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N,n-diethyl-4- (3-hydroxyphenyl)(piperidin-4-yl)amino benzamide derivatives: The development of diaryl amino piperidines as potent delta opioid receptor agonists with in vivo anti-nociceptive activity in rodent models

Academic Article
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Overview

authors

  • Jones, P.
  • Griffin, A. M.
  • Gawell, L.
  • Lavoie, R.
  • Delorme, D.
  • Roberts, Edward
  • Brown, W.
  • Walpole, C.
  • Xiao, W. H.
  • Boulet, J.
  • Labarre, M.
  • Coupal, M.
  • Butterworth, J.
  • St-Onge, S.
  • Hodzic, L.
  • Salois, D.

publication date

  • November 2009

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • We have investigated a series of phenolic diaryl amino piperidine delta opioid receptor agonists, establishing the importance of the phenol functional group and substitution on the piperdine nitrogen for delta agonist activity and selectivity versus the mu and kappa opioid receptors. This study uncovered compounds with improved agonist potency and selectivity compared to the standard, non-peptidic delta agonist SNC-80. In vivo anti-nociceptive activity of analog 8e in two rodent models is discussed, demonstrating the potential of delta agonists to provide a novel mechanism for pain relief.

subject areas

  • Analgesics
  • Animals
  • Benzamides
  • Diphenylamine
  • Disease Models, Animal
  • Mice
  • Piperidines
  • Rats
  • Receptors, Opioid, delta
  • Structure-Activity Relationship
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Research

keywords

  • Antinociception
  • Delta agonism
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2009.09.072

PubMed ID

  • 19800791
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Additional Document Info

start page

  • 5994

end page

  • 5998

volume

  • 19

issue

  • 21

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