In vitro and in vivo activity of cyclopeptide Dmt-c[d-Lys-Phe-Asp]NH 2 , a mu opioid receptor agonist biased toward β-arrestin.

Katarzyna Gach-Janczak,Justyna Piekielna-Ciesielska,Anna Adamska-Bartłomiejczyk,Karol Wtorek,Federica Ferrari,Girolamo Calo',Agata Szymaszkiewicz,Joanna Piasecka-Zelga,Anna Janecka

Peptides（2018）

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摘要

•Cyclopeptide Dmt-c[d-Lys-Phe-Asp]NH2 is a mu/delta bifunctional opioid analog.•Pharmacological profile of this analog was determined in vitro and in vivo.•Dmt-c[d-Lys-Phe-Asp]NH2 is the first reported opioid peptide biased toward β-arrestin.

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关键词

Cyclic opioid peptides,Binding assay,Calcium mobilization assay,Bioluminescence resonance energy transfer assay,Hot-plate test,Whole gastrointestinal transit test

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