Referenced in: none

Automatically associated channels: Kir6.2

Title: Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.

Authors: Sean C Turner, William A Carroll, Tammie K White, Michael E Brune, Steven A Buckner, Murali Gopalakrishnan, Adebola Fabiyi, Michael J Coghlan, Victoria E Scott, Neil A Castle, Anthony V Daza, Ivan Milicic, James P Sullivan

Journal, date & volume: Bioorg. Med. Chem. Lett., 2003 May 19 , 13, 1741-4

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/12729655

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 K(ATP) 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