Author/Authors :
Andrew A. Mortlock، نويسنده , , Colin Bath، نويسنده , , Roger J. Butlin، نويسنده , , Christine Heys، نويسنده , , Sarah J. Hunt، نويسنده , , Alan C. Reid، نويسنده , , Neil F. Sumner، نويسنده , , Eric K. Tang، نويسنده , , Elaine Whiting، نويسنده , , Campbell Wilson، نويسنده , , Nicola D. Wright، نويسنده ,
Abstract :
A series of novel sulphonamides have been discovered which show high affinity and selectivity for the endothelin ETA receptor. N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(3-methoxy-5-methylpyrazin-2-ylsulfamoyl)benzamide (18) is the most widely investigated compound and is a potent antagonist in vivo when dosed either i. v. or orally, and has prolonged oral duration of action.