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Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif

Academic Article
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Overview

authors

  • Frankowski, K. J.
  • Slauson, S. R.
  • Lovell, K. M.
  • Phillips, A. M.
  • Streicher, J. M.
  • Zhou, L.
  • Whipple, D. A.
  • Schoenen, F. J.
  • Prisinzano, T. E.
  • Bohn, Laura
  • Aube, J.

publication date

  • July 2015

journal

  • Bioorganic & Medicinal Chemistry  Journal

subject areas

  • Animals
  • Arrestins
  • Benzamides
  • CHO Cells
  • Chemistry Techniques, Synthetic
  • Cricetulus
  • Drug Evaluation, Preclinical
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • Humans
  • Naltrexone
  • Narcotic Antagonists
  • Receptors, Opioid, kappa
  • Structure-Activity Relationship
  • Sulfonamides
  • Tetrahydroisoquinolines
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Research

keywords

  • Antagonist
  • Kappa opioid receptor
  • Molecular constraint
  • Potency enhancement
  • Tetrahydroisoquinoline
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Identity

PubMed Central ID

  • PMC4468036

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/j.bmc.2014.12.033

PubMed ID

  • 25593096
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Additional Document Info

start page

  • 3948

end page

  • 3956

volume

  • 23

issue

  • 14

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