| Insulin secretion and its modulation by antiarrhythmic and sulfonylurea drugs. | |
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MedLine Citation:
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PMID: 9217874 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Cardiovascular drugs such as antiarrhythmic agents with Vaughan Williams class Ia action have been found to induce a sporadic hypoglycemia. Recent investigation has revealed that these drugs induce insulin secretion from pancreatic beta-cells by inhibiting ATP-sensitive K+ (KATP) channels in a manner similar to sulfonylurea drugs. The mechanism underlying block of KATP channels by antiarrhythmic drugs was different, however, from that of sulfonylureas: firstly, because binding of radioactive glibenclamide could not be inhibited by unlabelled antiarrhythmic agents, and vice versa; secondly, because the two compounds differ in the kinetics and sidedness of drug action-antiarrhythmic drugs act on the channel from the inner surface of the cell membrane, whereas glibenclamide binds through the intramembrane pathway; finally, it was shown that functional KATP channels in beta-cells are composed of two distinct molecules-a sulfonylurea receptor (SUR) and a channel pore-forming subunit, an inwardly-rectifying K channel with two transmembrane regions (Kir6.2). Antiarrhythmic drugs reversibly inhibit the K+ conductance displayed by the Kir6.1 (a putative KATP channel clone)-transfected NIH3T3 cells. Therefore they appear to interact directly with the pore-forming subunit, thereby inhibiting KATP channel currents and exerting an insulinotrophic effect. |
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Authors:
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M Horie; A Ishida-Takahashi; T Ai; T Nishimoto; Y Tsuura; H Ishida; Y Seino; S Sasayama |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't; Review |
Journal Detail:
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Title: Cardiovascular research Volume: 34 ISSN: 0008-6363 ISO Abbreviation: Cardiovasc. Res. Publication Date: 1997 Apr |
Date Detail:
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Created Date: 1997-08-11 Completed Date: 1997-08-11 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0077427 Medline TA: Cardiovasc Res Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 69-72 Citation Subset: IM |
Affiliation:
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Department of Cardiovascular Medicine, Kyoto University Graduate School of Medicine, Japan. horie@kuhp.kyoto-u.ac.jp |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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3T3 Cells ATP-Binding Cassette Transporters* Animals Anti-Arrhythmia Agents / pharmacology* Humans Hypoglycemic Agents / pharmacology* Insulin / secretion* Islets of Langerhans / drug effects, secretion* Mice Potassium Channels / drug effects* Potassium Channels, Inwardly Rectifying* Receptors, Drug / drug effects Sulfonylurea Compounds / pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/ATP-Binding Cassette Transporters; 0/Anti-Arrhythmia Agents; 0/Hypoglycemic Agents; 0/Potassium Channels; 0/Potassium Channels, Inwardly Rectifying; 0/Receptors, Drug; 0/Sulfonylurea Compounds; 0/sulfonylurea receptor; 11061-68-0/Insulin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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