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Issue 23, 2017
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Endomorphin-1 analogs containing α-methyl-β-amino acids exhibit potent analgesic activity after peripheral administration

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Abstract

This study describes the design and synthesis of endomorphin-1 analogs containing C-terminal aromatic α-methyl-β-amino acids and an N-terminal native tyrosine or 2,6-dimethyl-tyrosine. We show that, in comparison with the parent peptide, these analogs exhibit improved bioactivity and blood–brain barrier penetration after intravenous administration, and have a lower tendency to induce constipation and sedation than morphine.

Graphical abstract: Endomorphin-1 analogs containing α-methyl-β-amino acids exhibit potent analgesic activity after peripheral administration

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Publication details

The article was received on 06 May 2017, accepted on 18 May 2017 and first published on 18 May 2017


Article type: Communication
DOI: 10.1039/C7OB01115F
Citation: Org. Biomol. Chem., 2017,15, 4951-4955
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    Endomorphin-1 analogs containing α-methyl-β-amino acids exhibit potent analgesic activity after peripheral administration

    Y. Wang, J. Yang, X. Liu, L. Zhao, D. Yang, J. Zhou, D. Wang, L. Mou and R. Wang, Org. Biomol. Chem., 2017, 15, 4951
    DOI: 10.1039/C7OB01115F

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