The mechanisms responsible for the stimulation of insulin release from the pancreatic β-cell by hypoglycemic sulfonylureas are reviewed herein. One hypothesis postulates that these agents act, at the level of the plasma membrane, by causing the closure of a class of K+ channels characterized by their sensitivity to ATP. This may lead to depolarization of the plasma membrane, gating of voltage-sensitive Ca2+ channels, increase in cytosolic Ca2+ activity, and activation of the effector system for insulin release. However, it is not evident that the closure of ATP-sensitive K+ channels accounts for effects of sulfonylureas such as inhibition of K+ inflow into the islet cells, increase in their Na+ content, or even stimulation of Ca2+ inflow and insulin release at physiological or higher concentrations of Dglucose.
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August 01 1990
Mechanisms of Sulfonylurea-lnduced Insulin Release
Willy J Malaisse, MD, PhD;
Willy J Malaisse, MD, PhD
Laboratories of Experimental Medicine and Pharmacology, Brussels Free University
Brussels, Belgium
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Philippe Lebrun, MD, PhD
Philippe Lebrun, MD, PhD
Laboratories of Experimental Medicine and Pharmacology, Brussels Free University
Brussels, Belgium
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Address correspondence and reprint requests to W.J. Malaisse, MD, PhD, Laboratory of Experimental Medicine, Brussels Free University, 115 Boulevard de Waterloo, B-1000 Brussels, Belgium
Citation
Willy J Malaisse, Philippe Lebrun; Mechanisms of Sulfonylurea-lnduced Insulin Release. Diabetes Care 1 August 1990; 13 (Supplement_3): 9–17. https://doi.org/10.2337/diacare.13.3.9
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