Jump to main content
Jump to site search


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 a 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.

Back to tab navigation
Please wait while Download options loads

Supplementary files

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, Accepted Manuscript
  •   Request permissions

    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. Mu and R. Wang, Org. Biomol. Chem., 2017, Accepted Manuscript , DOI: 10.1039/C7OB01115F

Search articles by author