GLP-1R
G-protein-coupled receptor for GLP-1; molecular target of incretin-class metabolic peptides.
For laboratory and research use only — not for human consumption.
The glucagon-like peptide-1 receptor (GLP-1R) is a 463-amino-acid class B G-protein-coupled receptor expressed on pancreatic β-cells, central and peripheral neurons, gastrointestinal mucosa, and other tissues. Ligand binding activates Gαs, raising intracellular cAMP and triggering glucose-dependent insulin secretion in β-cells, suppression of glucagon release from α-cells, slowed gastric emptying, and central appetite suppression via the hypothalamic arcuate nucleus and brainstem area postrema. GLP-1R is the principal molecular target of the explosive class of incretin-mimetic peptide drugs that includes semaglutide (Ozempic, Wegovy), liraglutide, exenatide, dulaglutide, and the dual-agonist tirzepatide (which engages both GLP-1R and GIPR) and emerging triple-agonist retatrutide (GLP-1R/GIPR/glucagon receptor). Receptor desensitisation via β-arrestin-mediated internalisation is one mechanism limiting maximum efficacy and is partly addressed by biased agonists. GLP-1R is mechanistically distinct from the GH-axis receptors (GHRHR, GHSR) and from healing-peptide receptors (FPR2, VEGFR2). Its inclusion in this glossary reflects the prominence of GLP-1R agonist research in the modern peptide-research landscape.