descriptionPublicationkeyboard_double_arrow_right Article 01 Mar 2007 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 17, pages 1,270-1,273 (issn: 0960-894X,

Authors: Tsutomu Nakada; Vincent J. Huber; Kenji Sakimura; Mika Tsujita; Maya Yamazaki;

doi: 10.1016/j.bmcl.2006.12.010

pmid: 17178220

Identification of arylsulfonamides as Aquaporin 4 inhibitors

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Abstract

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.

Related Organizations

Niigata University
Japan

Keywords

Aquaporin 4, Osmosis, Sulfonamides, Water, Biological Transport, Transfection, Acetazolamide, Inhibitory Concentration 50, Structure-Activity Relationship, Phloretin, Oocytes, Animals, Humans, Arylsulfonic Acids

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