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 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.
Gögelein
H
H
Max-Planck-Institut für Biophysik, Frankfurt/Main, FRG.
Dahlem
D
D
Englert
H C
HC
Lang
H J
HJ
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D002412:Cations; D004553:Electric Conductivity; D005439:Flufenamic Acid / Q000494:pharmacology*; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects*; D008528:Mefenamic Acid / Q000494:pharmacology*; D009539:Nicotinic Acids / Q000494:pharmacology*; D009544:Niflumic Acid / Q000494:pharmacology*; D010179:Pancreas / Q000187:drug effects*; D051381:Rats
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002412:Cations; D007473:Ion Channels; D009539:Nicotinic Acids; D008528:Mefenamic Acid; D009544:Niflumic Acid; D005439:Flufenamic Acid