Inhibition of the antisecretory effects of [D-Ala2,D-Leu5]enkephalin in the guinea-pig ileum by a selective δ opioid antagonist

Rakesh Vinayek, David R. Brown*, Richard J. Miller

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

The novel opioid antagonist [dially-Tyr1,(CH2)S-Phe4,Leu5]enkephalin (M154,129) was examined for its ability to block the antisecretory effects of [D-Ala2,D-Leu5]enkephalin (DADLE) in isolated mucosal segments of the guinea-pig ileum, actions mediated predominantly through the δ opiate receptor. DADLE reduced transepithelial potential difference and short-circuit current (ED50 18 nM); these effects were competitively antagonized by M154,129 with a Ke value of 746 nM. These results are consistent with others demonstrating that M154,129 is a relatively selective although not highly potent blocker of δ opiate receptors.

Original languageEnglish (US)
Pages (from-to)159-161
Number of pages3
JournalEuropean Journal of Pharmacology
Volume94
Issue number1-2
DOIs
StatePublished - Oct 14 1983

Keywords

  • (CH)S-Phe
  • D-Leu]enkephalin
  • Leu]enkephalin
  • [D-Ala
  • [Dially-Tyr
  • δ Opiate receptor Intestinal electrolyte transport

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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