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Ipamorelin Peptide Therapy | A-Z Guide

Curious about Ipamorelin peptide therapy? Inside, we detail everything you need to know about the research chemical – dosing, benefits, side effects, and more.

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Ipamorelin Peptide Therapy
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Curious about Ipamorelin peptide therapy? Then you’re in the right place.

Ipamorelin is a synthetic peptide that stimulates the natural production of growth hormone in the body. This implicates the peptide in a range of biological processes, including bone formation, muscle growth, and fat loss.

While ipamorelin has been around for over two decades, most research into the peptide is limited to animal studies and in vitro experiments. To date, the only ipamorelin research involving human subjects has involved patients suffering from postoperative ileus, which is characterized by a loss of bowel function following a surgical procedure.

While the safety record on ipamorelin and related GH secretagogues appears favorable, the research community requires further investigation into this potent stimulator of growth hormone.

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Like most growth hormone secretagogue peptides, ipamorelin peptide has not been approved to treat any medical condition. Further, its use is prohibited by major sporting organizations subject to the World Anti-Doping Code, due to the peptide’s ability to enhance athletic performance. 

Nonetheless, qualified researchers may source this peptide online, but are encouraged to buy only from a reliable vendor that adheres to industry best practices. 

Our top recommendation for sourcing ipamorelin online is Peptide Sciences.

Read on as the team at Peptides.org discusses the research on ipamorelin, including its mechanism of action, potential therapeutic uses, and safety profile. 

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Ipamorelin

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What is Ipamorelin?

Ipamorelin is a synthetic growth hormone secretagogue (GHS) that stimulates the pituitary gland to release growth hormone (GH), thereby affecting key biological processes like bone health, metabolism, and body composition [1, 2]. 

Structurally, it is a pentapeptide composed of five amino acids, and an agonist of the ghrelin receptor (GHSR), which plays a key role in regulating energy homeostasis and body weight [1, 2].

Ipamorelin was identified in 1998 as the first synthetic GHS to achieve selective GH release, showing a selectivity that was comparable to growth hormone-releasing hormone (GHRH) [1, 2]. It was developed by the pharmaceutical company Novo Nordisk and assigned the developmental code name NNC 26-0161 [3]. 

Subsequently, ipamorelin was notably investigated as a treatment of postoperative ileus, which is characterized by a lack of propulsive ability of the intestine, leading to bowel obstruction [4, 5].

Although clinical research on ipamorelin is limited, research in animal models has shown its potential for treating childhood GH deficiency and other growth disorders [6]. 

However, more extensive clinical research is needed to fully understand the possible therapeutic applications of ipamorelin, along with its possible long-term effects. For the time being, ipamorelin is classed as a research peptide and available for purchase by qualified researchers for laboratory experimentation only. 
 

What Does Ipamorelin Do?

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Ipamorelin is a ghrelin receptor agonist, and thus mimics the effects of the naturally-occurring hormone ghrelin, which is responsible for regulating GH secretion. Ghrelin is also associated with physiological processes such as hunger and metabolism [7]. 

Ipamorelin’s binding to the ghrelin receptor in the brain triggers a series of downstream effects, including the direct stimulation of the cells in the pituitary gland, causing them to release GH and thus result in a rise in GH levels throughout the body [7]. The role of ipamorelin in triggering GH release has implications for a range of physiological processes, including metabolism, muscle growth, and bone formation [1, 2, 8]. 

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A seminal study found that ipamorelin, unlike many other GH secretagogues and rHGH treatment itself, does not elevate the plasma levels of other hormones in the body, such as the stress hormone cortisol. In other words, ipamorelin acts by selectively increasing GH, similar to the action of growth hormone-releasing hormone (GHRH) [1].

This targeted selectivity of ipamorelin is seen as advantageous when investigating its potential therapeutic uses. Researchers have called for closer investigation into the selectivity of ipamorelin as a targeted treatment of growth-related impairments that does not induce additional hormonal changes [1].  

Ipamorelin Benefits | Clinical Trials and Research

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While research into the potential therapeutic uses of ipamorelin is still in its early stages, animal and in vitro studies have provided some insights into its potential benefits, namely as regards bone formation, stimulation of GI motility, and effects on muscle growth.

Here is a summary of research-backed findings and benefits of ipamorelin administration:

Ipamorelin and Bone Health

An early study investigated the effects of ipamorelin on rats that were injected with glucocorticoid, a type of steroid hormone that is associated with bone density loss [8]. Study authors found that ipamorelin counteracted the decrease in bone formation and muscle strength initially caused by glucocorticoid treatment, proposing that ipamorelin may treat conditions that negatively affect bone health.

