2. Academic Validation
  3. Identification of arylsulfonamides as Aquaporin 4 inhibitors

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

Affiliation

  • 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.

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