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Issue 8, 2018
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Design, synthesis and biological profile of mixed opioid agonist/N-VGCC blocker peptides

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Abstract

In this paper we reported the synthesis and the in vitro and the in vivo biological evaluation of linear pseudo-peptides incorporating the N-VGCC blocker tripeptide Phe-NMe-Leu-Tyr(OBz)-NtBu and the biphalin pharmacophore Tyr-D-Ala-Gly-Phe. The novel sequences have been designed by using amino acids of different length to join the two pharmacophores and explore the structure–activity relationships of the novel compounds.

Graphical abstract: Design, synthesis and biological profile of mixed opioid agonist/N-VGCC blocker peptides

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Publication details

The article was received on 14 Dec 2017, accepted on 02 Mar 2018 and first published on 05 Mar 2018


Article type: Letter
DOI: 10.1039/C7NJ04969B
Citation: New J. Chem., 2018,42, 5656-5659
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    Design, synthesis and biological profile of mixed opioid agonist/N-VGCC blocker peptides

    A. Stefanucci, E. Novellino, G. Macedonio, M. P. Dimmito, S. Mirzaie, F. Caldas Cardoso, R. Lewis, F. Zádor, A. I. Erdei, S. Dvorácskó, C. Tömböly, S. Benyhe, S. Pieretti, P. Minosi and A. Mollica, New J. Chem., 2018, 42, 5656
    DOI: 10.1039/C7NJ04969B

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