氟芬那酸、甲芬那酸和尼氟酸可抑制大鼠外分泌胰腺中的单个非选择性阳离子通道。
Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas.
作者信息
Gögelein H, Dahlem D, Englert H C, Lang H J
机构信息
Max-Planck-Institut für Biophysik, Frankfurt/Main, FRG.
出版信息
FEBS Lett. 1990 Jul 30;268(1):79-82. doi: 10.1016/0014-5793(90)80977-q.
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.
非甾体抗炎药氟芬那酸、甲芬那酸和尼氟酸，能阻断大鼠胰腺外分泌细胞基底外侧膜外翻片中的Ca2(+)-激活非选择性阳离子通道。氟芬那酸和甲芬那酸的半数最大抑制浓度约为10微摩尔，而尼氟酸的效力较弱（IC50约为50微摩尔）。吲哚美辛、阿司匹林、地尔硫卓和布洛芬（100微摩尔）无此作用。结论是氟芬那酸盐、甲芬那酸盐和尼氟酸盐的抑制作用取决于由氨基桥连接的两个苯环组成的特定结构。
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