| Protein kinase C inhibitors suppress disc-sphere changes of human platelets, as assessed with the shape-change parameter. | |
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MedLine Citation:
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PMID: 8508906 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Changes in the shape of human platelets and the biochemical mechanism responsible were evaluated, using the shape-change parameter. Neither the Na+/H+ exchanger, nor intracellular or extracellular calcium ions (Ca2+) affected disc-sphere changes induced by low doses of thrombin. Treatment with inhibitors of Ca2+ mobilization, calmodulin or mysoin light-chain kinase had no significant effect on the shape change of platelets. Staurosporine and H-7, both of which are inhibitors of protein kinase C, inhibited disc-sphere changes at low concentrations. Moreover, calphostin C, a specific inhibitor of protein kinase C, effectively inhibited thrombin-induced shape change, as assessed by the shape-change parameter, in a dose-dependent manner. 1-Oleoyl-2-acetyl-glycerol and 1,2-dioctanoyl-glycerol, which are synthetic protein kinase C activators, induced shape changes similar to those induced by thrombin. A decrease in the surface area of platelet images on scanning electron micrographs was used to quantify the disc-sphere transformation. The mean platelet areas was significantly decreased after stimulation with thrombin or 1-oleoyl-2-acetyl-glycerol. Pretreatment with H-7 inhibited the thrombin-induced disc-sphere change, as assessed by changes in the platelet surface area. Our results obtained with various inhibitors suggest that thrombin-induced platelet change, as assessed by the shape-change parameter, are associated with activation of protein kinase C. |
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Authors:
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Y Ozaki; Y Jinnai; Y Yatomi; S Kume |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: European journal of pharmacology Volume: 235 ISSN: 0014-2999 ISO Abbreviation: Eur. J. Pharmacol. Publication Date: 1993 Apr |
Date Detail:
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Created Date: 1993-07-13 Completed Date: 1993-07-13 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 1254354 Medline TA: Eur J Pharmacol Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 255-65 Citation Subset: IM |
Affiliation:
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Department of Clinical and Laboratory Medicine, Yamanashi Medical College, Japan. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine Blood Platelets / cytology, drug effects* Calcium / metabolism Calcium Channel Blockers / pharmacology Calmodulin / antagonists & inhibitors Cell Size / drug effects, physiology Fura-2 / pharmacology Humans Ion Transport / drug effects Isoquinolines / pharmacology Microscopy, Electron, Scanning Piperazines / pharmacology Platelet Aggregation / drug effects Protein Kinase C / antagonists & inhibitors*, pharmacology Sodium / metabolism Thrombin / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Calcium Channel Blockers; 0/Calmodulin; 0/Isoquinolines; 0/Piperazines; 7440-23-5/Sodium; 7440-70-2/Calcium; 84477-87-2/1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; 96314-98-6/Fura-2; EC 2.7.11.13/Protein Kinase C; EC 3.4.21.5/Thrombin |
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