Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for its potential applications in research related to cachexia, gastroparesis, and gastric/intestinal dysmobility disorders [4] [5].
Human growth hormone-releasing factor stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary.Growth hormone-releasing hormone is a hormone produced in the hypothalamus. The main role of growth hormo
High affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). Blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
An endogenous ligand for the ghrelin receptor (GHS-R1a), produced by alternative splicing of the rat ghrelin gene. Potently induces Ca2+ release in cells expressing ghrelin receptors (EC50 = 2.4 nM) and stimulates GH release in vivo.
K-(D-1-Nal)-FwLL-NH2 TFA is a potent and high-affinity inverse agonist of the ghrelin receptor, exhibiting Ki values of 4.9 nM in COS7 cells and 31 nM in HEK293T cells. This compound effectively inhibits ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.