Identification of arylsulfonamides as Aquaporin 4 inhibitors

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 μM in an in vitro functional assay. AZA was found to have an IC50 against AQP4 of 0.9 μM. Phloretin was inactive under the same conditions.

A series of carbonic anhydrase inhibitors, including AZA, have been found to inhibit AQP4 mediated water transport in an in vitro functional assay. AZA has an apparent IC50 = 0.9 μM against human AQP4-M23.Figure optionsDownload as PowerPoint slide