GLP-1 Receptor (Glucagon-Like Peptide-1 Receptor)
The GLP-1 receptor is a G protein–coupled receptor (GPCR) primarily expressed on pancreatic beta cells, but also found in the brain, heart, gastrointestinal tract, and kidneys.
Physiological Role
GLP-1 receptors are activated by glucagon-like peptide-1 (GLP-1), an incretin hormone secreted by the intestinal L-cells in response to food intake.
Key Actions
Stimulates insulin secretion (glucose-dependent)
Inhibits glucagon release
Delays gastric emptying
Reduces appetite via central nervous system pathways
Enhances beta-cell survival and function
Therapeutic Relevance
GLP-1 Receptor Agonists (GLP-1 RAs)
Synthetic agents that mimic the action of endogenous GLP-1 by binding and activating the GLP-1 receptor. Common drugs include:
Semaglutide (Ozempic®, Wegovy®)
Liraglutide (Victoza®, Saxenda®)
Dulaglutide (Trulicity®)
Exenatide (Byetta®, Bydureon®)
Clinical Uses
Type 2 Diabetes Mellitus
Obesity and weight management
Cardiovascular risk reduction (certain agents)
Investigational uses: Alzheimer’s disease, Idiopathic Intracranial Hypertension (IIH), Parkinson’s disease
Central Nervous System Effects
GLP-1 receptors in the brain (especially hypothalamus and brainstem) influence:
Satiety and food intake regulation
Reward and addiction circuits
Neuroinflammation and neurodegenerative processes
References
Nauck MA, Meier JJ. “Incretin hormones: Their role in health and disease.” Diabetes Obes Metab. 2018.
Drucker DJ. “Mechanisms of Action and Therapeutic Application of GLP-1.” Cell Metab. 2018.