4.5 Article

Identification of arylsulfonamides as Aquaporin 4 inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 5, Pages 1270-1273

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.12.010

Keywords

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

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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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