Research on Ipamorelin Peptide?
Growth Hormone Release: Research has shown that Ipamorelin, a potent growth hormone secretagogue (GHS), stimulates GH release by acting on GHRP-like receptors with high efficacy and selectivity. Unlike other GHSs, ipamorelin does not significantly affect ACTH or cortisol levels, even at high doses, ensuring targeted GH release (1).
Studies show that its potency and efficacy are comparable to those of GHRP-6 in both in vitro and in vivo models, making it a promising candidate for treating GH deficiencies without undesired hormonal side effects (2).
Body Composition and Metabolism: Research suggests that Ipamorelin positively impacts body composition and metabolism by stimulating GH release, which promotes lipolysis and reduces adipose tissue. Studies show that GH-induced lipolysis enhances fat breakdown, particularly in metabolically active adipocytes, while improving insulin sensitivity and reducing lipotoxicity (3).
In hypogonadal and eugonadal males, ipamorelin has shown potential to counteract fat gain and muscle atrophy, improving overall body composition. Its targeted effects make it a promising adjunct therapy for metabolic and hormonal imbalances (4).
Bone Density: Research has demonstrated that Ipamorelin enhances bone density by stimulating growth hormone (GH) release, promoting bone mineral content (BMC) and formation. Studies in rats show ipamorelin increases tibial and vertebral BMC, primarily through bone growth and increased dimensions, while maintaining volumetric bone mineral density (BMD) (5).
Additionally, ipamorelin counteracts glucocorticoid-induced bone loss, significantly boosting periosteal bone formation rates. These findings highlight ipamorelin’s potential to support bone health and combat catabolic effects on skeletal integrity (6).
Gastrointestinal Function: Research suggests that Ipamorelin regulates inflammation and improves bowel function by stimulating ghrelin receptors, enhancing gastrointestinal motility. Clinical trials show ipamorelin reduces time to first tolerated meal in postoperative ileus (POI) patients, though not significantly (7).
In rodent models, repetitive dosing of ipamorelin accelerates colonic transit, increases fecal output, and improves food intake and weight gain after surgery (8). These findings highlight ipamorelin’s potential to alleviate POI symptoms and support recovery of bowel function post-surgery.
Neurocognitive Potential: Research has demonstrated that Ipamorelin, a ghrelin receptor agonist, offers neuroprotective benefits by activating GHS-R1a and inhibiting apoptotic pathways. Studies in Parkinson’s disease models show ghrelin, via GHS-R1a activation, reduces dopaminergic neuron loss, microglial activation, and pro-inflammatory molecules like TNF-alpha and IL-1beta.
It also suppresses matrix metalloproteinase-3 (MMP-3) expression in stressed neurons, indirectly deactivating microglia. These effects highlight ipamorelin’s potential as a therapeutic agent for neurodegenerative diseases by protecting neurons and reducing inflammation (9).
References
(1) J Ishida, M Saitoh, N Ebner, J Springer, et al (2020) Growth hormone secretagogues: history, mechanism of action, and clinical development – JCSM Communications, Volume 3, Issue 1, January/June 2020, Pages 25-37.
(2) K Raun, B S Hansen, N L Johansen, H Thøgersen, et al (1998) Ipamorelin, the first selective growth hormone secretagogue – European Journal of Endocrinology, 1998 Nov, Volume 139 (Issue 5), Pages 552-61.
(3) J J Kopchick, D E Berryman, V Puri, K Y Lee, et al (2019) The effects of growth hormone on adipose tissue: old observations, new mechanisms – Nature Reviews Endocrinology, 2019 Nov 28, Volume 16 (Issue 3), Pages 135–146.
(4) D K Sinha, A Balasubramanian, A J Tatem, J Rivera-Mirabal, et al (2020) Beyond the androgen receptor: the role of growth hormone secretagogues in the modern management of body composition in hypogonadal males – Translational Andrology Urology, 2020 Mar, Volume 9 (Suppl 2), Pages S149–S159.
(5) J Svensson, S Lall, S L Dickson, B A Bengtsson, et al (2000) The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats – Journal of Endocrinology, 2000 Jun, Volume 165 (Issue 3), Pages 569-77.
(6) N.B. Andersen, K. Malmlöf, P.B. Johansen, T.T. Andreassen, et al (2001) The growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats – Growth Hormone & IGF Research, Volume 11, Issue 5, October 2001, Pages 266-272.
(7) D E Beck, W B Sweeney, and M D McCarter (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, 2014 Dec, Volume 29 (Issue 12), Pages 1527-34.
(8) K Venkova, W Mann, R Nelson et al (2009) Efficacy of Ipamorelin, a Novel Ghrelin Mimetic, in a Rodent Model of Postoperative Ileus – The Journal of Pharmacology and Experimental Therapeutics, Volume 329, Issue 3, June 2009, Pages 1110-1116.
(9) M Moon, H Geun Kim, L Hwang, J-H Seo, et al (2009) Neuroprotective effect of ghrelin in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine mouse model of Parkinson’s disease by blocking microglial activation – Neurotoxicity Research, 2009 May, 15 (Issue 4), Pages 332-47.