Coumarinic acid-based cyclic prodrugs of opioid peptides that exhibit metabolic stability to peptidases and excellent cellular permeability

作者: Olafur S. Gudmundsson , Giovanni M. Pauletti , Wei Wang , Daxian Shan , Huijuan Zhang

DOI: 10.1023/A:1018828207920

关键词:

摘要: Purpose. To evaluate the cellular permeation characteristics and chemical enzymatic stability of coumarinic acid-based cyclic pro-drugs \(\underset{\raise0.3em\hbox{$\smash{\scriptscriptstyle-}$}}{1} \) \(\underset{\raise0.3em\hbox{$\smash{\scriptscriptstyle-}$}}{2} opioid peptides [Leu5]-enkephalin (H-Tyr-Gly-Gly-Phe-Leu-OH) DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH), respectively.

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