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.

Biological active analogues of the opioid peptide Biphalin: mixed a/b3-peptides

MOLLICA, ADRIANO;PINNEN, Francesco Enrico;COSTANTE, ROBERTO;LOCATELLI, Marcello;STEFANUCCI, AZZURRA;
2013-01-01

Abstract

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.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11564/432283
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