What you need to know about Ipamorelin
Ipamorelin peptide activates the ghrelin receptor upon binding to it. The ghrelin receptor is a growth hormone secretagogue (GHS-R) and plays a crucial role in the regulation of energy and body weight.
The GHS-R is found primarily and more abundantly in the brain, but can also show up in heart muscles, skeleton, and liver.
Research studying how Ipamorelin affects synaptic density, bone density, or muscle size may need months to show results.
Though it is better known as an anti-aging peptide, Ipamorelin is also beginning to be known as a fat-burning or lipogenic peptide. Rodent studies present that Ipamorelin speeds up the process of lipolysis, the organized deterioration of fat.
Peptides have lately been in the news and have created an extreme buzz as they continue to provide many health benefits. Whether you are looking for the means to fight obesity or aging, or simply a tool to boost your energy levels and metabolic rate – peptides are the way to go.
Aging is a natural and gradual process where normal human bodily functions begin to decline. Ipamorelin peptide helps to fight aging and maintain bodily functions by boosting one’s energy levels and maintaining and building lean muscles.
It is a known fact that naturally occurring growth hormones help boost body growth with increased energy levels and full body development. However, after the age of 30 years, human growth hormone levels begin to decline by an average of 14% per decade (1). This is where the Ipamorelin (IPA) peptide comes into play helping maintain the required bodily levels of growth hormones and energy.
What is Ipamorelin peptide?
Ipamorelin peptide is a potent, highly efficient synthetic peptide, which has definite and specific properties similar to human growth hormones (HGH).
[Image reference: Ipamorelin (nih.gov)]
Ipamorelin is a peptide made up of five amino acids (hence, called pentapeptide) and is formally known as a ‘growth hormone secretagogue’. This means that the peptide is not the growth hormone itself, however, it stimulates the development of the natural growth hormones in the body. The mechanism by which the peptide works is described later in the article.
What is the history of Ipamorelin?
Originally, Ipamorelin peptide was being studied for the treatment of postoperative ileus, which had become a significant challenge. However, post the clinical studies, upon analysis it was noted that no significant changes were observed between the patients treated with the peptide and those treated with placebo (2).
Later, these peptides were then used by athletes as a performance enhancing medication.
After conducting several research studies and chemistry programs, Ipamorelin was identified as a pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) which would trigger the pituitary gland and stimulate the release of growth hormones in the human body (3). Research studies are described in detail later in this article.
What makes Ipamorelin work?
Ipamorelin is the first synthetic growth hormone secretagogue which augments the production of natural growth hormone. It triggers the small part of the pituitary gland to secrete more growth hormones naturally and thereby maintain their level in the human body (3).
This peptide has a high selectivity for the growth receptors in the gland, and similar to the growth hormone receptor peptide (GHRP) receptor agonists, it binds to the GHRP receptors and secrete more human growth hormones (3).
What are the advantages of Ipamorelin?
- Controls aging
- Decreases body fat and increases lean muscle mass
- Improves sleep cycle
- Increased collagen production
- Increased bone intensity
Reduction in growth hormone levels is natural with age, however, growth hormone deficiency can also be a health-related problem, especially for patients suffering from pituitary adenoma (benign tumor in the pituitary gland), and AIDS or HIV related deficiency. Medical practitioners recommend HGH (human growth hormone) therapy which also includes administration of the Ipamorelin peptides.
Based on multiple research studies, it was discovered that unlike other HGH stimulating hormones, Ipamorelin does not increase the cortisol and Adrenocorticotropic (ACH) hormone levels significantly in the blood plasma. As a result, Ipamorelin turns out to be the first GHRP-receptor agonist with a high selectivity for growth hormone release without affecting the ACH and cortisol levels – making it a one-of-a-kind growth hormone stimulating peptide.
Research and Clinical Studies
In vivo and In vitro research studies
Based on the 1998 research study, Ipamorelin, when administered to the rats, released growth hormones from the pituitary cells with significant potency and efficacy. When Ipamorelin was administered to swine and pentobarbitone anaesthetized rats, it demonstrated to be equally potent in releasing the growth hormones.
Upon studying, it was discovered that, similar to other growth hormone (GH) stimulating peptides, Ipamorelin was a growth receptor agonist that stimulates GH release by showing high affinity towards the growth hormone receptors (3).
