Identification of arylsulfonamides as Aquaporin 4 inhibitors

  • Bioorg Med Chem Lett. 2007 Mar 1;17(5):1270-3. doi: 10.1016/j.bmcl.2006.12.010.
Vincent J Huber  1 ,  Mika Tsujita ,  Maya Yamazaki ,  Kenji Sakimura ,  Tsutomu Nakada
Affiliations
  • 1. Center for Integrated Human Brain Science, Brain Research Institute, University of Niigata, 1-757 Asahi Machi Dori, Niigata 951-8585, Japan. [email protected]
PMID: 17178220 DOI: 10.1016/j.bmcl.2006.12.010
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.