Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides.

ABSTRACT: Natural residues of the dimeric opioid peptide Biphalin were replaced by the corresponding homo-β(3) amino acids. The derivative 1 containing hβ(3) Phe in place of Phe showed good μ- and δ-receptor affinities (Ki(δ) = 0.72 nM; Ki(μ) = 1.1 nM) and antinociceptive activity in vivo together with an increased enzymatic stability in human plasma.

SUBMITTER: Mollica A 

PROVIDER: S-EPMC3942533 | biostudies-literature | 2013 Apr

REPOSITORIES: biostudies-literature