کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2505990 | 1557500 | 2008 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Protein concentration and pH affect the apparent P-glycoprotein-ATPase activation kinetics
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
علوم دارویی
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چکیده انگلیسی
Reliable predictions of the role of P-glycoprotein in the pharmacokinetics are needed already at the early stage of drug development. In order to obtain meaningful in vitro-in vivo scaling factors, it is essential to know the factors affecting the in vitro results. In this study, the apparent P-glycoprotein-ATPase activation kinetics were determined using the cell membrane fraction of human MDR1-transfected insect cells. The apparent affinities to P-glycoprotein of basic verapamil and quinidine were higher at pH 7.4 than at pH 6.8. However, this shift in pH did not have a significant effect on the apparent affinity of acidic monensin. The protein concentration used in the assay did not affect the apparent activator affinities, but was inversely related to the maximum activation achieved. Thus, pH and protein concentration should be taken into account when interpreting the Pgp-ATPase data.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 346, Issues 1â2, 4 January 2008, Pages 169-172
Journal: International Journal of Pharmaceutics - Volume 346, Issues 1â2, 4 January 2008, Pages 169-172
نویسندگان
Aki T. Heikkinen, Jukka Mönkkönen,