Glucagon Receptor Antagonists Small Molecules and Peptides

The glucagon receptor is a member of the glucagon receptor family that also includes GLP-1, GLP-2, secretin, GHRH and GIP receptors. The glucagon receptor regulates blood glucose levels via control of hepatic glycogenolysis and gluconeogenesis, and via regulation of insulin release from the β-cells of pancreatic islets.

The glucagon receptor is predominantly expressed in the pancreas, liver and kidneys, but is also found to a lesser extent in the heart, adipose tissue, spleen, thymus and adrenal glands. The human glucagon receptor gene is localized on chromosome 17q25.