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Am J Physiol Endocrinol Metab 274: E38-E44, 1998;
0193-1849/98 $5.00
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Vol. 274, Issue 1, E38-E44, January 1998

Metabolic inhibition impairs ATP-sensitive K+ channel block by sulfonylurea in pancreatic beta -cells

Eri Mukai1, Hitoshi Ishida1, Seika Kato1, Yoshiyuki Tsuura1, Shimpei Fujimoto1, Ayako Ishida-Takahashi2, Minoru Horie2, Kinsuke Tsuda3, and Yutaka Seino1

Departments of 1 Metabolism and Clinical Nutrition and of 2 Internal Medicine, Faculty of Medicine, and 3 Faculty of Integrated Human Studies, Kyoto University, Kyoto 606, Japan

The effect of metabolic inhibition on the blocking of beta -cell ATP-sensitive K+ channels (KATP channels) by glibenclamide was investigated using a patch-clamp technique. Inhibition of KATP channels by glibenclamide was attenuated in the cell-attached mode under metabolic inhibition induced by 2,4-dinitrophenol. Under a low concentration (0.1 µM) of ATP applied in the inside-out mode, KATP channel activity was not fully abolished, even when a high dose of glibenclamide was applied, in contrast to the dose-dependent and complete KATP channel inhibition under 10 µM ATP. On the other hand, cibenzoline, a class Ia antiarrhythmic agent, inhibits KATP channel activity in a dose-dependent manner and completely blocks it, even under metabolic inhibition. In sulfonylurea receptor (SUR1)- and inward rectifier K+ channel (Kir6.2)-expressed proteins, cibenzoline binds directly to Kir6.2, unlike glibenclamide. Thus, KATP channel inhibition by glibenclamide is impaired under the condition of decreased intracellular ATP in pancreatic beta -cells, probably because of a defect in signal transmission between SUR1 and Kir6.2 downstream of the site of sulfonylurea binding to SUR1.

sulfonylurea receptor; glibenclamide; intracellular metabolism


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