Description
Exendin-3 (9-39) amide is a truncated form of the exendin-4 peptide that acts as a potent competitive antagonist for the glucagon-like peptide 1 receptor (GLP-1R; K
d = 1.7 nM in CHL cells transfected with cloned human GLP-1). It inhibits exendin-3-induced increases in cAMP levels in guinea pig pancreas cells (IC
50 = 20 nM). Exendin-3 (9-39) amide administration in the hypothalamus (10 and 100 μg, i.c.v.) reverses GLP-1 inhibition of feeding behavior in rats.
Uses
Exendin-3 (9-39) is a potent and selective GLP-1 receptor antagonist.
General Description
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. It also prevents the production of cAMP by GIP. GLP-1, along with GIP, acts as a physiological incretin.
Biochem/physiol Actions
GLP-1 (glucagon-like peptide-1) receptor antagonist. Competitive inhibitor of exendin-3 and exendin-4.