Alpha-amylase inhibitor, CS-1036 binds to serum amylase in a concentration-dependent and saturable manner

(2R,3R,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-3-yl 4-O-(6-deoxy-β-D-glucopyranosyl)-α-D-glucopyranoside (CS-1036), which is an α-amylase inhibitor, exhibited biphasic and sustained elimination with a long t1/2 (18.4-30.0 hours) in rats and monkeys, but exhibited a short t1/2 (3.7-7.9 hours) in hu...

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Veröffentlicht in:	Drug metabolism and disposition 2014-03, Vol.42 (3), p.326-333
Hauptverfasser:	Honda, Tomohiro, Kaneno-Urasaki, Yoko, Ito, Takashi, Kimura, Takako, Matsushima, Nobuko, Okabe, Hiromi, Yamasaki, Atsushi, Izumi, Takashi
Format:	Artikel
Sprache:	eng
Schlagworte:	Adult Animals Blood Proteins - metabolism Disaccharides - blood Disaccharides - pharmacology Dose-Response Relationship, Drug Double-Blind Method Enzyme Inhibitors - blood Enzyme Inhibitors - pharmacology Escherichia coli - genetics Humans Immunoprecipitation Macaca fascicularis Male Pancreatic alpha-Amylases - antagonists & inhibitors Pancreatic alpha-Amylases - blood Pancreatic alpha-Amylases - genetics Protein Binding Pyrrolidines - blood Pyrrolidines - pharmacology Rats Rats, Inbred F344 Rats, Sprague-Dawley Recombinant Proteins Salivary alpha-Amylases - antagonists & inhibitors Salivary alpha-Amylases - blood Salivary alpha-Amylases - genetics Species Specificity Ultrafiltration Young Adult
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