FLUFENAMIC ACID, MEFENAMIC-ACID AND NIFLUMIC ACID INHIBIT SINGLE NONSELECTIVE CATION CHANNELS IN THE RAT EXOCRINE PANCREAS

被引:185
作者
GOGELEIN, H [1 ]
DAHLEM, D [1 ]
ENGLERT, HC [1 ]
LANG, HJ [1 ]
机构
[1] MAX PLANCK INST BIOPHYS,W-6000 FRANKFURT 70,GERMANY
关键词
Flufenamic acid; Indomethacin; Mefenamic acid; Niflumic acid; Non-selective cation channel; Rat exocrine pancreas;
D O I
10.1016/0014-5793(90)80977-Q
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
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. © 1990.
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页码:79 / 82
页数:4
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