| Staurosporine inhibits the effects of leukotrienes C4 and D4 in isolated guinea pig heart and trachea. | |
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MedLine Citation:
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PMID: 8577209 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Isolated hearts from guinea pigs were perfused at 37 degrees C with Tyrode's solution according to the technique of Langendorff. Coronary flow, left ventricular pressure amplitude and heart rate were measured. Bolus injection of 30 ng leukotriene C4 caused a long-lasting decrease in coronary flow and left ventricular pressure amplitude while heart rate was not affected. A similar but shorter lasting effect was induced by 100 ng leukotriene D4. The effects of the leukotrienes were completely blocked by 1 microM staurosporine. Staurosporine at concentrations of 100 and 10 nM, in contrast to 1 microM, influenced basic cardiac function slightly or not at all, but antagonized the effects of 30 ng leukotriene C4. In isolated tracheal muscle preparations, leukotriene C4 and D4 induced concentration-dependent contractures. Staurosporine at concentrations of 25-100 nM antagonized the effects of leukotriene C4 and D4 in a noncompetitive manner with inhibitor constants of 47.6 and 75.9 nM, respectively. The results indicate that staurosporine is a potent noncompetitive antagonist of the effects of leukotriene C4 and D4 in smooth muscle. |
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Authors:
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S Schäfer; A Walland |
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Publication Detail:
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Type: In Vitro; Journal Article |
Journal Detail:
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Title: Methods and findings in experimental and clinical pharmacology Volume: 17 ISSN: 0379-0355 ISO Abbreviation: Methods Find Exp Clin Pharmacol Publication Date: 1995 Sep |
Date Detail:
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Created Date: 1996-03-12 Completed Date: 1996-03-12 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 7909595 Medline TA: Methods Find Exp Clin Pharmacol Country: SPAIN |
Other Details:
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Languages: eng Pagination: 469-76 Citation Subset: IM |
Affiliation:
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Department of Pharmacology, Boehringer Ingelheim KG, Ingelheim, Germany. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Alkaloids
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metabolism,
pharmacology* Animals Coronary Circulation / drug effects Enzyme Inhibitors / pharmacology* Female Guinea Pigs Heart / drug effects* Heart Rate / drug effects Leukotriene C4 / antagonists & inhibitors*, pharmacology Leukotriene D4 / antagonists & inhibitors*, pharmacology Male Muscle, Smooth / drug effects Muscle, Smooth, Vascular / drug effects Staurosporine Trachea / drug effects* Ventricular Function, Left / drug effects |
| Chemical | |
Reg. No./Substance:
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0/Alkaloids; 0/Enzyme Inhibitors; 62996-74-1/Staurosporine; 72025-60-6/Leukotriene C4; 73836-78-9/Leukotriene D4 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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