Biological properties of Phe°-opioid peptide analogues

Andrzej W. Lipkowski, Aleksandra Misicka, Keiko Hosohata, Peg Davis, Henry I. Yamamura, Frank Porreca, Victor J. Hruby

Research output: Contribution to journalArticlepeer-review

2 Scopus citations


Biological properties of new analogues, which represent Phe°-propeptides of a variety of opioid peptides, are described. All Phe°-opioid analogues expressed both receptor binding affinities and in vitro biological activities at least at the level of the primary opioid peptides. Surprisingly, some of the propeptides expressed slightly higher activity than the primary opioid peptides. Nevertheless, no significant shift in receptor selectivity was observed, which indicate that these Phe°-analogues undoubtedly are propeptides. The possible role of membrane proteolytic enzymes associated with opioid receptors in transformation of propeptides is discussed.

Original languageEnglish (US)
Pages (from-to)969-972
Number of pages4
JournalLife Sciences
Issue number8
StatePublished - Jan 12 2001


  • Drug design
  • Opioid peptides
  • Prodrugs

ASJC Scopus subject areas

  • General Biochemistry, Genetics and Molecular Biology
  • Pharmacology, Toxicology and Pharmaceutics(all)


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