Background:

Avexitide (Exendin (9-39)) is a specific and competitive glucagon-like peptide-1 receptor antagonist.

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 in mice and humans. Avexitide (Exendin (9-39)) significantly inhibits amino acid-stimulated insulin secretion in pancreatic islets isolated from neonates with KATPHI[1].

Insulin-to-glucose ratios are significantly lower during Avexitide (Exendin (9-39)) infusion compared with vehicle[1]. Continuous subcutaneous infusion of Avexitide (Exendin (9-39)) significantly raises fasting blood glucose levels in SUR-1 ?/? mice without affecting glucose tolerance or insulin sensitivity[2].

参考文献:
[1]. Calabria AC, et al. GLP-1 receptor antagonist exendin-(9-39) elevates fasting blood glucose levels in congenital hyperinsulinism owing to inactivating mutations in the ATP-sensitive K+ channel. Diabetes. 2012 Oct;61(10):2585-91.
[2]. De León DD, et al. Exendin-(9-39) corrects fasting hypoglycemia in SUR-1-/- mice by lowering cAMP in pancreatic beta-cells and inhibiting insulin secretion. J Biol Chem. 2008 Sep 19;283(38):25786-93.