Author/Authors :
Kumiko Takeuchi، نويسنده , , William G. Holloway، نويسنده , , Jamie H. McKinzie، نويسنده , , Todd M. Suter، نويسنده , , Michael A. Statnick، نويسنده , , Peggy L. Surface، نويسنده , , Paul J. Emmerson، نويسنده , , Elizabeth M. Thomas، نويسنده , , Miles G. Siegel، نويسنده , , James E. Matt Jr.، نويسنده , , Chad N. Wolfe، نويسنده , , Charles H. Mitch، نويسنده ,
Abstract :
A structurally unique and new class of opioid receptor antagonists (OpRAs) that bear no structural resemblance with morphine or endogenous opioid peptides has been discovered. A series of carboxamido-biaryl ethers were identified as potent receptor antagonists against mu, kappa and delta opioid receptors. The structure–activity relationship indicated para-substituted aryloxyaryl primary carboxamide bearing an amine tether on the distal phenyl ring was optimal for potent in vitro functional antagonism against three opioid receptor subtypes.
