Issue 23, 2017

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

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

Supplementary files

Article information

Article type
Communication
Submitted
06 May 2017
Accepted
18 May 2017
First published
18 May 2017

Org. Biomol. Chem., 2017,15, 4951-4955

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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