Topographical requirements for delta opioid ligands: The synthesis and biological properties of a cyclic analogue of deltorphin I

Aleksandra Misicka, Gregory Nikiforovich, Andrzej W. Lipkowski, Robert Horvath, Peg Davis, Thomas H. Kramer, Henry I. Yamamura, Victor J. Hruby

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

A cyclic constrained analogue of deltorphin, {A figure is presented} has been proposed on the basis of an energetically favored model of a delta-selective conformation for deltorphin. The biological properties of this synthetic analogue demonstrate that incorporation of a disulfide bridge into Deltorphin I does not affect its high affinity for delta opioid receptors. The analogue shows low receptor selectivity as a result of a large increase in its affinity for mu receptors when compared to the parent deltorphin.

Original languageEnglish (US)
Pages (from-to)547-552
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume2
Issue number6
DOIs
StatePublished - Jun 1992

ASJC Scopus subject areas

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

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