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.