Growth hormone secretagogue receptor (GHSR)

The Growth hormone secretagogue receptor (GHSR), commonly known as the ghrelin receptor, is a G protein-coupled receptor (GPCR) primarily expressed in the pituitary gland and hypothalamus, as well as in peripheral tissues like the gastrointestinal tract and pancreas (NIH, 2026; Wikipedia, 2024). It is the functional receptor for ghrelin, a peptide hormone often called the hunger hormone, and plays a central role in regulating energy homeostasis, appetite, and growth hormone secretion (NIH, 2020; NIH, 2024). Beyond its metabolic functions, GHSR is involved in modulating gastric motility, glucose metabolism, and reward-related behaviors in the central nervous system (NIH, 2010; NIH, 2015). Dysregulation of the ghrelin-GHSR pathway is associated with various conditions, including obesity, diabetic gastroparesis, and cancer-related cachexia (NIH, 2014; ResearchGate, 2018). Consequently, GHSR is a significant therapeutic target; agonists like anamorelin and relamorelin are developed to treat cachexia and gastroparesis, while antagonists and inverse agonists are explored for managing obesity and substance use disorders (NIH, 2020; PatSnap, 2024).

Other names

Ghrelin receptorGHS-RGHSR1aGrowth hormone secretagogue receptor type 1GH-releasing peptide receptor

Agonist, Antagonist, Inverse agonist