GLP-1 receptor
Category: Receptors · Last updated
The Glucagon-Like Peptide 1 receptor (GLP-1R) is a class-B Gαs-coupled G-protein-coupled receptor expressed on pancreatic β-cells, hypothalamic and brainstem neurons, gastric smooth muscle, and other tissues. Its endogenous ligand is GLP-1, a 30/31-amino-acid incretin peptide secreted by intestinal L-cells in response to nutrient intake.
Signaling
GLP-1R agonism activates adenylate cyclase → cAMP → PKA + EPAC2. The net effects:
- Glucose-dependent insulin secretion from pancreatic β-cells
- Suppressed glucagon release from α-cells (above the hypoglycemic threshold)
- Delayed gastric emptying
- Central appetite suppression via brainstem and hypothalamic GLP-1R
Relevance to research peptides
- Semaglutide · once-weekly GLP-1R agonist (Ozempic / Wegovy / Rybelsus)
- Liraglutide · once-daily GLP-1R agonist (Victoza / Saxenda)
- Tirzepatide · dual GLP-1R / GIP-R agonist
- Retatrutide · triple GLP-1R / GIPR / GCGR agonist