Autor: |
Mollica, Adriano, Pinnen, Francesco, Costante, Roberto, Locatelli, Marcello, Stefanucci, Azzurra, Pieretti, Stefano, Davis, Peg, Lai, Josephine, Rankin, David, Porreca, Frank, Hruby, Victor J. |
Zdroj: |
Journal of Medicinal Chemistry; 20240101, Issue: Preprints |
Abstrakt: |
Natural residues of the dimeric opioid peptide Biphalin were replaced by the corresponding homo-β3amino acids. The derivative 1containing hβ3Phe in place of Phe showed good μ- and δ-receptor affinities (Kiδ= 0.72 nM; Kiμ= 1.1 nM) and antinociceptive activity in vivo together with an increased enzymatic stability in human plasma. |
Databáze: |
Supplemental Index |
Externí odkaz: |
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