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PMID: 1696554 Published · ppublish English Journal Article

Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas.

FEBS letters ·Vol. 268 ·No. 1 ·1990-07-30 ·Pages 79-82

Gögelein H, Dahlem D, Englert HC, Lang HJ

Abstract

The non-steroidal anti-inflammatory drugs, flufenamic acid, mefenamic acid and niflumic acid, block Ca2(+)-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells. Half-maximal inhibition was about 10 microM for flufenamic acid and mefenamic acid, whereas niflumic acid was less potent (IC50 about 50 microM). Indomethacin, aspirin, diltiazem and ibuprofen (100 microM) had not effect. It is concluded that the inhibitory effect of flufenamate, mefenamate and niflumate is dependent on the specific structure, consisting of two phenyl rings linked by an amino bridge.

MeSH Terms
Animals Anti-Inflammatory Agents, Non-Steroidal/pharmacology Cations Electric Conductivity Flufenamic Acid/pharmacology In Vitro Techniques Ion Channels/drug effects Mefenamic Acid/pharmacology Nicotinic Acids/pharmacology Niflumic Acid/pharmacology Pancreas/drug effects Rats
Chemicals
Anti-Inflammatory Agents, Non-Steroidal Cations Ion Channels Nicotinic Acids Mefenamic Acid Niflumic Acid Flufenamic Acid
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Gögelein H
Max-Planck-Institut für Biophysik, Frankfurt/Main, FRG.
Dahlem D
Englert H C
Lang H J
Article Info
Journal
FEBS letters
Abbr.
FEBS Lett
ISSN
0014-5793
Published
1990-07-30
Pages
79-82
Language
English
Region
England
NLM ID
0155157
Subset
IM
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