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Characterization of the Efflux Transporter(s) Responsible for Restricting Intestinal Mucosa Permeation of an Acyloxyalkoxy-Based Cyclic Prodrug of the Opioid Peptide DADLE

โœ Scribed by Fuxing Tang; Ronald T. Borchardt


Book ID
110345912
Publisher
Springer US
Year
2002
Tongue
English
Weight
112 KB
Volume
19
Category
Article
ISSN
0724-8741

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The objective of this study was to elucidate the role of P-glycoprotein (P-gp) in restricting the intestinal mucosal permeation of cyclic prodrugs (AOA-DADLE, CA-DADLE, and OMCA-DADLE) of the opioid peptide DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH). In the Caco-2 cell model, the high P app,BL-to-AP /P ap

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โœ Hui Ouyang; Weiqing Chen; Thomas E. Andersen; Bente Steffansen; Ronald T. Borcha ๐Ÿ“‚ Article ๐Ÿ“… 2009 ๐Ÿ› John Wiley and Sons ๐ŸŒ English โš– 286 KB

The objective of this study was to determine the relative importance of metabolism by cytochrome P450 (CYP) enzymes versus efflux by P-glycoprotein (P-gp) in restricting the intestinal mucosal permeation of cyclic prodrugs (AOA-DADLE, CA-DADLE, OMCA-DADLE) of the opioid peptide DADLE (H-Tyr-D-Ala-Gl