Glyburide

Biochem/physiol Actions

Cell permeable: no

Reversible: no

Product does not compete with ATP.

Primary TargetATP-sensitive K+ channels

General description

A sulfonylurea that selectively blocks ATP-sensitive K⁺ channels. Reduced K⁺ conductance causes membrane depolarization and influx of Ca²⁺ through voltage sensitive Ca²⁺ channels. Blocks vascular smooth muscle relaxation produced by K_ATP channel openers. Inhibits the vasorelaxing effects of nitric oxide.

Antidiabetic sulfonylurea that selectively blocks ATP-sensitive K⁺ channels. Reduced K⁺ conductance causes membrane depolarization and influx of Ca²⁺ through voltage sensitive Ca²⁺ channels. Blocks vascular smooth muscle relaxation produced by K_ATP channel openers. High-affinity binding sites are widely distributed and have been identified in the cardiovascular system, the central nervous system, and pancreatic β-cells. In cultured cells, glyburide enhances insulin action and stimulates the synthesis of glucose transporters. Displays large potency difference in action on pancreatic tissue (IC₅₀ in nM range) and vascular tissue (IC₅₀ in µM range).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Holzmann, S., et al. 1992. Eur. J. Pharmacol.215, 1.Rabuazzo, A.M., et al. 1992. Endocrinology131, 1815.Miller, J.A., et al. 1991. J. Pharmacol. Exp. Ther.256, 358.Jacobs, D.R., et al. 1989. Diabetes 38, 205.

Packaging

1 g in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)