Abstract
Further structure activity relationship studies on a previously reported 8-azabicyclo[3.2.1]octan-3-yloxy-benzamide series of potent and selective kappa opioid receptor antagonists is discussed. Modification of the pendant N-substitution to include a cyclohexylurea moiety produced analogs with greater in vitro opioid and hERG selectivity such as 12 (κ IC 50 = 172 nM, μ:κ ratio = 93, δ:κ ratio = >174, hERG IC 50 = >33 μM). Changes to the linker conformation and identity as well as to the benzamide ring moiety were also investigated.
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