Glyburide

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).

Cell permeable: no

Primary Target
ATP-sensitive K+ channels

Product does not compete with ATP.

Reversible: no

Toxicity: Standard Handling (A)

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

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.

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