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

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Gögelein,  Heinz
Department of Physiology, Max Planck Institute of Biophysics, Max Planck Society;

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Dahlem,  D.
Department of Physiology, Max Planck Institute of Biophysics, Max Planck Society;

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Englert,  H.C.
Department of Physiology, Max Planck Institute of Biophysics, Max Planck Society;

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Lang,  H.J.
Department of Physiology, Max Planck Institute of Biophysics, Max Planck Society;

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Citation

Gögelein, H., Dahlem, D., Englert, H., & Lang, H. (1990). Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas. FEBS Letters, 268(1), 79-82. doi:10.1016/0014-5793(90)80977-q.


Cite as: http://hdl.handle.net/21.11116/0000-0007-DDD5-0
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.