1. [Mechanisms of action of peroral antidiabetics. Sulfonylurea preparations block the ATP-dependent potassium channels].
- Author
-
Larsson O, Kindmark H, Bränström R, and Berggren PO
- Subjects
- Administration, Oral, History, 20th Century, Humans, Hypoglycemic Agents administration & dosage, Hypoglycemic Agents chemistry, Hypoglycemic Agents history, Models, Molecular, Molecular Structure, Sulfonylurea Compounds administration & dosage, Sulfonylurea Compounds chemistry, Sulfonylurea Compounds history, Adenosine Triphosphate physiology, Hypoglycemic Agents pharmacology, Potassium Channels drug effects, Sulfonylurea Compounds pharmacology
- Abstract
Although hypoglycaemic sulphonylureas have been used to treat non-insulin-dependent diabetes mellitus (NIDDM) for the past forty years, their mechanisms of action at the molecular level have only recently been elucidated. A combination of electrophysiological and molecular biological techniques showed the target of sulphonylureas to be a sulphonylurea receptor (SUR1) and potassium channel (Kir6.2) complex. Together, these two proteins form the ATP-dependent potassium (KATP) channel occurring in insulin-secreting cells. An increase in the blood glucose level triggers a chain of events in insulin-secreting cells and K(ATP) channel closure which is a prerequisite for insulin secretion. In NIDDM, however, an increase in blood glucose fails to close the K(ATP) channel satisfactorily, but this can be remedied by the administration of sulphonylureas.
- Published
- 1997