.gov/22493744/
10. Tivesten A, Bollano E, Caidahl K, Kujacic V, Sun XY, Hedner T, Hjalmarson A, Bengtsson BA, Isgaard J. The growth hormone secretagogue hexarelin improves cardiac function in rats after experimental myocardial infarction. Endocrinology. 2000 Jan;141(1):60-6. https://pubmed.ncbi.nlm.nih.gov/10614623/
11. Rahim A, O’Neill P, Shalet SM. The effect of body composition on hexarelin-induced growth hormone release in normal elderly subjects. Clin Endocrinol (Oxf). 1998 Nov;49(5):659-64. https://pubmed.ncbi.nlm.nih.gov/10197083/
12. Massoud AF, Hindmarsh PC, Matthews DR, Brook CG. The effect of repeated administration of hexarelin, a growth hormone releasing peptide, and growth hormone releasing hormone on growth hormone responsivity. Clin Endocrinol (Oxf). 1996 May;44(5):555-62. https://pubmed.ncbi.nlm.nih.gov/8762732/
13. Imbimbo, B.P., Mant, T., Edwards, M. et al. Growth hormone-releasing activity of hexarelin in humans. Eur J Clin Pharmacol 46, 421–425 (1994). https://doi.org/10.1007/BF00191904
14. 2021 WADA Prohibited list. https://www.wada-ama.org/en/content/what-is-prohibited/prohibited-at-all-times/peptide-hormones-growth-factors-related-substances-and-mimetics
Hexarelin Benefits Research
In various research studies, Hexarelin peptide has been found to help with injury prevention and recovery, fat loss, muscle building, and skin elasticity.
Get more research details by reading our latest Hexarelin Review – Benefits, Side Effects 2021 blog post.
Synonyms/Aliases: Hexarelin, Examorelin
NOTE: These products are intended for laboratory research use only. Hexarelin for sale is not for personal use. Please review and adhere to our Terms and Conditions before ordering.
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