[3H]phenamil, a radiolabelled diuretic for the analysis of the amiloride-sensitive Na+ channels in kidney membranes.
[3H]phenamil, a radiolabelled diuretic for the analysis of the amiloride-sensitive Na+ channels in kidney membranes.
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[3H]phenamil，一种放射性标记利尿剂，用于分析肾膜中阿米洛利敏感的 Na 通道。
DOI：
10.1016/0006-291x(86)90937-x
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发表时间：
1986
影响因子：
3.1
通讯作者：
M. Lazdunski
中科院分区：
文献类型：
--
作者：
P. Barbry;C. Frelin;P. Vigne;E. Cragoe;M. Lazdunski
通过~(22)Na~+摄取实验，研究了阿米洛利及其衍生物与猪肾膜钠离子通道的相互作用。所测不同分子的效价顺序为：非那米>；苯并胺>；阿米洛利；乙基异丙基阿米洛利。制备了标记的非那米，并用于滴定猪肾膜上的Na+通道。动力学实验、平衡结合实验和非标记非那米的竞争实验表明，非那米可识别一组结合位点，Kd值为20 nM，最大结合容量为11.5pmol/mg蛋白质。在[~3H]非那米竞争实验中测试的不同阿米洛利类似物的药效顺序与心尖Na+通道抑制22Na+摄取的药效顺序相同。
The interaction of amiloride and amiloride derivatives with the Na+channels of pig kidney membranes was studied from22Na+uptake experiments. The order of potency of the different molecules tested is: phenamil > benzamil > amiloride, ethylisopropylamiloride. [3H]labelled phenamil was prepared and used to titrate Na+channels in pig kidney membranes. Kinetics experiments, equilibrium binding studies and competition experiments between [3H]phenamil and unlabelled phenamil indicate that phenamil recognizes a single family of binding sites with a Kdvalue of 20 nM and a maximum binding capacity of 11.5 pmol/mg of protein. The order of potency of different amiloride analogs tested in [3H]phenamil competition experiments is identical to that found for the inhibition of22Na+uptake by apical Na+channels.
一种简单而灵敏的程序，用于测量异质膜囊泡群体中通过离子特异性通道的同位素通量。
DOI：
--
发表时间：
1983
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Garty,H;Rudy,B;Karlish,SJ
通讯作者：
Karlish,SJ