Many studies have been conducted on the growth hormone (GH) secretagogue Ipamorelin. These studies suggest that it seems to be a powerful agonist of the growth hormone/ghrelin secretagogue receptor, making it one of the most selective secretagogues [i]. Ipamorelin’s selectivity is explained by the fact that it does not seem to influence the production of other pituitary hormones. Included in this category are hormones, including prolactin, follicle-stimulating hormone (FSH), luteinizing hormone (LH), thyroid-stimulating hormone (TSH), and adrenocorticotropic hormone (ACTH).
Research suggests Ipamorelin seems to promote growth hormone production by acting like that of the naturally occurring hormone ghrelin [ii]. The negative feedback loop that controls this process ensures that excessive GH production has no harmful consequences. Findings imply that Ipamorelin may be found to influence a wide variety of biological systems due to the widespread distribution of ghrelin receptors. These systems include the central nervous system, the respiratory system, the digestive system, the adipose tissue, the kidney, the pancreas, and the immunological system. Researchers have speculated that Ipamorelin may improve bowel movement and stomach function, enhance the development and repair of muscles, facilitate the release of insulin hormone from the pancreas, and stimulate the growth and development of bones, all based on their findings. Besides these roles, investigations purport that Ipamorelin may also help repair damaged cells, revitalize the skin, boost collagen formation, and give the skin a youthful appearance and feel [iii]. This practice supposedly enhances cognitive performance, sleep, immunity, and cardiovascular disease risk. The combination of CJC-1295 and Ipamorelin has been proposed as a possible adjuvant to speed up recovery from injury, enhance sleep quality, boost memory, and enhance cognitive performance.
The peptide hormone Somatocrinin has a synthetic analog called peptide CJC-1295. It has also been suggested to stimulate the growth hormone-releasing hormone receptor, increasing GH production [iv]. Their primary proposed function is to induce pulsatile production of growth hormone. Excessive growth hormone production seems to be prevented due to the presence of a negative feedback system that controls this process. In addition, there is some speculation that CJC-1295 may have anti-aging properties [v]. Mice given the compound every 48 and 72 hours grew much larger and longer than their counterparts given a placebo, as reported by Alba et al. It may also play a role in cellular regeneration and repair.
Further, researchers report that they tested CJC-1295’s efficacy in reversing growth retardation in a mouse model of GHRH gene ablation (GHRHKO). A favorable growth response may have occurred in the CJC-1295 group since they seemed to have normal body weight and length. The effects of CJC-1295 on bone length and body composition were examined, and lean mass and subcutaneous fat mass seemed unaffected. The data also suggested an uptick in total pituitary RNA and GH mRNA levels, suggesting that CJC-1295 might have been responsible for these effects.
Ipamorelin Peptide and Gastrointestinal Studies
Ipamorelin’s possible activation of ghrelin receptors may be responsible for its stimulatory potential on stomach function. In one study, scientists looked at the possible processes by which Ipamorelin seems to speed up stomach emptying. The amount of radioactivity still present in the stomach 15 minutes after an intragastric gavage was used to calculate the gastric emptying rate. The researchers suggested that a significant portion of the meal may have been left in the stomach of the vehicle control group due to a delay in gastric emptying, which might have been induced by abdominal surgery.
