Sermorelin is a 29-residue N-terminal analog of growth hormone-releasing hormone (GHRH) that retains the ability to stimulate growth hormone (GH) release.1 Sermorelin (1 μg/kg, i.v.) increases serum GH levels in rats by approximately 17% compared with saline control after 15 minutes.2 It also increases GH release in pigs when administered at a dose of 250 ng/kg.3 Sermorelin (1 μM) increases proliferation of NCI-H727 human bronchial carcinoid cells by 30% and increases vascular endothelial growth factor (VEGF) secretion.4 It increases phosphorylation of focal adhesion kinase (FAK) and expression of VEGF in A549 lung cancer cells when used at a concentration of 0.1 μM.5 Formulations containing sermorelin have been used to diagnose and treat growth hormone deficiency.
1.Rivier, J., Spiess, J., Thorner, M., et al.Characterization of a growth hormone-releasing factor from a human pancreatic islet tumourNature300(5889)276-278(1982) 2.Izdebski, J., Pinski, J., Horvath, J.E., et al.Synthesis and biological evaluation of superactive agonists of growth hormone-releasing hormoneProc. Natl. Acad. Sci. USA92(11)4872-4876(1995) 3.Lance, V.A., Murphy, W.A., Sueiras-Diaz, J., et al.Super-active analogs of growth hormone-releasing factor (1-29)-amideBiochem. Bioph. Res. Commun.119(1)265-272(1984) 4.Stepie, T., Sacewicz, M., Lawnicka, H., et al.Stimulatory effect of growth hormone-releasing hormone (GHRH(1-29)NH2) on the proliferation, VEGF and chromogranin A secretion by human neuroendocrine tumor cell line NCI-H727 in vitroNeuropeptides43(5)397-400(2009) 5.Siejka, A., Barabutis, N., and Schally, A.V.GHRH antagonist inhibits focal adhesion kinase (FAK) and decreases expression of vascular endothelial growth factor (VEGF) in human lung cancer cells in vitroPeptides37(1)63-68(2012)