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In a pair of separate studies on female rats, the peptide was shown to increase the bone growth rate of the proximal tibia in rodents [6] and increased their bone mineral content and bone dimensions [10]. Increased bone mineral content due to ipamorelin peptide therapy is posited to reduce the risk of bone fracture, pointing to the peptide’s potential osteoprotective effect [11].

In light of these preliminary results, clinical trials are necessary to investigate the therapeutic possibilities of ipamorelin in relation to bone health.

Ipamorelin and Gastric Motility

Ipamorelin has been shown to stimulate gastrointestinal motility in rodents with delayed gastric emptying disorder via ghrelin receptor-mediated mechanisms [9]. Treatment with ipamorelin was observed to significantly accelerate gastric emptying and prompt bowel movement in the rodents.

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In clinical trials, researchers examined the impact of ipamorelin on patients with postoperative ileus, a relatively common post-surgery condition where patients experience difficulty in eating and digesting solid foods. The study found that ipamorelin drastically shortened the time it took for the patients to be able to take their first meal, by about 12 hours [4]. Despite showing effectiveness for this use and being well-tolerated by the patients, the ipamorelin trials were discontinued due to a financial decision taken by the investigating firm. 

Ipamorelin and Muscle Strength

In the above-mentioned glucocorticoid-treated rat study by Andersen et al, the rats treated with both ipamorelin and glucocorticoids showed a higher degree of muscle strength than those receiving glucocorticoids alone [8]. This finding demonstrates that ipamorelin may have a protective effect against loss of muscle strength, especially in cases where medications like glucocorticoids that lead to muscle atrophy are taken.

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Growth hormone itself is known to possess anabolic properties, working to increase muscle strength by enhancing muscle mass [12]. While the direct impact of ipamorelin on muscle strength has not yet been studied, the peptide’s ability to stimulate GH is widely believed to enhance muscle performance in competitive athletics and muscle function in the elderly subjects. 

Ipamorelin and GH Deficiency

An early study looked into the impact of a related synthetic peptide and ipamorelin predecessor, GHRP-2, on GH-deficient children. Six children with GH deficiency were administered subcutaneous injections of GHRP-2 for four successive periods of two months, with GHRH added to the fourth period of administration. While GHRP-2 was successful in promoting nocturnal GH secretion and increased growth velocity in the treatment phase, the authors called for the development of a treatment with a longer duration of action [13]. 

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While there is clear benefit to the use of ipamorelin as a treatment of GHD, given its selectivity for the ghrelin receptor, research on this use is still needed.

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Ipamorelin Safety and Side Effects

Due to the paucity of clinical trial data on ipamorelin, researchers still do not have a clear picture of the safety and potential side effects of ipamorelin treatment. 

To date, only one clinical study has investigated the effects of ipamorelin treatment, involving just 114 participants over the course of seven days. Ipamorelin administered by intravenous infusion at a dose of 0.03mg/kg twice daily was found to be well tolerated by the patients, who were experiencing postoperative ileus as a consequence of abdominal surgery [4].

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Despite the lack of human data, the initial findings are encouraging and offer a strong basis for future study into the effects and safety of ipamorelin.

Drawing on the existing research, researchers have observed recently that adverse effects due to ipamorelin treatment are rare and similar to those of sermorelin, another GH secretagogue that was previously FDA-approved to treat growth hormone deficiency in children [14]. Such side effects may include:

•    Facial flushing
•    Nausea
•    Vomiting
•    Headache
•    Redness at the injection site

These effects are typically transient and cease with discontinuation of treatment.

Given the limited data available, it is not possible to definitively conclude on the safety profile of ipamorelin at this time. Further clinical study is needed to fully understand the safety and effectiveness of ipamorelin treatment. 

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Is Ipamorelin Legal?

Ipamorelin, like many other research peptides, is legal for purchase, sale, and handling strictly for research purposes. As a research chemical, it should only be handled by licensed research professionals for laboratory experimentation. 

Ipamorelin has not been approved by the United States Food and Drug Administration to treat any medical condition, and may not be marketed in the United States for human use at this time. 

Accordingly, researchers should take care to avoid buying peptide products from online vendors who unlawfully market peptides, often with insufficient disclaimers and unsupported medical claims.

To ensure the purchase of a high-quality and safe peptide product, researchers should undertake to purchase only from a vendor who:

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•    Indicates that their products are sold for research purposes only and not for human use, and may only be handled by qualified research personnel; 
•    Provides accurate, up-to-date information on their products and refrains from making any unfounded medical claims regarding the use of their products; and,
•    Publishes the results of third-party laboratory reports to confirm the identity and purity of the peptide products offered for sale.

