Chemistry:Ipamorelin
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| Routes of administration | Intravenous, subcutaneous |
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| Elimination half-life | 2 hours[1] |
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| Formula | C38H49N9O5 |
| Molar mass | 711.868 g·mol−1 |
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Ipamorelin (INN) (developmental code name NNC 26-0161) is a peptide selective agonist of the ghrelin/growth hormone secretagogue receptor (GHS) and a growth hormone secretagogue.[2][3] It is a pentapeptide with the amino acid sequence Aib-His-D-2-Nal-D-Phe-Lys-NH2 that was derived from GHRP-1.[4]
Ipamorelin significantly increases plasma growth hormone (GH) levels in both animals and humans.[1][3][5] In addition, ipamorelin stimulates body weight gain in animals.[5] Like pralmorelin and GHRP-6, ipamorelin does not affect prolactin, follicle-stimulating hormone (FSH), luteinizing hormone (LH), or thyroid-stimulating hormone (TSH) levels.[3] However, unlike pralmorelin (GHRP-2) and GHRP-6, but similarly to growth hormone-releasing hormone (GHRH), ipamorelin does not stimulate the secretion of adrenocorticotropic hormone (ACTH), or cortisol, and is highly selective for inducing the secretion only of GH.[3]
Ipamorelin was originally developed by Novo Nordisk, and was investigated in phase II clinical trials by Helsinn Therapeutics for the treatment of postoperative ileus, but was discontinued due to lack of efficacy.[6][7]
Ipamorelin has been used by athletes as a performance enhancing drug.[8][9][10]
See also
- List of growth hormone secretagogues
References
- ↑ 1.0 1.1 "Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers". Pharmaceutical Research 16 (9): 1412–6. September 1999. doi:10.1023/A:1018955126402. PMID 10496658.
- ↑ "Recent developments in ghrelin receptor ligands". ChemMedChem 2 (9): 1242–59. September 2007. doi:10.1002/cmdc.200700015. PMID 17520591.
- ↑ 3.0 3.1 3.2 3.3 "Ipamorelin, the first selective growth hormone secretagogue". European Journal of Endocrinology 139 (5): 552–61. November 1998. doi:10.1530/eje.0.1390552. PMID 9849822.
- ↑ "Growth hormone secretagogues". Combinatorial Chemistry & High Throughput Screening 9 (3): 175–80. March 2006. doi:10.2174/138620706776055458. PMID 16533150.
- ↑ 5.0 5.1 "Chronic In Vivo Ipamorelin Treatment Stimulates Body Weight Gain and Growth Hormone (GH) Release In Vitro in Young Female Rats". European Journal of Anatomy 6 (1): 37–46. 2002. ISSN 1136-4890. https://www.researchgate.net/publication/28093664.
- ↑ "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 29 (12): 1527–34. December 2014. doi:10.1007/s00384-014-2030-8. PMID 25331030.
- ↑ "Ipamorelin". AdisInsight. Springer Nature Switzerland AG. http://adisinsight.springer.com/drugs/800011351.
- ↑ "Peptides under greater scrutiny in MLB's performance-enhancing drug battle" (in en). USA TODAY. 5 May 2016. https://www.usatoday.com/story/sports/mlb/2016/05/04/peptides-mlb--investigation-performance-enhancing-drugs-biogenesis/83915662/.
- ↑ Maloney, Jack (13 April 2018). "NBA Playoffs 2018: Wizards' Jodie Meeks suspended 25 games for failing drug test" (in en). CBSSports.com. https://www.cbssports.com/nba/news/nba-playoffs-2018-wizards-jodie-meeks-suspended-25-games-for-failing-drug-test/.
- ↑ "Nets' Chandler suspended 25 games for PED use" (in en). nba.com. https://www.nba.com/article/2019/08/29/nets-wilson-chandler-suspended-official-release/.
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