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

FEBS Letters

Lang, H.J.¹  Englert, H.C.¹  Gögelein, H.¹  Dahlem, D.¹ 

[1] Max-Planck-Institut für Biophysik, Kennedyallee 70, D-600 Frankfurt/Main 70, FRG

关键词: Mefenamic acid;    Flufenamic acid;    Niflumic acid;    Indomethacin;    Non-selective cation channel;    Rat exocrine pancreas;   

DOI  :  10.1016/0014-5793(90)80977-Q

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 μM for flufenamic acid and mefenamic acid, whereas niflumic acid was less potent (IC₅₀ 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.

【 授权许可】

Unknown