Alamethicin for using in bioavailability studies? - Re-evaluation of its effect

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• 作者：Maren Vollmer ^{Maren.Vollmer@chemie.uni-hamburg.de} ; Mirko Klingebiel ^{mikl1710@kdwelt.de} ; Sascha Rohn ; ^{rohn@chemie.uni-hamburg.de} ; Ronald Maul ^{maul@chemie.uni-hamburg.de}
• 关键词：Clint ; intrinsic clearance ; Clint app. ; apparent intrinsic clearance ; DAD ; diod array detector ; DMSO ; dimethyl sulfoxide ; ER ; endoplasmic reticulum ; fu ; unbound fraction of a drug in the microsomal incubation mixture ; HPLC ; high performance liquid chromatography ; Km ; Michaelis-Menten constant ; P ; partition coefficient ; S ; substrate concentration ; UDP ; uridine diphosphate ; UDPGA ; uridine 5&prime ; -diphosphoglucuronic acid trisodium salt ; UGT ; UDP-glucuronosyltransferase ; v ; velocity ; Vmax ; maximal
• 刊名：Toxicology in Vitro
• 出版年：2017
• 出版时间：March 2017
• 年：2017
• 卷：39
• 期：Complete
• 页码：111-118
• 全文大小：609 K
• 卷排序：39

文摘

Alamethicin affects glucuronidation of phenolic substrates. Different alamethicin concentrations lead to different depletion rates. A maximal glucuronidation activity could be assigned to different but distinct alamethicin concentrations. Alamethicin application is a crucial factor to deduce enzyme kinetic parameter from in vitro metabolic assays. Correlations between the substrate lipophilicity and alamethicin effect were not detected.