Synthesis and evaluation of novel peripherally restricted κ-opioid receptor agonists

Virendra Kumar,Deqi Guo,Joel A. Cassel,Jeffrey D. Daubert,Robert N. DeHaven,Diane L. DeHaven-Hudkins,Erin K. Gauntner,Susan L. Gottshall,Susan L. Greiner,Michael Koblish,Patrick J. Little,Erik Mansson,Alan L. Maycock

Bioorganic & Medicinal Chemistry Letters（2005）

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摘要

Analogs (3) of parent compound 1 (R=H) were prepared as novel potent kappa receptor agonists with improved peripheral restriction indices (platform sedation ED50/writhing ED50).

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关键词

κ-opioid receptor agonists,Peripherally restricted

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