Appendix One - Overview of Peptides
Peptides is a generic name given to any group of amino acids that are linked together to form a chain. Essentially, they are similar to proteins, though in much shorter lengths (less than 50 units long). In the world of sport, peptides generally refer to one of two things: either broken protein fragments from hydrolysed proteins; or peptide hormones and related compounds.
Protein peptides are whole proteins that are broken down into smaller peptide fragments by a process of hydrolysis. Hydrolysed proteins are absorbed much faster than other forms of protein and are commonly found in supplements that contain hydrolysed whey protein.
A peptide hormone is a protein which is released in the blood stream. Usually, the peptide hormone is secreted by the pituitary gland. Peptide hormones include growth hormone and insulin. The substances involved in this case stimulate the production of peptide hormones, which is different to substances that mimic the effects of peptide hormones such as somatropin (a synthetic human growth hormone).
The substances identified as being used in Australia are GHRP-2, GHRP-6, CJC-1295, AOD-9604 and hexarelin. An overview summary of these substances is provided below:
GHRP-2 and GHRP-6
GHRP-2 and GHRP-6 are growth hormone-releasing factors and are therefore prohibited S2 Hormones and Related Substances according to the WADA Prohibited List. They are part of the growth hormone-releasing peptide (GHRP) family, which includes GHRP-1, GHRP-2, GHRP-4, GHRP-6, alexamorelin, ipamorelin and hexarelin. GHRPs are used to stimulate the release of Growth Hormone (GH) by the pituitary gland. They also promote food intake by stimulating hunger and aid in energy metabolism.
Purported benefits of using GHRPs include bone mineral density, increased lean muscle mass, improved strength, rejuvenation and strengthening of joints and improved recovery from injury such as bone fractures. Side effects from the use of GHRP may include hot flushes, loud stomach rumbling, white blood cell count increase, sweating and increased appetite.
GHRP-2 and 6 are administered by subcutaneous injection. GHRP-2 and GHRP-6 are detectable in urine.
CJC-1295 is considered a growth hormone-releasing factor and is therefore considered to be prohibited according to the WADA Prohibited List in the S2 category (Peptide hormones, growth factors and related substances). CJC-1295 is a synthetic peptide hormone, similar in structure to GHRH, which stimulates the release of growth hormone, and subsequently IGF-1, from the pituitary gland. CJC-1295 was initially developed to treat those suffering from growth disorders, muscle wasting diseases or burns victims. However, CJC-1295 is not approved for human use.
CJC-1295’s purported anabolic effects may increase lean muscle mass, reduce fat and improve performance. In addition, CJC-1295 has anti-inflammatory properties if administered directly to the related area soon after injury, can reduce pain and swelling and also assist in the repair of injured tissue. It is also purported to promote slow wave sleep (SWS) which is responsible for the highest level of muscle growth and memory retention. Further benefits include reduced body fat, increased energy and vitality, increased endurance, accelerated healing, and strengthening of the heart.
CJC-1295 is administered by subcutaneous injection, usually in the abdomen. It is also available as a cream.
AOD-9604 is not currently prohibited under category S2 of the WADA Prohibited List.
AOD-9604 works by mimicking the way natural GH regulates the metabolism of fat by stimulating lipolysis (the breakdown or destruction of fat) and inhibits lipogenesis (the transformation of non-fat food materials into body fat). Reports by Caldaza Ltd have shown that AOD-9604 had positive (anabolic) effects on cartilage tissue formation as well as enhancements in the ‘differential of muscle progenitor cells (cells that create muscle cells) to muscle cells’. Other purported benefits of AOD-9604 include increasing muscle mass and IGF-1 levels. AOD-9604 is not approved for human use.
Hexarelin is considered a growth hormone releasing factor and is therefore prohibited under category S2, Hormones and Related Substances, according to the WADA Prohibited List. As with GHRP-6, hexarelin stimulates the release of GH, with effects similar to those experienced when using a synthetic growth hormone.
Purported beneficial effects of hexarelin use include increased strength, growth of new muscle fibres and increases in the size of existing muscle fibres, joint rejuvenation and assistance in healing. Hexarelin may also be beneficial in fat reduction. Unlike GHRP-6, there is no effect on appetite as it does not increase ghrelin levels responsible for increased hunger and gastric emptying.
Hexarelin can be administered orally in tablet form or via subcutaneous injection.