Mollica, Adriano; Pinnen, Francesco; Costante, Roberto; Locatelli, Marcello; Stefanucci, Azzurra; Pieretti, Stefano; Davis, Peg; Lai, Josephine; Rankin, David; Porreca, Frank; Hruby, Victor J
Journal of medicinal chemistry,
2013-Apr-25, 20130425, Letnik:
56, Številka:
8
Journal Article
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.
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