芳基磺胺作为水通道蛋白4抑制剂的鉴定。
Identification of arylsulfonamides as Aquaporin 4 inhibitors.
作者信息
Huber Vincent J, Tsujita Mika, Yamazaki Maya, Sakimura Kenji, Nakada Tsutomu
机构信息
Center for Integrated Human Brain Science, Brain Research Institute, University of Niigata, 1-757 Asahi Machi Dori, Niigata 951-8585, Japan.
出版信息
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1270-3. doi: 10.1016/j.bmcl.2006.12.010. Epub 2006 Dec 15.
Carbonic anhydrase inhibitors AZA, EZA, and 4-acetamidobenzsulfonamide were found to inhibit human AQP4-M23 mediated water transport by 80%, 68%, and 23%, respectively, at 20 microM in an in vitro functional assay. AZA was found to have an IC50 against AQP4 of 0.9 microM. Phloretin was inactive under the same conditions.
在体外功能试验中，发现碳酸酐酶抑制剂氮杂环丙烷（AZA）、依他尼酸（EZA）和4-乙酰氨基苯磺酰胺在20微摩尔浓度下分别抑制人水通道蛋白4-M23（AQP4-M23）介导的水转运80%、68%和23%。发现AZA对AQP4的半数抑制浓度（IC50）为0.9微摩尔。在相同条件下，根皮素无活性。
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