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Discovery of small molecule kappa opioid receptor agonist and antagonist chemotypes through a HTS and Hit refinement strategy

Academic Article
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Overview

authors

  • Frankowski, K. J.
  • Hedrick, M. P.
  • Gosalia, P.
  • Li, K. L.
  • Shi, S. H.
  • Whipple, D.
  • Ghosh, P.
  • Prisinzano, T. E.
  • Schoenen, F. J.
  • Su, Y.
  • Vasile, S.
  • Sergienko, E.
  • Gray, W.
  • Hariharan, S.
  • Milan, L.
  • Heynen-Genel, S.
  • Mangravita-Novo, A.
  • Vicchiarelli, M.
  • Smith, L. H.
  • Streicher, J. M.
  • Caron, M. G.
  • Barak, L. S.
  • Bohn, Laura
  • Chung, T. D. Y.
  • Aube, J.

publication date

  • March 2012

journal

  • ACS Chemical Neuroscience  Journal

abstract

  • Herein we present the outcome of a high throughput screening (HTS) campaign-based strategy for the rapid identification and optimization of selective and general chemotypes for both kappa (κ) opioid receptor (KOR) activation and inhibition. In this program, we have developed potent antagonists (IC(50) < 120 nM) or agonists of high binding affinity (K(i) < 3 nM). In contrast to many important KOR ligands, the compounds presented here are highly modular, readily synthesized and, in most cases, achiral. The four new chemotypes hold promise for further development into chemical tools for studying the KOR or as potential therapeutic lead candidates.
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Research

keywords

  • Kappa opioid receptor agonist
  • high-throughput screening
  • kappa opioid receptor antagonist
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Identity

PubMed Central ID

  • PMC3378255

International Standard Serial Number (ISSN)

  • 1948-7193

Digital Object Identifier (DOI)

  • 10.1021/cn200128x

PubMed ID

  • 22737280
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Additional Document Info

start page

  • 221

end page

  • 236

volume

  • 3

issue

  • 3

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