The oral hypoglycemic agent, U-56324, inhibits the activity of ATP-sensitive potassium channels in cell-free membrane patches from cultured mouse pancreatic B-cells.
U-56324, a hypoglycemic agent derived from nicotinic acid, inhibited the activity of ATP-sensitive potassium channels in excised patches from mouse pancreatic B-cells. The effect of U-56324 on channel activity was reversible and concentration-dependent while it had no effect on single channel conductance. The positional isomer, U-59588, which has relatively little hypoglycemic activity, had no effect on channel properties. U-56324, at the same concentrations, had no effect on calcium-activated potassium channels. The basis for the potentially antidiabetic properties of U-56324 may therefore be due to direct and specific inhibition of ATP-sensitive potassium channels.
Hopkins
W F
WF
Department of Physiology and Biophysics, University of Washington School of Medicine, Seattle.
Fatherazi
S
S
Cook
D L
DL
D000255:Adenosine Triphosphate / Q000502:physiology; D000818:Animals; D002462:Cell Membrane / Q000502:physiology; D002474:Cell-Free System; D002478:Cells, Cultured; D004553:Electric Conductivity; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D066298:In Vitro Techniques; D007515:Islets of Langerhans / Q000378:metabolism*; D051379:Mice; D009539:Nicotinic Acids / Q000494:pharmacology*; D011188:Potassium / Q000502:physiology; D015221:Potassium Channels / Q000187:drug effects*; D013329:Structure-Activity Relationship
D007004:Hypoglycemic Agents; D009539:Nicotinic Acids; D015221:Potassium Channels; C054138:U 56324; D000255:Adenosine Triphosphate; D011188:Potassium