Hexarelin is an appetite-regulating factor secreted from peripheral organs that is involved in regulation of energy homoeostasis via binding to the receptor resulting in the secretion of by the pituitary gland. The pathway activated by binding of Hexarelin to the secretagogue receptor, GHSR1a, regulates the activation of the downstream mitogen-activated protein kinase, Akt, nitric oxide synthase, and AMPK cascades in different cellular systems.
One of the important features of GHSR1a displays constitutive activity possessing basal activity in the absence of an agonist, resulting in a high degree of receptor internalization as well as of signaling activity.Inverse agonists for the Hexarelin receptor could be particularly interesting for the treatment of obesity.This activity seems to provide a tonic signal required for the development of normal height, probably through an effect on the GH axis.
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