| Opposite effects of tolbutamide and diazoxide on the ATP-dependent K+ channel in mouse pancreatic beta-cells. | |
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MedLine Citation:
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PMID: 2431383 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The influence of the antidiabetic sulphonylurea tolbutamide on K+ channels of mouse pancreatic beta-cells was investigated using different configurations of the patch clamp technique. The dominant channel in resting cells is a K+ channel with a single-channel conductance of 60 pS that is inhibited by intracellular ATP or, in intact cells, by stimulation with glucose. In isolated patches of beta-cells membrane, this channel was blocked by tolbutamide (0.1 mM) when applied to either the intracellular or extracellular side of the membrane. The dose-dependence of the tolbutamide-induced block was obtained from whole-cell experiments and revealed that 50% inhibition was attained at approximately 7 microM. In cell-attached patches low concentrations of glucose augmented the action of tolbutamide. Thus, the simultaneous presence of 5 mM glucose and 0.1 mM tolbutamide abolished channel activity and induced action potentials. These were not produced when either of these substances was added alone at these concentrations. The inhibitory action of tolbutamide or glucose on the K+ channel was counteracted by the hyperglycaemic sulphonamide diazoxide (0.4 mM). Tolbutamide (1 mM) did not affect Ca2+-dependent K+ channels. It is concluded that the hypo- and hyperglycaemic properties of tolbutamide and diazoxide reflect their ability to induce the closure or opening, respectively, of ATP-regulated K+ channels. |
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Authors:
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G Trube; P Rorsman; T Ohno-Shosaku |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Pflügers Archiv : European journal of physiology Volume: 407 ISSN: 0031-6768 ISO Abbreviation: Pflugers Arch. Publication Date: 1986 Nov |
Date Detail:
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Created Date: 1987-01-12 Completed Date: 1987-01-12 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0154720 Medline TA: Pflugers Arch Country: GERMANY, WEST |
Other Details:
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Languages: eng Pagination: 493-9 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Action Potentials Adenosine Triphosphate / metabolism* Animals Cells, Cultured Diazoxide / pharmacology* Glucose / pharmacology Glyburide / pharmacology Ion Channels / metabolism* Islets of Langerhans / drug effects, metabolism* Mice Potassium / metabolism* Tolbutamide / antagonists & inhibitors, pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Ion Channels; 10238-21-8/Glyburide; 364-98-7/Diazoxide; 50-99-7/Glucose; 56-65-5/Adenosine Triphosphate; 64-77-7/Tolbutamide; 7440-09-7/Potassium |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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