The antidiabetic sulfonylurea glibenclamide is a potent blocker of the ATP-modulated K+ channel in insulin secreting cells

Biochem Biophys Res Commun. 1987 Jul 15;146(1):21-5. doi: 10.1016/0006-291x(87)90684-x.

Abstract

The ATP-sensitive K+ channel of RINm5F insulinoma cells is activated after an intracellular ATP depletion. This activation can be followed by 86Rb+ efflux. Once activated by ATP depletion, the K+ channel can be blocked by the hypoglycemic drug, glibenclamide. The blockade is of a high-affinity type (K0.5 = 0.06 nM). Recording of the activity of ATP-sensitive K+ channels with the patch-clamp technique confirmed that they could be completely blocked with 20 nM glibenclamide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / metabolism*
  • Animals
  • Electrophysiology
  • Glyburide / pharmacology*
  • Insulin / metabolism*
  • Insulin Secretion
  • Insulinoma / metabolism
  • Ion Channels / metabolism*
  • Kinetics
  • Pancreatic Neoplasms / metabolism
  • Potassium / metabolism*
  • Rats
  • Rubidium / metabolism

Substances

  • Insulin
  • Ion Channels
  • Adenosine Triphosphate
  • Rubidium
  • Potassium
  • Glyburide