Exendin Fragment 9-39 is an antagonist of glucagon-like peptide-1 (GLP-1) receptor, and also acts as an inhibitor of glucosedependent insulinotropic polypeptide (GIP)-receptor binding.
Glucagon-like peptide-1 (GLP-1) is a product of proglucagon cleavage synthesized in L cells in the intestinal mucosa, α-cells in the pancreatic islet, and neurons in the nucleus of the solitary tract. GLP-1 is released in response to nutrient absorption in the gut and helps to stimulate insulin secretion in the pancreaticb-cells while also suppressing glucagonsecretion[1]. GLP-1 plays a role in the control of fasting glucose. Avexitide (Exendin (9-39)), a truncated form of the GLP-1 agonist exendin-4, is a specific GLP-1 receptor antagonist. Exendin-(9-39) prevents hypoglycemia and maintains stability of blood glucose during a prolonged fast in individuals with KATPHI.[2]. It is an antagonist of the action of GLP-1(7-36) amide on arterial blood pressure and heart rate of rats. (3000ng of exendin 3-39 and 10ng of GLP-1 (7-36) amide)[3]. It inhibits exendin-3-induced increases in cAMP levels in guinea pig pancreas cells (IC50 = 20 nM)[4].
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