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.File in questo prodotto:
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Journal of Medicinal Chemistry (2013) 56 3419−3423.pdf
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