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. Epub 2006 Dec 15.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetazolamide / pharmacology
  • Animals
  • Aquaporin 4 / antagonists & inhibitors*
  • Arylsulfonic Acids / pharmacology*
  • Biological Transport / drug effects
  • Humans
  • Inhibitory Concentration 50
  • Oocytes
  • Osmosis
  • Phloretin / pharmacology
  • Structure-Activity Relationship
  • Sulfonamides / pharmacology*
  • Transfection
  • Water / metabolism

Substances

  • Aquaporin 4
  • Arylsulfonic Acids
  • Sulfonamides
  • Water
  • Acetazolamide
  • Phloretin