Synthesis and evaluation of novel peripherally restricted κ-opioid receptor agonists
A series of 3-substituted analogs (3) of the parent κ agonist, 1, were prepared to limit access to the central nervous system. With the exception of compound 3j, all other compounds bound to the human κ opioid receptor with high affinity (Ki =
Kumar, Virendra,Guo, Deqi,Cassel, Joel A.,Daubert, Jeffrey D.,DeHaven, Robert N.,DeHaven-Hudkins, Diane L.,Gauntner, Erin K.,Gottshall, Susan L.,Greiner, Susan L.,Koblish, Michael,Little, Patrick J.,Mansson, Erik,Maycock, Alan L.
p. 1091 - 1095
(2007/10/03)
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