What is the Origin of Ghrelin Receptor Agonists?

The term is derived from the endogenous hormone ghrelin, which was named based on its role as a "Growth Hormone-releasing peptide" (GHrelin). "Agonist" is a pharmacological term from the Greek agonistes (contestant), referring to a substance that initiates a physiological response when it binds to a receptor. Their relevance is central to the neuroendocrine regulation of the somatotropic axis.

What is the Mechanism of Ghrelin Receptor Agonists?

These agonists bind to the GHSR-1a receptor, which is a G-protein coupled receptor expressed in the hypothalamus, pituitary, and other tissues. Receptor activation initiates an intracellular signaling cascade, primarily leading to an increase in intracellular calcium concentration in somatotroph cells of the pituitary. This signal transduction culminates in the pulsatile secretion of Growth Hormone, which then exerts systemic anabolic and lipolytic effects through its mediator, Insulin-like Growth Factor 1 (IGF-1).

Ghrelin Receptor Agonists ∞ Area

Ghrelin Receptor Agonists

Meaning

Ghrelin receptor agonists are a class of compounds that bind to and activate the Ghrelin Receptor, also known as the Growth Hormone Secretagogue Receptor type 1a (GHSR-1a). These agents mimic the action of the endogenous hormone ghrelin, primarily stimulating the release of Growth Hormone (GH) from the anterior pituitary gland. Clinically, they are studied for their potential to enhance anabolic processes, stimulate appetite, and modulate body composition and energy balance.