Identification of arylsulfonamides as Aquaporin 4 inhibitors

被引：119

作者：

Huber, Vincent J.

Tsujita, Mika

Yamazaki, Maya

Sakimura, Kenji

Nakada, Tsutomu

机构：

[1] Niigata Univ, Inst Brain Res, Ctr Integrated Human Brain Sci, Niigata 9518585, Japan

[2] Niigata Univ, Inst Brain Res, Dept Cellular Neurobiol, Niigata 9518585, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 05期

关键词：

aquaporin; 4; AQP4; inhibitors; acetazolamide; AZA; 6-ethoxybenzothiazole-2-sulfonamide; EZA; phloretin;

D O I：

10.1016/j.bmcl.2006.12.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

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.

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页码：1270 / 1273

页数：4

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