Author/Authors :
Paul A. Tuthill، نويسنده , , Pamela R. Seida، نويسنده , , William Barker، نويسنده , , Joel A. Cassel، نويسنده , , Serge Belanger، نويسنده , , Robert N. DeHaven، نويسنده , , Michael Koblish، نويسنده , , Susan L. Gottshall، نويسنده , , Patrick J. Little، نويسنده , , Diane L. DeHaven-Hudkins، نويسنده , , Roland E. Dolle، نويسنده ,
Abstract :
A new class of κ-opioid receptor agonists is described. The design of these agents was based upon energy minimization and structural overlay studies of the generic azepin-2-one structure 3 with the crystal structure of arylacetamide κ agonist 1, ICI 199441. The most active compound identified was ligand 4a (Ki = 0.34 nM), which demonstrated potent antinociceptive activity after oral administration in rodents.