Animal studies related to the subcutaneous administration of Ipamorelin
In 1999, additional research study was carried out in adult female rats where Ipamorelin was administered three times daily via subcutaneous route of administration in multiple doses of 0, 18, 90 and 450 microgram per day. Post treatment for 15 days, it was discovered that not only were the growth hormone levels elevated, but the longitudinal bone growth rate (LGR) was also increased from 42 micro meter per day to up to 52 micrometer per day. Also, there was a dose dependent gain on the body weight. This was a positive discovery which opened the possibilities of potential use of the peptide for children suffering from growth retardation (4).
Clinical studies on healthy individuals
In late 1999, a clinical trial was carried out on 8 healthy male volunteers where Ipamorelin was administered with dose escalation design of 4, 14, 42, 84 and 140 nmol/kg over every 15 minutes. After 2 hours post treatment, it was concluded that the levels of growth hormones had exponentially increased with the highest peak recorded within a single episode of the peptide (5).
Clinical studies on growth hormone deficient adult patients
Since 2001, there have been multiple clinical studies being conducted on individuals with growth hormone deficiency. Growth hormone releasing peptides had demonstrated their efficacy through two ways – (i) via stimulating the pituitary gland to release growth hormones and (ii) via acting on the arcuate nucleus of the hypothalamus. While these peptides, including Ipamorelin, demonstrated high releases of growth hormones, it remains unclear which of the two mechanisms worked in vivo.
Additionally, it has been proven that these peptides modulate food intake, cardiac tone, and sleep through specific receptor agonistic effects (6).
Clinical studies on growth hormone deficient children
Six children with growth hormone deficiency and growth failure were administered with graded doses of 0.3 to 3 micrograms per kg per day for a period of eight months. Throughout this study, the children were monitored every 12 hours for episodic growth hormone secretion and toxicity levels. After two months of the graded dose treatment, it was noticed that the children showed a great spike in the growth hormone levels during the treatment and for a short period of time after the treatment, with little effect on the GH levels at the later stages. No toxicities and side effects were noticed.
While the studies proved to be phenomenally successful, more studies were to be conducted to modulate the dosage forms and/or routes of administration to prolongate the medicated effects (7).
What are the Side Effects?
Based on the research and clinical trials conducted, it has been proven that the peptide is usually highly tolerated and does not show any side effects.
However, there could be few potential side effects depending on the dosage form and individual body profile, such as (2):
- Redness, itchiness, swelling or irritation at the injection site
- Elevated appetite
- Dry mouth
- Increased weight
How is Ipamorelin administered?
Ipamorelin is generally available in subcutaneous injectables format and is generally meant to be applied in the stomach or abdominal area. While this has proven to show desirable results, it is recommended to consult a medical practitioner prior to use to help determine the best dose as per individual patient profile.
What is the recommended dosage of Ipamorelin?
Based on the scientific studies and clinical trials, the optimal dose of the peptide is 100mcg to 500 mcg to be administered one to three times every day (3), (4).
The effects of the peptide are dependent on the amount of dose an individual takes.
Recommended dose of 300mcg three times a day stimulates performance enhancement and boosts energy levels. Whereas a daily dose of 200mcg stimulates anti-aging properties.
Hence, it is best recommended to seek medical advice prior to use to ensure best results.
When is the best time to take Ipamorelin?
One should have the peptide either in the morning or at night, however, it is recommended to administer the peptide at the same time daily for best results.
Additionally, one should avoid consuming any food or drinks at the minimum for one hour before and after administration. This is to allow the medication to flow easily through the bloodstream and have it absorbed easily within the body.
Common Ipamorelin Combinations or Blends
Ipamorelin is a short acting substance with an average half life of 2 hours. In other words, an individual starts losing 75% of the peptide effects within a matter of 4 hours. Due to this, it is recommended to have Ipamorelin in combination with other similar peptides as described below.
Ipamorelin and CJC 1295 Blend
CJC 1295 is an anti-aging peptide that starts showing effects after approximately 4 hours of administration, but the effect lasts for several weeks. When it is taken in combination with Ipamorelin peptide, the anti-aging effects start kicking in almost instantly – with Ipamorelin stimulating the effects immediately up to 4 hours and as it starts weaning off, then the other peptide starts acting.
