(Des-octanoyl)-Ghrelin Trifluoroacetate, Bachem
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Small synthetic molecules called growth-hormone secretagogues (GHSs) stimulate the release of growth hormone (GH) from the pituitary through a G protein-coupled receptor (GHS-R). Recently, ghrelin ("ghre" is the Proto-Indo-European root of the word "grow") has been identified as an endogenous ligand for GHS-R. These peptides consist of 28 amino acids with an octanoyl-residue at Ser³, which is essential for expressing activity. Ghrelin stimulates GH release from rat primary culture pituitary cells in a dose-dependent manner and induces an increase in intracellular Ca²⁺ in GHS-R-expressing cells with an EC₅₀ value of 2.5 nM. Human ghrelin is homologous to rat ghrelin apart from two amino acids. The occurrence of ghrelin in both rat and human indicates that GH release from the pituitary may be regulated not only by hypothalamic GHRH, but also by ghrelin. In future, ghrelin might be used in the treatment of aging patients as well as in patients with idiopathic GH deficiency, obesity, osteoporosis or cardiovascular diseases.
Most circulating ghrelin is des-octanoyl ghrelin. The non-acylated ghrelin was considered inactive at first, though biological activities such as stimulation of adipogenesis and control of cell growth could be demonstrated more recently. Both ghrelin and the more abundant endogenous form des-octanoyl ghrelin could play a role in the paracrine regulation of vascular tone in humans.
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