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标题：Uptake of Enalapril by Rabbit Small Intestinal Brush-Border Membrane Vesicles
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作者：Shuji KITAGAWA ; Junko TAKEDA ; Shinji SATO 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1999
卷号：22
期号：7
页码：762-764
DOI：10.1248/bpb.22.762
出版社：The Pharmaceutical Society of Japan
摘要：Uptake of the angiotensin-converting enzyme (ACE) inhibitor enalapril by rabbit small intestinal brush border membrane vesicles was examined. In the presence of an inward H⁺ gradient the uptake of this peptide mimetic drug was accelerated and an overshoot phenomenon was observed. The uptake was more stimulated by higher H⁺ gradient. Initial uptake rate was saturable in the presence of an inward H⁺ gradient, with apparent K_m value of 4.2 mM. These findings suggest the involvement of the H⁺-coupled carrier-mediated transport in the uptake of enalapril. The uptake was inhibited by ACE inhibitor trandolapril but hardly or only slightly inhibited by aminocephalosporins.
关键词：ACE inhibitor;enalapril;small intestine;brush-border membrane vesicle;intestinal absorption