A modified coumarinic acid-based cyclic prodrug of an opioid peptide: Its enzymatic and chemical stability and cell permeation characteristics

To evaluate the chemical/enzymatic stability and the cell permeation characteristics of the modified coumarinic acid-based cyclic prodrug 2 of DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH), which has an aldehyde equivalent (oxymethyl) inserted between the phenolic group of the promoiety and the carboxylic ac...

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Veröffentlicht in:	Pharmaceutical research 2002-06, Vol.19 (6), p.794-801
Hauptverfasser:	HUI OUYANG, FUXING TANG, SIAHAAN, Teruna J, BORCHARDT, Ronald T
Format:	Artikel
Sprache:	eng
Schlagworte:	Acids - chemistry Acids - metabolism Amino acids Animals Bioavailability Biological and medical sciences Caco-2 Cells Cell Line Coumarins - chemistry Coumarins - pharmacokinetics Dogs Drugs Enkephalin, Leucine-2-Alanine - chemistry Enkephalin, Leucine-2-Alanine - pharmacokinetics Enzyme Stability - drug effects Enzyme Stability - physiology General pharmacology Genes, MDR - physiology Humans Liver - enzymology Male Medical sciences Mitochondrial Proteins Narcotics Penicillin Peptides Permeability - drug effects Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Plasma Prodrugs - chemistry Prodrugs - pharmacokinetics Rats Rats, Sprague-Dawley Ribosomal Proteins - metabolism Saccharomyces cerevisiae Proteins
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