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

The non-steroidal anti-inflammatory drugs, flufenamic acid, mefenamic acid and niflumic acid, block Ca 2+-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells. Half-maximal inhibition was about 10 μM for flufenamic acid and mefe...

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Bibliographic Details
Published in:FEBS letters 1990-07, Vol.268 (1), p.79-82
Main Authors: Gögelein, H., Dahlem, D., Englert, H.C., Lang, H.J.
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents, Non-Steroidal - pharmacology
Biological and medical sciences
Cations
Electric Conductivity
Exocrine pancreas
Flufenamic acid
Flufenamic Acid - pharmacology
Fundamental and applied biological sciences. Psychology
In Vitro Techniques
Indomethacin
Ion Channels - drug effects
Mefenamic acid
Mefenamic Acid - pharmacology
Nicotinic Acids - pharmacology
Niflumic acid
Niflumic Acid - pharmacology
Non-selective cation channel
pancreas
Pancreas - drug effects
Rat exocrine pancreas
Rats
Vertebrates: digestive system
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Summary:The non-steroidal anti-inflammatory drugs, flufenamic acid, mefenamic acid and niflumic acid, block Ca 2+-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells. Half-maximal inhibition was about 10 μM for flufenamic acid and mefenamic acid, whereas niflumic acid was less potent (IC 50 about 50 μM). Indomethacin, aspirin, diltiazem and ibuprofen (100μM) 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.
ISSN:0014-5793
1873-3468
DOI:10.1016/0014-5793(90)80977-Q