Any researcher involved in the field of competitive athletics should note that ipamorelin is explicitly listed in the Prohibited List of the World Anti-Doping Code of the World Anti-Doping Agency (WADA) [15]. Ipamorelin is a class S2 non-specified substance, and prohibited to any athlete subject to the Code at all times, whether in or out of competition. In the United States, the United States Anti-Doping Agency (USADA) is tasked with adopting and enforcing the WADA Code, and has also prohibited the use of ipamorelin in sport, notably in competitions of the Ultimate Fighting Championship (UFC) [16].

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The prohibition of the use of ipamorelin in sport is due its potential to enhance athletic performance, providing an unfair advantage to the user over other competitors. Notably, UFC athlete David Branch was handed a two-year suspension from competition by USADA in September 2019, for having tested positive for ipamorelin based on a urine sample provided to the organization [17]. 

Despite the challenges associated with the legal and regulatory status of ipamorelin at this time, there is great promise in ipamorelin peptide therapy and it should be further investigated for a host of potential applications.

Ipamorelin Dosage and Cycle

Ipamorelin has not been approved for medical use and there are no established guidelines for determining a safe and effective dose of this peptide. Research on the peptide is strictly limited to laboratory experimentation, unless research in test subjects is authorized.

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However, researchers may be interested to know how ipamorelin may be dosed in future experiments. 

Based on the available literature, here are some notes regarding ipamorelin administration and dosage [4, 14]:

•    Ipamorelin is most commonly delivered via subcutaneous or intramuscular injection, the methods considered most effective.
•    Treatment with ipamorelin has been shown to be dose-dependent and doses will vary depending on the desired therapeutic outcome.
•    A common dosing protocol used by researchers is 200mcg to 500mcg of ipamorelin per day via subcutaneous injection. Doses greater than 200mcg may be split into two to three injections, administered at different times of day.
•    Researchers are encouraged to begin with a low dose, before gradually increasing the daily ipamorelin dosage.
•    Current research does not generally support the long-term use of ipamorelin in subjects, for periods exceeding 12 weeks.

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Sample Ipamorelin Dosing Protocol

Based on above, researchers may refer to this sample ipamorelin dosing protocol for improving body composition in test subjects:

•    Ipamorelin Dosage: 200mcg to 500mcg of ipamorelin administered via subcutaneous injection, daily. 
•    Timing and Frequency: Administer ipamorelin at the same time daily. For total doses over 200mcg, administer two daily injections, one in the morning and one in the afternoon.
•    Study Duration: 8-12 weeks
•    Ipamorelin Cycle: The application of ipamorelin should be cycled to avoid over-activation of the GHS-R receptors, allowing the subject rest periods equivalent to the length of each administration period, immediately following said period.
•    Notes: This dosing protocol calls for two to four 10mg vials of ipamorelin per subject for a 12-week course.

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Researchers are encouraged to follow best practices for peptide reconstitution and administration, while staying up-to-date on emerging research regarding ipamorelin treatment. 

Where to Buy Ipamorelin Online?

If you’re a qualified researcher looking to buy ipamorelin online , source your material only from a vetted and reliable vendor to guarantee quality and safety in experimentation. 

The research team at Peptides.org has tested a variety of ipamorelin vendors, finding that only one meets our strict criteria of product purity, ease of ordering, and customer service.

Based on our experience, Peptide Sciences is the top destination for purchasing ipamorelin online. 

The vendor also offers a 10mg ipamorelin/CJC-1295 blend for further enhancing the benefits provided by these two distinct GH secretagogues. 

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Here are some reasons why we wholeheartedly endorse this vendor:

•    Research-Grade Peptides: Peptide Sciences offers 99% pure peptides that have undergone third-party laboratory testing via state-of-the-art HPLC-MS techniques. Peptide batches are tested and backed by a certificate of analysis that details the contents and purity of your ipamorelin.

•    Cost-Effective Research: Peptide Sciences offers a cost-effective option for qualified research professionals looking to purchase ipamorelin. Single ipamorelin 5mg vials retail for $46, and there are discounts available for researchers buying 5 or 10 vials at a time. The 10mg ipamorelin/CJC-1295 blend has an attractive per-unit price of $80.

•    Convenient Shipping: Peptide Sciences offers free shipping for U.S. orders above $200, and ships to various international locations with rates calculated at checkout. In our experience, orders in the United States take two to three business days to arrive.

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•    Flexible Payments: Researchers can take advantage of a simple ordering process on the Peptide Sciences website, enabling them to place their orders in a range of payment methods, including major credit cards, electronic checks, and cryptocurrencies.