Ipamorelin and Sermorelin Blend
In this peptide combination, Ipamorelin is in fact the longer acting drug because Sermorelin is effective for only up to a few minutes. The main benefit here is that both substances have different mechanisms of action, where Ipamorelin peptide acts on the pituitary gland while the Sermorelin peptide acts solely on the growth hormone secreting receptors. Therefore, an individual administering this combination gets a higher “kick” and immediate results rather than just administering one medication.
Both the above combinations are recommended to be administered in a 1:1 ratio and the blended mixture is administered subcutaneously, with a total dose of 300 micrograms per day.
Based on the referenced studies, both of the above combinations are recommended to be administered in a 1:1 ratio and the blended mixture is administered subcutaneously, with a total dose of 300 micrograms per day (3), (4), (8).
Ipamorelin is a synthetic pentapeptide proven to demonstrate similar effects as human growth hormones and is commonly known as the ‘growth hormone secretagogue.’ The peptide has shown to have anti-aging effects along with elevating metabolic rate and increased bone density in human body.
All research and clinical studies of this peptide have demonstrated a highly safe, effective, and completely non-toxic drug profile where the medication has shown mechanism in two distinct ways i.e., either via acting on the pituitary gland or on the hypothalamus with agonistic effects on the growth hormone receptors.
Proven to exhibit abilities similar to the naturally occurring growth hormones, Ipamorelin has opened several possibilities of its potential long-term use on children with naturally growth hormone deficiency. There are still ongoing studies being conducted in this area.
Should you consider opting for Ipamorelin, we recommend seeking medical advice prior to use. While this article captures all the medical uses, side effects, and recommended drug combinations for the Ipamorelin peptide, a tailored prescription and medical advice is required based on individual profile.
1. A Giustina, JD Veldhius, Pathophysiology of the neuro regulation of growth hormone secretion in experimental animals and the human, Endocrinology, 1 December 1998.
2. David E. Beck et al., Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients, International Journal of Colorectal Disease, 2014.
3. K. Raun et al., Ipamorelin, the first selective growth hormone secretagogue, Endocrinology, November 1998.
4. P.B Johansen et al, Ipamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats, Growth Hormone IGF Research, April 1999.
5. Gobburu, J.V.S., Agersø, H., Jusko, W.J. et al. Pharmacokinetic-Pharmacodynamic Modeling of Ipamorelin, a Growth Hormone Releasing Peptide, in Human Volunteers. Pharm Res 16, 1412–1416 (1999).
6. Rogério G. Gondo et al, Growth Hormone-Releasing Peptide-2 Stimulates GH Secretion in GH-Deficient Patients with Mutated GH-Releasing Hormone Receptor, The Journal of Clinical Endocrinology & Metabolism, Volume 86, Issue 7, 1 July 2001, Pages 3279–3283.
7. Mericq V, Cassorla F, Salazar T, Avila A, Iñiguez G, Bowers CY, Merriam GR. Effects of eight months treatment with graded doses of a growth hormone (GH)-releasing peptide in GH-deficient children. J Clin Endocrinol Metabolism, Jul 1998; 83(7):2355-60.
8. Sinha, D. K., Balasubramanian, A., Tatem, A. J., Rivera-Mirabal, J., Yu, J., Kovac, J., Pastuszak, A. W., & Lipshultz, L. I. (2020). Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males. Translational andrology and urology, 9(Suppl 2), S149–S15.
For more details on Ipamorelin peptide research, an overall review and its potential benefits, read our latest Ipamorelin Weight Loss, Anti Aging Benefits, Side Effects blog post.
There’s also increased levels of research being done with peptide blends, in particular CJC 1295 Ipamorelin Peptide Blend. To read more about this Ipamorelin CJC blend, check out our extensive review in our CJC 1295 Ipamorelin Research Benefits blog post.
NOTE: These products are all intended for laboratory research use only. Ipamorelin peptide is not for personal use. Please review and adhere to our Terms and Conditions before ordering.
Dr. Marinov (MD, Ph.D.) is a researcher and chief assistant professor in Preventative Medicine & Public Health. Prior to his professorship, Dr. Marinov practiced preventative, evidence-based medicine with an emphasis on Nutrition and Dietetics. He is widely published in international peer-reviewed scientific journals and specializes in peptide therapy research.