Transport of peptidomimetic thrombin inhibitors with a 3-amidino-phenylalanine structure : Permeability and efflux mechanism in monolayers of a human intestinal cell line (Caco-2)

Peptidomimetic thrombin inhibitors derived from Nalpha-(2-naphthylsulfonyl)-3-amidino-phenylalanine with different basic and acidic substituents were investigated with respect to their intestinal transport behavior. Intestinal permeability coefficients were studied using Caco-2 monolayers and a reve...

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Veröffentlicht in:	Pharmaceutical research 2001-08, Vol.18 (8), p.1110-1118
Hauptverfasser:	KAMM, Walter, HAUPTMANN, Jörg, BEHRENS, Isabel, STÜRZEBECHER, Jörg, DULLWEBER, Frank, GOHLKE, Holger, STUBBS, Milton, KLEBE, Gerhard, KISSEL, Thomas
Format:	Artikel
Sprache:	eng
Schlagworte:	Amidines - chemistry Amidines - metabolism Bioavailability Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Caco-2 Cells Cell culture Cell Membrane Permeability Cell physiology Chemical Phenomena Chemistry, Physical Chromatography, High Pressure Liquid Epithelial Cells - drug effects Epithelial Cells - metabolism Fundamental and applied biological sciences. Psychology Glucose Glycoproteins Hemostatics - antagonists & inhibitors Humans Indicators and Reagents Intestinal Absorption - drug effects Investigations Medical sciences Membrane and intracellular transports Metabolism Metabolites Molecular and cellular biology Molecular Mimicry Peptides Permeability Pharmacology. Drug treatments Phenylalanine - analogs & derivatives Phenylalanine - chemistry Phenylalanine - metabolism Solubility Spectrometry, Fluorescence Spectrophotometry, Ultraviolet Structure-Activity Relationship Temperature Thrombin - antagonists & inhibitors
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