•    Excellent Customer Service: Peptide Sciences has friendly and knowledgeable customer service representatives who are available by email to walk customers through any inquiries or concerns.

How to Reconstitute Ipamorelin

When purchasing ipamorelin for injection, you will receive the peptide in the form of a lyophilized powder. Lyophilization preserves the peptide and allows it to be transported and kept at room temperature without undergoing degradation.

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To prepare ipamorelin for injection, the peptide must be reconstituted with a solution like bacteriostatic water, which will dissolve the peptide into a clear liquid that may then be injected

To complete this process, researchers will need a selection of laboratory equipment including alcohol swabs, needles, and bacteriostatic water. 

The experts at Peptides.org suggest purchasing a complete research kit from BacteriostaticWater.org , to ensure a smooth and safe reconstitution process. 

Here are some basic guidelines for reconstituting ipamorelin with bacteriostatic water: 

1.    Wash your hands thoroughly and prepare all necessary materials, including the vial of ipamorelin powder, bacteriostatic water, alcohol wipes, a syringe, and a needle. 
2.    Use an alcohol swab to wipe the rubber stoppers of both the bacteriostatic water and ipamorelin vials. 
3.    Insert the needle into the bacteriostatic water container and draw up the amount needed. 
4.    Then, transfer the correct quantity of bacteriostatic water into the vial of ipamorelin powder.
5.    Gently rotate the ipamorelin vial to fully mix the contents. Ensure not to stir or shake the vial. The ipamorelin solution should be clear with no visible powder. 
6.    The ipamorelin is ready for injection. Adhere to standard medical guidelines for subcutaneous or intramuscular injection.

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As always, refrigerate any reconstituted solution that will not be used right away.

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Ipamorelin

Ipamorelin FAQ 

How to Take Ipamorelin?

Ipamorelin is usually available as a lyophilized powder that must be reconstituted with bacteriostatic water prior to administration via subcutaneous injection.

How is Ipamorelin Delivered

After reconstitution, ipamorelin may be delivered via subcutaneous or intramuscular injection. It has also been delivered via intravenous infusion in a trial involving postoperative ileus patients.

Is Ipamorelin Dangerous?

Ipamorelin is a research peptide that must be handled strictly by trained professionals. Based on the limited research to date, it is well-tolerated with few adverse events reported. Researchers are encouraged to consult the literature on related growth hormone secretagogues, which are believed to present similar safety profiles. 

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Is Ipamorelin a Steroid?

No. Ipamorelin is a synthetic peptide and not an anabolic-androgenic steroid; it does not have affinity for the androgen receptor. 

Does Ipamorelin Increase Testosterone?

No. Current research does not indicate any role of ipamorelin in the production of testosterone. Via its simulation of the ghrelin receptor, it does impact the production of human growth hormone (GH) in the body.

Does Ipamorelin Build Muscle?

There is some evidence that ipamorelin may contribute to the development of muscle mass and strength, via its impact on GH and IGF-1 levels when administered [12]. The peptide has also been found to counter muscle catabolism in glucocorticoid-treated rats [8]. However, more research is necessary to establish a clear connection between ipamorelin treatment and muscle growth in subjects.

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Does Ipamorelin Cause Weight Gain?

Ipamorelin has not been shown to cause weight gain in test subjects, and its impact on GH and IGF-1 levels, insulin release, and food intake patterns may have the opposite effect, especially in obese subjects. 

Ipamorelin Peptide Therapy | Review

Ipamorelin is a synthetic ghrelin receptor agonist with a potent effect on growth hormone secretion. Discovered in 1998, it is one of the most selective GH secretagogues identified to date, allowing it to stimulate natural growth hormone production without affecting other hormones like cortisol.

It is implicated in important processes like bone formation, metabolism, and body composition, and has been investigated as a treatment of postoperative ileus. While few adverse events have been linked to ipamorelin, more research is needed to gain a fuller understanding of the peptide’s potential benefits and safety profile. 

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Qualified research professionals looking to source research-grade ipamorelin should head directly to top supplier Peptide Sciences .

References

1.    Raun K, Hansen BS, Johansen NL, Thøgersen H, Madsen K, Ankersen M, Andersen PH. Ipamorelin, the first selective growth hormone secretagogue. Eur J Endocrinol. 1998 Nov;139(5):552-61. doi: 10.1530/eje.0.1390552. PMID: 9849822.

