Identification of arylsulfonamides as Aquaporin 4 inhibitors
Identification of arylsulfonamides as Aquaporin 4 inhibitors
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DOI：
10.1016/j.bmcl.2006.12.010
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发表时间：
2007-03-01
影响因子：
2.7
通讯作者：
Nakada, Tsutomu
中科院分区：
文献类型：
--
作者：
Huber, Vincent J.;Tsujita, Mika;Nakada, Tsutomu
在一项体外功能测定中，发现碳酸酐酶抑制剂乙酰唑胺（AZA）、乙氧苯唑胺（EZA）和4 - 乙酰氨基苯磺酰胺在20μM浓度下，分别抑制人水通道蛋白4 - M23介导的水转运80%、68%和23%。发现乙酰唑胺对水通道蛋白4的半数抑制浓度（IC50）为0.9μM。根皮素在相同条件下无活性。（c）2006爱思唯尔有限公司。保留所有权利。
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 mu M in an in vitro functional assay. AZA was found to have an IC50 against AQP4 of 0.9 mu M. Phloretin was inactive under the same conditions. (c) 2006 Elsevier Ltd. All rights reserved.