Glucagon
Overview
The principal counter-regulatory hormone to insulin, secreted by pancreatic α-cells. Used clinically for severe hypoglycemia and as a smooth-muscle relaxant in radiologic procedures. Increasingly studied as a component of multi-receptor incretin agonists.
Research profile · for clinicians
Based on research: the counter-regulatory hormone to insulin, with established emergency use in severe hypoglycemia. Increasingly studied as a component of dual and triple incretin co-agonists (retatrutide, survodutide) for its effects on energy expenditure and hepatic fat oxidation.
Mechanism of action
GCGR agonism activates hepatic adenylyl cyclase, driving glycogenolysis and gluconeogenesis. At higher exposures, also increases energy expenditure and hepatic fatty-acid oxidation — the rationale for its inclusion in retatrutide and survodutide.
Research record
- [01]Emergency hypoglycemia management — standard clinical use.
- [02]Glucagon-receptor agonism in dual/triple incretin co-agonists (survodutide, retatrutide).
Selected references
Glucagon receptor as a drug target
Mol. Metab., 2019