Para-substituted phenylalanine-4 analogues of [L-Ala3]DPDPE: Highly selective δ opioid receptor ligands

Ronald C. Haaseth, Teresa Zalewska, Peg Davis, Henry I. Yamamura, Frank Porreca, Victor J. Hruby

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

Several para-substituted Phe4 analogues of the δ1-selective antagonist [L-Ala3]DPDPE (DPADPE) were prepared and evaluated for their brain-binding and in vitro pharmacological effects. Unlike the p-haloPhe4 analogues of DPDPE and the deltorphins, similar analogues of DPADPE with electron-withdrawing groups substituted at the para-position of the Phe4 aromatic ring did not all have increased potency and selectivity for δ opioid receptors, but all retained high potency and selectivity for δ opioid receptors greater than DPDPE.

Original languageEnglish (US)
Pages (from-to)171-177
Number of pages7
JournalJournal of Peptide Research
Volume50
Issue number3
DOIs
StatePublished - 1997

Keywords

  • Brain binding
  • Enkephalin analogues
  • MVD and GPI opioid activity
  • Receptor selective
  • δ opioid ligands

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology

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