Explore studies of ipamorelin.
Sequential backbone modifications of ipamorelin produced smaller peptidomimetic compounds that retained potent GH secretagogue activity, advancing the goal of orally active GH-releasing peptides.
Ankersen, M; Johansen, N L; Madsen, K; Hansen, B S; Raun, K; Nielsen, K K; Thogersen, H; Hansen, T K; Peschke, B; Lau, J; Lundt, B F; Andersen, P H · In Vitro
Ipamorelin demonstrated approximately 20% nasal bioavailability in rats, superior to GHRP-2, GHRP-6, and two other peptides, supporting its potential for non-invasive nasal delivery.
Johansen, P B; Hansen, K T; Andersen, J V; Johansen, N L · Animal Study
Ipamorelin released GH with potency similar to GHRP-6 but did not increase ACTH, cortisol, prolactin, or FSH even at doses 200-fold higher than effective GH-releasing doses, making it the first truly selective GH secretagogue.
Raun, K; Hansen, B S; Johansen, N L; Thøgersen, H; Madsen, K; Ankersen, M; Andersen, P H · Clinical Trial
Ipamorelin (18-450 μg/day SC, three daily injections for 15 days) increased longitudinal bone growth rate and body weight dose-dependently in rats, with sustained GH release throughout the treatment period.
Johansen, P B; Nowak, J; Skjaerbaek, C; Flyvbjerg, A; Andreassen, T T; Wilken, M; Orskov, H · Animal Study
Ipamorelin maintained GH-releasing activity during 8 days of methylprednisolone treatment in rats and partially preserved longitudinal bone growth over 15 days despite glucocorticoid-induced growth suppression.
Malmlöf, K; Johansen, P B; Haahr, P M; Wilken, M; Oxlund, H · Animal Study
GHRP-6 and the oral GHS NN703 concentrated in rat gastric tissue containing ghrelin-producing cells, suggesting GH secretagogues may act partly by stimulating endogenous ghrelin release as a secondary mechanism.
Ahnfelt-Rønne, I; Nowak, J; Olsen, U B · Animal Study
Three months of ipamorelin (SC injection) counteracted methylprednisolone-induced decreases in bone formation rate, bone mineral content, and partially preserved skeletal muscle mass in adult female rats.
Andersen, N B; Malmlöf, K; Johansen, P B; Andreassen, T T; Ørtoft, G; Oxlund, H · Animal Study
NN703-ipamorelin hybrid GH secretagogues showed low nanomolar in vitro potency in pituitary cell assays and effective GH release in pigs in vivo, validating the hybrid design approach.
Hansen, T K; Ankersen, M; Raun, K; Hansen, B S · In Vitro
Chronic ipamorelin treatment maintained somatotroph GH-releasing responsiveness without desensitization, though GHRH and somatostatin receptor expression were modulated — adaptive changes that preserved overall drug effectiveness.
Jiménez-Reina, L; Cañete, R; de la Torre, M J; Bernal, G · Animal Study
Ipamorelin improved nitrogen balance and reduced urea synthesis in dexamethasone-treated rats comparably to GH injection, demonstrating GH secretagogue equivalence to direct GH for counteracting steroid-induced protein catabolism.
Aagaard, Niels Kristian; Grøfte, Thorbjørn; Greisen, Jacob; Malmlöf, Kjell; Johansen, Peter B; Grønbaek, Henning; Ørskov, Hans; Tygstrup, Niels; Vilstrup, Hendrik · Animal Study
Discovered a putative β-arrestin-biased GHSR superagonist through dual screening (calcium antagonism + ERK1/2 phosphorylation). Activity not completely blocked by competitive antagonist, suggesting allosteric binding mechanism.
Karaki, Fumika; Oki, Tomoya; Sakao, Yuma; Sato, Noriko; Hirayama, Shigeto; Miyano, Kanako; Uezono, Yasuhito; Fujii, Hideaki · In Vitro