The antidiabetic sulfonylurea glibenclamide is a potent blocker of the ATP-modulated K+ channel in insulin secreting cells.
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.
D000255:Adenosine Triphosphate / Q000378:metabolism*; D000818:Animals; D004594:Electrophysiology; D005905:Glyburide / Q000494:pharmacology*; D007328:Insulin / Q000378:metabolism*; D000078790:Insulin Secretion; D007340:Insulinoma / Q000378:metabolism; D007473:Ion Channels / Q000378:metabolism*; D007700:Kinetics; D010190:Pancreatic Neoplasms / Q000378:metabolism; D011188:Potassium / Q000378:metabolism*; D051381:Rats; D012413:Rubidium / Q000378:metabolism
D007328:Insulin; D007473:Ion Channels; D000255:Adenosine Triphosphate; D012413:Rubidium; D011188:Potassium; D005905:Glyburide