Mouse;Rat (Des-octanoyl)-Ghrelin Trifluoroacetate

Supplier: BACHEM AMERICAS INC

4049310.0500 4049310.1000

H-6264.0500BAEA 722.85 CAD

H-6264.0500BA H-6264.1000BA

Mouse;Rat (Des-octanoyl)-Ghrelin Trifluoroacetate

Proteins and Peptides

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.

In contrast to the octanoylated peptide, the non-acylated ghrelin does not activate growth hormone secretagogue receptor-expressing cells. The peptide decreases food intake and gastroduodenal motility in conscious rats, probably by crossing the blood-brain barrier and activating the brain receptor directly.

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