A highly selective δ1-opioid receptor antagonist: 7-benzylidenenaltrexone

P. S. Portoghese, M. Sultana, H. Nagase, A. E. Takemori

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182 Scopus citations

Abstract

In guinea pig brain membranes 7-benzylideneraltrexone (BNTX) possesses 100-fold greater affinity (Ki = 0.1 nM) for [3H]DPDPE [3H][D-Pen2,D-Pen5]enkephalin) binding sites (δin1) relative to those of [3H]DSLET ([3H][D-Ser2, Leu5] enkephalin-Thr6) (δ2). The ED50 dose ratio (tail flick) in mice for the antagonism of DPDPE-induced antinociception of BNTX (6.3 pmol i.c.v.) was 7.2, whereas for DSLET, morphine and U69593 it was not significantly different from unity. The fact that there was no correlation of the binding or in vivo data for BNTX with antagonist potency in smooth muscle preparations suggest that the in vitro pharmacologic activity is mediated by δ-opioid subtypes that are different from those in the brain.

Original languageEnglish (US)
Pages (from-to)195-196
Number of pages2
JournalEuropean Journal of Pharmacology
Volume218
Issue number1
DOIs
StatePublished - Jul 21 1992

Keywords

  • 7-Benzylidenenaltrexone (BNTX)
  • Antinociception
  • δ-Opioid receptor subtypes binding

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