What is the Origin of GHS Receptor Agonism?

This precise term originates from molecular pharmacology and endocrinology, following the discovery of ghrelin, the endogenous ligand for the GHSR. The etymology combines the acronym GHS (Growth Hormone Secretagogue) with the clinical term 'receptor agonism,' which describes the activation of a receptor by a binding molecule. The concept has been instrumental in developing new classes of compounds for age-related GH deficiency.

What is the Mechanism of GHS Receptor Agonism?

The GHS receptor is predominantly expressed in the hypothalamus and pituitary gland. Upon agonist binding, the receptor undergoes a conformational change, activating intracellular G-proteins and subsequent signaling pathways, primarily the phospholipase C pathway. This cascade ultimately increases intracellular calcium concentration in somatotroph cells, triggering the fusion of GH-containing vesicles with the cell membrane and the pulsatile release of growth hormone into the systemic circulation.

GHS Receptor Agonism

Meaning

The pharmacological action of a substance that selectively binds to and activates the Growth Hormone Secretagogue (GHS) receptor, also known as the ghrelin receptor (GHSR-1a). This agonistic action initiates a signaling cascade that potently stimulates the release of endogenous growth hormone (GH) from the pituitary gland. GHS receptor agonism is a therapeutic strategy employed to increase systemic GH and Insulin-like Growth Factor 1 (IGF-1) levels, promoting anabolism, tissue repair, and metabolic balance.