Y. Wang, Junxian Yang, Xin Liu
Jun 14, 2017
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0
Influential Citations
6
Citations
Journal
Organic & biomolecular chemistry
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.