title: N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: a Novel Class of Selective, Nonbasic, Nitrogen-Containing κ-Opioid Receptor Ligands.
abstract: Herein we report that N-alkyl-octahydroisoquinolin-1-one-8-carboxamides are a novel class of readily-synthesized, selective ϰ-opioid receptor (KOR) ligands. A striking feature of this class of compounds is the absence of any basic nitrogen atoms. Many of these compounds have demonstrated exclusive affinity for the KOR over not only the δ-opioid receptor (DOR) and the μ-opioid receptor (MOR), but 38 other GPCR targets as well. The general binding affinity of this class of compounds for the KOR combined with a streamlined route for analog synthesis provide strong motivation for pursuing this interesting new scaffold as a basis toward new probes targeting the KOR.
authors: Department of Medicinal Chemistry, University of Kansas, 2121 Simons Drive, Lawrence, Kansas 66047.
authors: Kevin J
authors: KJ
authors: Frankowski
authors: Partha
authors: P
authors: Ghosh
authors: Vincent
authors: V
authors: Setola
authors: Thuy B
authors: TB
authors: Tran
authors: Bryan L
authors: BL
authors: Roth
authors: Jeffrey
authors: J
authors: Aubé