Ipamorelin

Ipamorelin
Ipamorelin.svg
Clinical data
Routes of
administration
Intravenous, subcutaneous
ATC code
  • None
Pharmacokinetic data
Elimination half-life2 hours[1]
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC38H49N9O5
Molar mass711.85296 g/mol g·mol−1
3D model (JSmol)

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 .[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 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]

See also

References

  1. ^ a b Gobburu, Jogarao V. S.; Agersø, Henrik; Jusko, William J.; Ynddal, Lars (1999). "Pharmacokinetic-Pharmacodynamic Modeling of Ipamorelin, a Growth Hormone Releasing Peptide, in Human Volunteers". Pharmaceutical Research. 16 (9): 1412–1416. doi:10.1023/A:1018955126402. ISSN 0724-8741.
  2. ^ Moulin, Aline; Ryan, Joanne; Martinez, Jean; Fehrentz, Jean-Alain (2007). "Recent Developments in Ghrelin Receptor Ligands". ChemMedChem. 2 (9): 1242–1259. doi:10.1002/cmdc.200700015. ISSN 1860-7179. PMID 17520591.
  3. ^ a b c d Raun, K; Hansen, B.; Johansen, N.; Thogersen, H; Madsen, K; Ankersen, M; Andersen, P. (1998). "Ipamorelin, the first selective growth hormone secretagogue". European Journal of Endocrinology. 139 (5): 552–561. doi:10.1530/eje.0.1390552. ISSN 0804-4643.
  4. ^ Isidro, Maria; Cordido, Fernando (2006). "Growth Hormone Secretagogues". Combinatorial Chemistry & High Throughput Screening. 9 (3): 175–180. doi:10.2174/138620706776055458. ISSN 1386-2073.
  5. ^ a b Estrada, R. Cañete; Jiménez-Reina, L.; de la Torre, M.J.; Bernal, J. (2002). "Chronic In Vivo Ipamorelin Treatment Stimulates Body Weight Gain and Growth Hormone (GH) Release In Vitro in Young Female Rats". 6 (1): 37–46. ISSN 1136-4890.
  6. ^ Beck, David E.; Sweeney, W. Brian; McCarter, Martin D. (2014). "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): 1527–1534. doi:10.1007/s00384-014-2030-8. ISSN 0179-1958.
  7. ^ AdisInsight. "Ipamorelin". Retrieved 10 June 2015.
  8. ^ "Peptides under greater scrutiny in MLB's performance-enhancing drug battle". USA TODAY. Retrieved 2018-04-14.
  9. ^ "NBA Playoffs 2018: Wizards' Jodie Meeks suspended 25 games for failing drug test". CBSSports.com. Retrieved 2018-04-14.

External links