2.    PubChem [Internet]. Bethesda (MD): National Library of Medicine (US), National Center for Biotechnology Information; 2004-. PubChem Compound Summary for CID 9831659, Ipamorelin; [cited 2023 Feb. 5]. Available from: https://pubchem.ncbi.nlm.nih.gov/compound/Ipamorelin

3.    Ishida J, Saitoh M, Ebner N, Springer J, Anker SD, von Haehling S. Growth hormone secretagogues: history, mechanism of action, and clinical development. JCSM Rapid Communications. 2020; 3(1): 25- 37.

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4.    Beck DE, Sweeney WB, McCarter MD; Ipamorelin 201 Study Group. Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients. Int J Colorectal Dis. 2014 Dec;29(12):1527-34. doi: 10.1007/s00384-014-2030-8. Epub 2014 Oct 21. PMID: 25331030.

5.    Buchanan L, Tuma F. Postoperative Ileus. 2022 Aug 1. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan–. PMID: 32809615.

6.    Johansen PB, Nowak J, Skjaerbaek C, Flyvbjerg A, Andreassen TT, Wilken M, Orskov H. Ipamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats. Growth Horm IGF Res. 1999 Apr;9(2):106-13. doi: 10.1054/ghir.1999.9998. PMID: 10373343.

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7.    Devesa J. The Complex World of Regulation of Pituitary Growth Hormone Secretion: The Role of Ghrelin, Klotho, and Nesfatins in It. Front Endocrinol (Lausanne). 2021 Mar 11;12:636403. doi: 10.3389/fendo.2021.636403. PMID: 33776931; PMCID: PMC7991839.

8.    Andersen NB, Malmlöf K, Johansen PB, Andreassen TT, Ørtoft G, Oxlund H. The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats. Growth Horm IGF Res. 2001 Oct;11(5):266-72. doi: 10.1054/ghir.2001.0239. PMID: 11735244.

9.    Greenwood-Van Meerveld B, Tyler K, Mohammadi E, Pietra C. Efficacy of ipamorelin, a ghrelin mimetic, on gastric dysmotility in a rodent model of postoperative ileus. J Exp Pharmacol. 2012 Oct 19;4:149-55. doi: 10.2147/JEP.S35396. PMID: 27186127; PMCID: PMC4863553.

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10.    Svensson J, Lall S, Dickson SL, Bengtsson BA, Rømer J, Ahnfelt-Rønne I, Ohlsson C, Jansson JO. The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats. J Endocrinol. 2000 Jun;165(3):569-77. doi: 10.1677/joe.0.1650569. PMID: 10828840.

11.    Haseltine KN, Chukir T, Smith PJ, Jacob JT, Bilezikian JP, Farooki A. Bone Mineral Density: Clinical Relevance and Quantitative Assessment. J Nucl Med. 2021 Apr;62(4):446-454. doi: 10.2967/jnumed.120.256180. Epub 2020 Dec 11. PMID: 33310738; PMCID: PMC8049374.

12.    Chikani V, Ho KK. Action of GH on skeletal muscle function: molecular and metabolic mechanisms. J Mol Endocrinol. 2013 Dec 19;52(1):R107-23. doi: 10.1530/JME-13-0208. PMID: 24163428.

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13.    Verónica Mericq, Fernando Cassorla, Teresa Salazar, Alejandra Avila, Germán Iñiguez, Cyril Y. Bowers, George R. Merriam, Effects of Eight Months Treatment with Graded Doses of a Growth Hormone (GH)-Releasing Peptide in GH-Deficient Children, The Journal of Clinical Endocrinology & Metabolism, Volume 83, Issue 7, 1 July 1998, Pages 2355–2360, https://doi.org/10.1210/jcem.83.7.4969

14.    Sinha DK, Balasubramanian A, Tatem AJ, Rivera-Mirabal J, Yu J, Kovac J, Pastuszak AW, Lipshultz LI. Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males. Transl Androl Urol. 2020 Mar;9(Suppl 2):S149-S159. doi: 10.21037/tau.2019.11.30. PMID: 32257855; PMCID: PMC7108996.

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15.    The prohibited list [Internet]. World Anti Doping Agency. 2023 [cited 2023Feb8]. Available from: https://www.wada-ama.org/en/prohibited-list?q=ipamorelin 

16.    The UFC Prohibited List [Internet]. USADA. 2023 [cited 2023Feb8]. Available from: https://ufc.usada.org/wp-content/uploads/2023-UFC-Prohibited-List.pdf 

17.    David Branch Receives Sanction for Violation of UFC Anti-Doping Policy [Internet]. USADA. Sep 18, 2019 [cited 2023Feb8]. Available from: https://ufc.usada.org/david-branch-receives-doping-sanction

Disclaimer: The above is a sponsored post, the views expressed are those of the sponsor/author and do not represent the stand and views of Outlook Editorial.

 

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