Synthesis and biological evaluation of 14-alkoxymorphinans. XIV. 14-Ethoxy-5-methyl substituted indolomorphinans with δ opioid receptor selectivity

Helmut Schmidhammer, Dietmar Daurer, Martina Wieser, Krisztina Monory, Anna Borsodi, Jackie Elliott, John R. Traynor

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13 Citations (Scopus)

Abstract

The 5-methyl and 14-ethoxy substituted analogues (compounds 2 - 4) of the δ opioid receptor antagonist naltrindole showed similar selectivity when compared with the reference drug. Compound 2 was a δ receptor antagonist in the mouse vas deferens preparation (MVD) exhibiting considerably higher selectivity ratios than naltrindole, while compound 4 was found to be a full and potent δ receptor agonist in the MVD.

Original languageEnglish
Pages (from-to)151-156
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume7
Issue number2
DOIs
Publication statusPublished - Jan 21 1997

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ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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