Synthesis and biological activities of YkFA analogues: Effects of position 4 substitutions and altered ring size on in vitro opioid activity

John E. Burden, Peg Davis, Frank Porreca, Arno F. Spatola

Research output: Contribution to journalArticle

12 Scopus citations

Abstract

Substitution in position 4 of the potent opioid peptide YkFA with aliphatic hydrophobic residues resulted in compounds that retained low nanomolar activities at both μ and δ opioid receptors, while ring contraction by incorporation of diaminobutyric acid in position 2 resulted in a more pronounced decrease in potency at both receptors for the ψ[CH2NH] pseudopeptide as compared to the all amide parent.

Original languageEnglish (US)
Pages (from-to)213-216
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number2
DOIs
StatePublished - Jan 21 2002

ASJC Scopus subject areas

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

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