Author/Authors :
Sean C. Turner، نويسنده , , William A. Carroll، نويسنده , , Tammie K. White، نويسنده , , Michael E. Brune، نويسنده , , Steven A. Buckner، نويسنده , , Murali Gopalakrishnan، نويسنده , , Adebola Fabiyi، نويسنده , , Michael J. Coghlan، نويسنده , , Victoria E. Scott، نويسنده , , Neil A. Castle، نويسنده , , Anthony V. Daza، نويسنده , , Ivan Milicic، نويسنده , , James P. Sullivan، نويسنده ,
Abstract :
We have discovered a novel series of N-[2-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-naphthalen-1-yl] amides that are potent openers of KATP channels and investigated structure–activity relationships (SAR) around the 1,2-disubstituted naphthyl core. A-151892, a prototype compound of this series, was found to be a potent and efficacious potassium channel opener in vitro in transfected Kir6.2/SUR2B cells and pig bladder strips. Additionally, A-151892 was found to selectively inhibit unstable bladder contractions in vivo in an obstructed rat model of myogenic bladder function