In contrast to the vehicle control group, the Ipamorelin group suggested a statistically significant increase in stomach emptying time. This data suggests that Ipamorelin may be able to increase the rate at which the stomach is emptied. The potential effects of Ipamorelin on acetylcholine- and electrical-field-induced contractions in stomach smooth muscle were next evaluated. Gastric smooth muscle contractile responses to acetylcholine and electrical field stimulation were significantly attenuated, supporting the hypothesis that abdominal surgery and intestinal manipulation may cause this effect. However, the inhibition may have been alleviated when Ipamorelin and ghrelin were delivered together. This data suggests that Ipamorelin may enhance stomach contractility and counteract the procedures’ inhibiting effect. [vi]
Researchers speculate that the peptide’s probable role in digestion may also increase hunger and weight gain. One study suggests that Ipamorelin caused a weight gain of around 15% among the test subjects. It has been postulated that Ipamorelin may have contributed to an increase in relative body fat as measured by dual-energy X-ray absorptiometry (DEXA) by increasing the weights of fat pads concerning body weight. Serum leptin is a hormone thought to have a role in controlling energy balance and hunger, and Ipamorelin looked to boost its levels. Therefore, the researchers hypothesized the Ipamorelin groups could have eaten more. [vii]
CJC-1295 Peptide and the Pituitary
The pituitary cell GHRH receptor may target CJC-1295 since the compound may bind to certain locations on the receptor protein. This may cause structural modifications to the receptor, which might set in motion a cascade of molecular processes in the target cells and lead to the activation of signal transduction pathways. G-proteins, signaling proteins speculated to be located on the intracellular side of the GHRH receptor, may be activated by the binding-induced conformational changes. [viii]
Once engaged, these G-proteins might prompt the creation of secondary signaling molecules, including cyclic adenosine monophosphate (cAMP) or inositol pyrophosphate (IP3). Protein kinases, enzymes thought to be responsible for phosphorylating target proteins, may be activated by these second messengers, especially cAMP [ix]. Potentially, protein kinases control many biological functions. Protein kinase activation may result in the phosphorylation of transcription factors, proteins that may regulate gene expression. Transcriptional factors that have been phosphorylated may reach the nucleus and normalize the expression of genes involved in growth hormone production and secretion. Studies suggest that CJC-1295 binding may possibly set in motion a cascade of molecular processes that might lead, in the end, to the fusion of secretory vesicles carrying growth hormone with the plasma membrane. The union of these cells might lead to the release of growth hormone beyond the pituitary, where it could then exercise its biological effects. [x]
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References
[i] 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.
[ii] 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.
[iii] Venkova K, Mann W, Nelson R, Greenwood-Van Meerveld B. Efficacy of ipamorelin, a novel ghrelin mimetic, in a rodent model of postoperative ileus. J Pharmacol Exp Ther. 2009 Jun;329(3):1110-6. doi: 10.1124/jpet.108.149211. Epub 2009 Mar 16. PMID: 19289567.
[iv] Teichman SL, Neale A, Lawrence B, Gagnon C, Castaigne JP, Frohman LA. Prolonged stimulation of growth hormone (GH) and insulin-like growth factor I secretion by CJC-1295, a long-acting analog of GH-releasing hormone, in healthy adults. J Clin Endocrinol Metab. 2006 Mar;91(3):799-805. doi: 10.1210/jc.2005-1536. Epub 2005 Dec 13. PMID: 16352683.
[v] Alba M, Fintini D, Sagazio A, Lawrence B, Castaigne JP, Frohman LA, Salvatori R. Once-daily administration of CJC-1295, a long-acting growth hormone-releasing hormone (GHRH) analog, normalizes growth in the GHRH knockout mouse. Am J Physiol Endocrinol Metab. 2006 Dec;291(6):E1290-4. doi: 10.1152/ajpendo.00201.2006. Epub 2006 Jul 5. PMID: 16822960.
[vi] Greenwood-Van Meerveld, B., Tyler, K., Mohammadi, E., & Pietra, C. (2012). Efficacy of ipamorelin, a ghrelin mimetic, on gastric dysmotility in a rodent model of postoperative ileus. Journal of experimental pharmacology, 4, 149–155. https://doi.org/10.2147/JEP.S35396
[vii] Lall, S., Tung, L. Y., Ohlsson, C., Jansson, J. O., & Dickson, S. L. (2001). Growth hormone (GH)-independent stimulation of adiposity by GH secretagogues. Biochemical and biophysical research communications, 280(1), 132–138. https://doi.org/10.1006/bbrc.2000.4065
[viii] Martin, B., Lopez de Maturana, R., Brenneman, R., Walent, T., Mattson, M. P., & Maudsley, S. (2005). Class II G protein-coupled receptors and their ligands in neuronal function and protection. Neuromolecular medicine, 7(1-2), 3–36. https://doi.org/10.1385/nmm:7:1-2:003
[ix] Newton, A. C., Bootman, M. D., & Scott, J. D. (2016). Second Messengers. Cold Spring Harbor perspectives in biology, 8(8), a005926. https://doi.org/10.1101/cshperspect.a005926
[x] Ionescu, M., & Frohman, L. A. (2006). Pulsatile secretion of growth hormone (GH) persists during continuous stimulation by CJC-1295, a long-acting GH-releasing hormone analog. The Journal of clinical endocrinology and metabolism, 91(12), 4792–4797. https://doi.org/10.1210/jc.2006-1702