The Sound of Evolution
Nateglinide
Mechanism of action:
Nateglinide is a benzoic acid derivative. Nateglinide binds to and inhibits sulfonylurea receptor 1 (SUR1) on the membrane of pancreatic β cells. This receptor is the regulatory subunit of the ATP-sensitive potassium channel. When inhibited by nateglinide, potassium efflux decreases and the cell membrane undergoes depolarization. This depolarization opens calcium channels, increases calcium influx, and stimulates insulin release.
Reference(s):
1. Hu S et al. (2000). Pancreatic beta-cell K(ATP) channel activity and membrane-binding studies with nateglinide: A comparison with sulfonylureas and repaglinide. J Pharmacol Exp Ther.
2. Sunaga Y et al. (2001). The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide. Eur J Pharmacol.