Biological active analogues of the opioid peptide biphalin: Mixed α/β3-peptides

Adriano Mollica, Francesco Pinnen, Roberto Costante, Marcello Locatelli, Azzurra Stefanucci, Stefano Pieretti, Peg Davis, Josephine Lai, David Rankin, Frank Porreca, Victor J. Hruby

Research output: Contribution to journalArticlepeer-review

35 Scopus citations


Natural residues of the dimeric opioid peptide Biphalin were replaced by the corresponding homo-β3 amino acids. The derivative 1 containing hβ3 Phe in place of Phe showed good μ- and δ-receptor affinities (Kiδ = 0.72 nM; K iμ = 1.1 nM) and antinociceptive activity in vivo together with an increased enzymatic stability in human plasma.

Original languageEnglish (US)
Pages (from-to)3419-3423
Number of pages5
JournalJournal of Medicinal Chemistry
Issue number8
StatePublished - Apr 25 2013

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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