| Flufenamic and tolfenamic acids inhibit calcium influx in human polymorphonuclear leukocytes. | |
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MedLine Citation:
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PMID: 7746266 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Fenamates, a subgroup of nonsteroidal anti-inflammatory drugs, inhibit several functions of human polymorphonuclear leukocytes (PMNs) in vitro, by a thus far unknown mechanism. To determine the mechanism behind this action, we studied the effects of two fenamates (flufenamic and tolfenamic acids) on Ca2+ metabolism in human PMNs. The two fenamates inhibited the increases in intracellular free calcium concentration induced by either the chemotactic peptide N-formyl-L-methionyl-L-leucyl-L-phenylalanine or the calcium ionophore A23187 in fura-2-labeled PMNs. This inhibition was concluded to be due to blocking of the cation influx, as evidenced by measurement of Mn2+ influx and the influx of radioactive calcium. In addition, the actions of flufenamic and tolfenamic acids were similar to those of an experimental blocker of nonselective cation channels (SK&F 96365). The two other control compounds, an antagonist of voltage-dependent calcium channels (nifedipine) and an inhibitor of prostanoid synthesis (ketoprofen), were ineffective. In conclusion, inhibition of calcium influx in PMNs is introduced as a novel prostanoid-independent mode of action of two nonsteroidal anti-inflammatory drugs with fenamate structure, flufenamic and tolfenamic acids, which could explain their earlier documented inhibitory effects on PMN functions. |
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Authors:
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H Kankaanranta; E Moilanen |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Molecular pharmacology Volume: 47 ISSN: 0026-895X ISO Abbreviation: Mol. Pharmacol. Publication Date: 1995 May |
Date Detail:
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Created Date: 1995-06-12 Completed Date: 1995-06-12 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0035623 Medline TA: Mol Pharmacol Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 1006-13 Citation Subset: IM |
Affiliation:
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Medical School, University of Tampere, Finland. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Anthranilic Acids
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pharmacology* Anti-Inflammatory Agents, Non-Steroidal / pharmacology Calcimycin / pharmacology Calcium / metabolism* Calcium Channel Blockers / pharmacology Diphenylamine / analogs & derivatives, pharmacology Flufenamic Acid / pharmacology* Humans Imidazoles / pharmacology Intracellular Fluid / metabolism Ion Transport / drug effects Ketoprofen / pharmacology Manganese / metabolism N-Formylmethionine Leucyl-Phenylalanine / pharmacology Neutrophils / drug effects*, metabolism* Nifedipine / pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Anthranilic Acids; 0/Anti-Inflammatory Agents, Non-Steroidal; 0/Calcium Channel Blockers; 0/Imidazoles; 122-39-4/Diphenylamine; 130495-35-1/1-(2-(3-(4-methoxyphenyl)propoxy)-4-methoxyphenylethyl)-1H-imidazole; 13710-19-5/tolfenamic acid; 17870-85-8/3',5-dichlorodiphenylamine-2-carboxylic acid; 21829-25-4/Nifedipine; 22071-15-4/Ketoprofen; 52665-69-7/Calcimycin; 530-78-9/Flufenamic Acid; 59880-97-6/N-Formylmethionine Leucyl-Phenylalanine; 7439-96-5/Manganese; 7440-70-2/Calcium |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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