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 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.
Huber
Vincent J
VJ
Center for Integrated Human Brain Science, Brain Research Institute, University of Niigata, 1-757 Asahi Machi Dori, Niigata 951-8585, Japan. vjhuber@bri.niigata-u.ac.jp
Tsujita
Mika
M
Yamazaki
Maya
M
Sakimura
Kenji
K
Nakada
Tsutomu
T
D000086:Acetazolamide / Q000494:pharmacology; D000818:Animals; D051401:Aquaporin 4 / Q000037:antagonists & inhibitors*; D017739:Arylsulfonic Acids / Q000494:pharmacology*; D001692:Biological Transport / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D009865:Oocytes; D009995:Osmosis; D010693:Phloretin / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology*; D014162:Transfection; D014867:Water / Q000378:metabolism
D051401:Aquaporin 4; D017739:Arylsulfonic Acids; D013449:Sulfonamides; D014867:Water; D000086:Acetazolamide; D010693:Phloretin